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Antineoplastic agents r

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  • R-(-)-gossypol acetic acid - The orally bioavailable solvate of the R-(-) enantiomer of gossypol and acetic acid with potential antineoplastic activity. As a BH3 mimetic, R-(-)-gossypol binds to the hydrophobic surface binding groove BH3 of the anti-apoptotic proteins Bcl-2 and Bcl-xL, blocking their heterodimerization with pro-apoptotic members of the Bcl-2 family of proteins such as Bad, Bid, and Bim; this may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Racemic gossypol is a polyphenolic compound isolated from cottonseed.
  • Rabusertib - An inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine-threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types.
  • Racemetyrosine/methoxsalen/phenytoin/sirolimus sm-88 - A combination agent containing racemetyrosine, methoxsalen, phenytoin and sirolimus, with potential antineoplastic activity. Upon administration of racemetyrosine/methoxsalen/phenytoin/sirolimus SM-88, racemetyrosine, being a dysfunctional and modified form of the non-essential amino acid tyrosine, is specifically taken up by cancer cells through the transporter L-amino acid transferase-1 (LAT1; CD98). As a tyrosine derivative and faulty amino acid protein building block, racemetyrosine prevents protein synthesis in cancer cells. Specifically, this prevents mucin-1 (MUC1) protein synthesis. MUC1 is highly overexpressed by most cancer cells and regulates the increased reactive oxygen species (ROS) in cancer cells created from the altered metabolism that cancer cells utilize, by upregulating key antioxidant defenses and preventing ROS-mediated apoptosis. In the absence of MUC1, ROS levels are increased, leading to an increase in oxidative stress, and induction of apoptosis. Also, being a protective transmembrane protein, MUC1 is part of the protective layer on the outside of cancer cells and plays a key role in shielding the cancer cell from the immune system. The loss of MUC1 compromises the cell membrane, thereby making the cancer cell more vulnerable to be recognized and attacked by the immune system. Rapamycin, a mammalian target of rapamycin (mTOR) inhibitor, increases the cancer cells' need for tyrosine uptake and increases the uptake of racemetyrosine by LAT1. Phenytoin stimulates the release of reactive lipid species by the liver which accumulate in the tumor microenvironment (TME) and are taken up by cancer cells, thereby further increasing ROS within the cancer cell and increasing oxidative-related apoptosis. Mehoxsalen promotes toxic electron transfer and increases melanin, increases oxidative reactions and production of ROS. This further stimulates oxidative stress-mediated apoptosis. Normal cells do not regularly take up certain non-essential amino acids, such as tyrosine, but readily convert phenylalanine to tyrosine, so normal healthy cells are not expected to consume racemetyrosine.
  • Racotumomab - An anti-idiotype murine monoclonal antibody (MoAb) specific to P3 MoAb with anti-metastatic effect. Racotumomab binds to the idiotype region of P3 MoAb and functionally mimics the three-dimensional structure of N-glycolyl ceramides of mono-sialyl lactose, the antigenic target of P3. As a result, this anti-idiotype antibody may stimulate the host immune system to elicit humoral and cellular immune responses against tumor cells expressing NeuGc-GM3 gangliosides, which are expressed in a wide variety of tumor cells.
  • Rad51 inhibitor cyt-0851 - An orally bioavailable inhibitor of the DNA damage repair protein RAD51, with potential antineoplastic and sensitizing activities. Upon oral administration, the RAD51 inhibitor CYT-0851 targets, binds to and inhibits the activity of RAD51. This prevents RAD51-mediated DNA damage repair in susceptible tumor cells and induces tumor cell apoptosis. RAD51, the central protein involved in homologous repair (HR) of DNA double-strand breaks (DSBs), is overexpressed in many tumor cell types.
  • Radgocitabine - An analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Upon administration, radgocitabine is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis.
  • Radgocitabine hydrochloride - The hydrochloride salt form of radgocitabine, an analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Upon administration, radgocitabine is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis.
  • Radiolabeled cc49 - A radioimmunoconjugate comprised of a humanized monoclonal antibody with antitumor activity. The monoclonal antibody CC49 is developed from the murine monoclonal antibody B72.3 and is humanized by grafting the hypervariable regions onto the variable light (VL) and variable heavy (VH) frameworks of the monoclonal antibodies LEN and 21/28' CL. The resultant antibody binds the pancarcinoma tumor-associated glycoprotein (TAG)-72 with high affinity. Furthermore, the antibody is commonly radiolabeled resulting in an effective agent for use in radioimmunotherapy for treatment of cancer.
  • Radium bromatum - An orally available homeopathic preparation with potential radioprotective activities. Upon administration, radium bromatum may reduce the occurrence of, and ameliorate the symptoms associated with radiation-induced dermatitis.
  • Radium ra 223 dichloride - A radiopharmaceutical composed of the dichloride salt of the alpha-emitting isotope radium Ra 223, with antineoplastic activity. Like calcium, radium targets bone tissue and preferentially accumulates in osteoblastic lesions, such as those seen in areas of bone metastases. Radium Ra 223 forms complexes with hydroxyapatite and becomes incorporated into the bone matrix. The radioisotope Ra 223 kills bone cancer cells through local emission of high energy alpha particles, causing DNA double-strand breaks and tumor regression in the skeleton. The short range effects of alpha emission allows for localized DNA damage with limited toxicity to nearby healthy bone tissue.
  • Radium ra 224-labeled calcium carbonate microparticles - A radiopharmaceutical composed of biodegradable calcium carbonate microspheres labeled with the alpha-emitting radioisotope radium Ra 224, with antineoplastic activity. Upon intraperitoneal (IP) administration of the radium Ra 224-labeled calcium carbonate microparticles, Ra 224 kills tumor cells through local emission of high energy alpha particles, causing DNA double-strand breaks. The short range effects of alpha emission allows for localized DNA damage with limited toxicity to nearby healthy tissue.
  • Radix angelicae sinensis/radix astragali herbal supplement - A traditional Chinese medicine comprising of Radix Angelicae Sinensis (RAS) and Radix Astragali (RA), with potential anti-inflammatory, immunostimulatory, neuroprotective, anti-hepatotoxic and antineoplastic activities. The main chemical constituents of RAS include ferulic acid, Z-ligustilide, butylidenephthalide and various polysaccharides. RA is the dried root of Astragalus membranaceus with primary constituents such polysaccharides, triterpenoids as well as isoflavones. Though their mechanisms of action remain largely elusive, Radix Angelicae Sinensis/Radix Astragali herbal supplements are commonly used for the treatment of various health conditions affecting women including premenstrual syndrome, dysmenorrhea, pelvic pain, recovery from childbirth and menopausal symptoms. These agents are also used for alleviating constipation, preventing and treating anemia and allergic attacks, and for the management of hypertension, joint pain and ulcers.
  • Radotinib hydrochloride - An orally available, hydrochloride salt form of radotinib, a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib. PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature.
  • Raf kinase inhibitor l-779450 - A synthetic triarylimidazole with potential antineoplastic activity. As a Raf kinase inhibitor, L-779450 competes with ATP for binding to the Raf-1 and A-Raf catalytic sites, thus inhibiting their enzymatic activities and blocking various signal transduction pathways that depend on Raf-1 kinase (particularly the Ras-Raf-MEK-ERK cascade which is often up-regulated in neoplasms).
  • Raf kinase inhibitor xl281 - An orally active, small molecule with potential antineoplastic activity. XL281 specifically inhibits RAF kinases, located downstream from RAS in the RAS/RAF/MEK/ERK kinase signaling pathway, which may result in reduced proliferation of tumor cells. RAS mutations may result in constitutive activation of the RAS/RAF/MEK/ERK kinase signaling pathway, and have been found to occur frequently in human tumors.
  • Ragifilimab - An anti-human glucocorticoid-induced tumor necrosis factor receptor (tumor necrosis factor superfamily, member 18; TNFRSF18; GITR; CD357) agonistic humanized monoclonal antibody, with potential immune checkpoint modulating activity. Ragifilimab binds to and activates GITRs found on multiple types of T-cells. This stimulates the immune system, induces both the activation and proliferation of tumor-antigen-specific T effector cells (Teff), and suppresses the function of activated T regulatory cells (Tregs). This leads to tumor cell eradication. GITR, a member of the TNF receptor superfamily and T-cell receptor co-stimulator, is expressed on the surface of multiple immune cell types, including Tregs, Teffs, B-cells, and natural killer (NK) cells. Inappropriately activated Tregs suppress Teffs and suppress T-cell receptor (TCR) signaling.
  • Ralaniten acetate - An orally bioavailable, small molecule inhibitor of the acetate form of ralaniten, a N-terminal domain (NTD) of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration of ralaniten acetate, ralaniten specifically binds to the NTD of AR, thereby inhibiting both AR activation and the AR-mediated signaling pathway. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells.
  • Ralimetinib mesylate - The dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities. Upon administration, ralimetinib inhibits the activity of p38, particularly the alpha and beta isoforms, thereby inhibiting MAPKAPK2 phosphorylation and preventing p38 MAPK-mediated signaling. This may inhibit the production of a variety of cytokines involved in inflammation, cellular proliferation and angiogenesis such as tumor necrosis factor alpha (TNFa), interleukin (IL)-1, -6 and -8, vascular endothelial growth factor, and macrophage inflammatory protein-1 alpha. Ultimately this induces apoptosis and reduces tumor cell proliferation. In addition, inhibition of the p38 MAPK pathway by LY2228820 increases the antineoplastic activity of certain chemotherapeutic agents. p38 MAPK, a serine/threonine protein kinase that is often upregulated in cancer cells, plays a crucial role in tumor cell proliferation, angiogenesis and metastasis.
  • Raloxifene - A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects.
  • Raloxifene hydrochloride - The hydrochloride salt form of raloxifene, a selective benzothiophene estrogen receptor modulator (SERM) with lipid lowering effects and activity against osteoporosis. Raloxifene hydrochloride specifically binds to estrogen receptors in responsive tissue, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it promotes or suppresses the transcription of estrogen-regulated genes, thereby exerting its agonistic or antagonistic effects. This agent functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In tissue like bone, it decreases bone resorption and bone turnover and increases bone mineral density. Raloxifene hydrochloride acts as an estrogen antagonist in uterine and breast tissue. This agent also exerts an anti-proliferative effect on estrogen-sensitive breast cancer.
  • Raltitrexed - A quinazoline folate analogue with antineoplastic activity. After transport into cells via the reduced folate carrier, raltitrexed undergoes intracellular polyglutamation and blocks the folate-binding site of thymidylate synthase, thereby inhibiting tetrahydrofolate activity and DNA replication and repair and resulting in cytotoxicity.
  • Ramucirumab - A recombinant, fully human monoclonal antibody directed against human vascular endothelial growth factor receptor 2 (VEGFR-2) with antiangiogenesis activity. Ramucirumab specifically binds to and inhibits VEGFR-2, which may result in an inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR-2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells.
  • Ranibizumab - A second-generation, recombinant humanized IgG1 kappa monoclonal antibody fragment directed against human vascular endothelial growth factor (VEGF) alpha. Ranibizumab binds to VEGF alpha and inhibits VEGF alpha binding to its receptors, VEGFR1 and VEGFR2, thereby preventing the growth and maintenance of tumor blood vessels. The molecular weight of this agent (48 kD) is much smaller than the molecular weight of bevacizumab (MW ~149 kD), allowing complete penetration of the retina and the subretinal space following intravitreal injection. In contrast to other anti-VEGF aptamers such as pegaptanib, ranibizumab has a high specificity and affinity for all soluble human isoforms of VEGF.
  • Ranimustine - A chloroethylnitrosourea derivative that inhibits proliferation and growth of tumor cells by alkylation and cross-linkage of DNA strands of tumor cells. (NCI)
  • Ranolazine - An orally available, piperazine derivative with anti-anginal and potential antineoplastic activities. Ranolazine's mechanism of action for its anti-ischemic effects has yet to be fully elucidated but may involve the alteration of the trans-cellular late sodium current in the ischemic myocyte. By preventing the rise of intracellular sodium levels, ranolazine may affect the transport activity of sodium-dependent calcium channels and prevent the calcium overload during myocardial ischemia, thereby preventing cellular injury. Ranolazine's potential antineoplastic effect may depend on its inhibitory effect on fatty acid oxidation, which may sensitize tumor cells to apoptosis and decrease tumor cell proliferation; fatty acid oxidation provides energy and promotes tumor cell proliferation and survival.
  • Ranpirnase - A natural homologue of ribonuclease A isolated from the eggs of the frog Rana pipiens. Ranpirnase primarily degrades cellular transfer RNA with a substrate specificity for uridine-guanidine base-pair sequences, resulting in inhibition of protein synthesis and cytotoxicity. This agent also activates caspase-9 in mitochondria, resulting in tumor cell apoptosis.
  • Raralpha agonist irx5183 - An orally bioavailable retinoid acid receptor alpha (RARalpha) agonist and vitamin A derivative, with potential antineoplastic activity. Upon administration, RARalpha agonist IRX5183 binds to and activates RARalpha, which promotes RARalpha-mediated signaling. This results in the transcription of RARalpha-responsive genes, which are responsible for cellular differentiation and proliferation. This results in the induction of cellular differentiation and apoptosis, and leads to the inhibition of cellular proliferation and tumorigenesis. RARalpha is a nuclear receptor and a member of the steroid receptor superfamily; reduced RARalpha signaling is correlated with cancer development in a variety of cancer cell types.
  • Ras peptide asp - A synthetic form of the ras peptide containing a point mutation at position 12 (glycine to aspartic acid) with potential antineoplastic activity. Vaccination with ras peptide Asp may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for this ras mutation, resulting in decreased tumor growth.
  • Ras peptide cancer vaccine - A cancer vaccine containing a RAS oncogene-encoded peptide with potential antineoplastic activity. RAS peptide cancer vaccine may stimulate a RAS peptide-specific antitumoral T-cell cytotoxic immune response, resulting in an inhibition of tumor cell proliferation and tumor cell death.
  • Ras peptide cys - A synthetic form of the Ras peptide containing a point mutation at position 12 (glycine to cysteine) with potential antineoplastic activity. Vaccination with this peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for this Ras mutation, resulting in decreased tumor growth.
  • Ras peptide val - A synthetic form of the Ras peptide containing a point mutation at position 12 (glycine to valine) with potential antineoplastic activity. Vaccination with this peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for this Ras mutation, resulting in decreased tumor growth.
  • Razoxane - An orally bioavailable bis-dioxopiperazine and a derivative of the chelating agent ethylenediaminetetraacetic acid (EDTA) with antineoplastic, antiangiogenic, and antimetastatic activities. Razoxane specifically inhibits the enzyme topoisomerase II without inducing DNA strand breaks, which may result in the inhibition of DNA synthesis and cell division in the premitotic and early mitotic phases of the cell cycle. This agent may also exhibit antiangiogenic and antimetastatic activities although the precise molecular mechanisms of these actions are unknown.
  • Realgar-indigo naturalis formulation - An orally bioavailable, traditional Chinese medicine (TCM)-based formulation composed of Realgar-Indigo naturalis formula (RIF) with potential antineoplastic activity. The main constituents in RIF are realgar, Indigo naturalis, and Salvia miltiorrhiza, with tetraarsenic tetrasulfide (As4S4), indirubin and tanshinone IIA as the main active ingredients, respectively, which appear to exert synergistic effects on cancer cells. Tetraarsenic tetrasulfide specifically induces the ubiquitination and degradation of promyelocytic leukemia retinoic acid receptor alpha (PML-RARalpha) oncoprotein. In addition, the active ingredients in the Realgar-Indigo naturalis formulation enhance the expression of myeloid differentiation genes, and induce G(1)/G(0) cell cycle arrest. PML-RARalpha, an acute promyelocytic leukemia (APL)-specific fusion gene, inhibits differentiation and promotes survival of myeloid precursor cells
  • Rebastinib tosylate - The tosylate salt of rebastinib, an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity. Rebastinib binds to and inhibits the Bcr-Abl fusion oncoprotein by changing the conformation of the folded protein to disallow ligand-dependent and ligand-independent activation; in addition, this agent binds to and inhibits Src family kinases LYN, HCK and FGR and the receptor tyrosine kinases TIE-2 and VEGFR-2. Rebastinib may exhibit more potent activity against T315I Bcr-Abl gatekeeper mutant kinases than other Bcr-Abl kinase inhibitors. The TIE-2 and VEGFR-2 receptor tyrosine kinases regulate angiogenesis, respectively, while the Src family kinases Abl, LYN, and HCK Src regulate a variety of cellular responses including differentiation, division, adhesion, and the stress response.
  • Rebeccamycin - An indolocarbazole glycoside antineoplastic antibiotic isolated from the bacterium Saccharothrix aerocolonigenes. Rebeccamycin intercalates into DNA and stabilizes the DNA-topoisomerase I complex, thereby interfering with the topoisomerase I-catalyzed DNA breakage-reunion reaction and initiating DNA cleavage and apoptosis.
  • Rebimastat - A sulfhydryl-based second-generation matrix metalloproteinase (MMP) inhibitor with potential antineoplastic activity. Rebimastat selectively inhibits several MMPs (MMP 1, 2, 8, 9, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
  • Receptor tyrosine kinase inhibitor r1530 - A pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. Mitosis-angiogenesis inhibitor (MAI) R1530 inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta, FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis.
  • Recombinant 70-kd heat-shock protein - A recombinant peptide that is chemically identical to or similar to the endogenous 70-kD heat shock protein (HSP70). HSP70 is a molecular chaperone that prevents physiologic stress-induced cell death by inhibiting both caspase-dependent and caspase-independent apoptosis. Because this peptide is often overexpressed in tumor cells, autologous vaccination with HSP70 derived from tumor cells may stimulate the host immune system to mount a tumoricidal cytotoxic T lymphocyte (CTL) response.
  • Recombinant adenovirus 5 encoding tumor necrosis factor-related apoptosis-inducing ligand - An adenovirus type 5 (Ad5) encoding human tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), with potential apoptosis-inducing and antineoplastic activities. Upon administration of recombinant Ad5 encoding TRAIL, the adenovirus selectively infects tumor cells and expresses TRAIL. The virally expressed TRAIL binds to and activates its receptors TRAIL receptor-1 (TRAIL-R1, death receptor 4, DR4) and TRAIL receptor-2 (TRAIL-R2, death receptor 5, DR5), which subsequently activate caspases and induce apoptosis in TRAIL-R1/R2-expressing tumor cells. The pro-apoptotic cell surface receptors TRAIL-R1 and -R2, members of the TNF receptor family, are overexpressed by a variety of cancer cell types.
  • Recombinant adenovirus encoding p53 - A replication-defective, recombinant adenoviral vector encoding the wild-type human tumor-suppressor protein p53 gene with potential antineoplastic activity. Upon intratumoral administration, rAD-p53 binds to the coxsackie-and-adenovirus receptor (CAR) on tumor cells and enters cells selectively via receptor-mediated endocytosis, which may result in the overexpression of wild-type p53 intracellularly and p53-mediated tumor regression. In addition, this agent may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against tumor cells, may activate natural killer (NK) cells to exert antitumor 'bystander effects' and may downregulate the expression of various oncogenes. The p53 protein blocks tumor cell cycle progression and directly initiates apoptosis; the p53 gene, a tumor suppressor gene, is deleted or mutated in a significant number of cancers.
  • Recombinant adenovirus-hifn-beta - A recombinant replication-defective adenovirus which encodes the gene for the cytokine human interferon-beta (IFN-beta). Once inserted into and replicating in host tumor cells, recombinant adenovirus-hIFN-beta expresses human IFN-beta, which may stimulate an antiproliferative natural killer (NK) cell response against tumor cells and induce caspase-mediated tumor cell apoptosis.
  • Recombinant adenovirus-l523s vaccine - A replication-defective adenovirus containing a gene that encodes the human protein L523S with potential antineoplastic activity. Upon administration, recombinant adenovirus-L523S vaccine expresses L523S, which may stimulate antibody and cytotoxic T lymphocyte (CTL) responses against tumor cells expressing L523S. L523S is an RNA-binding protein that belongs to the KOC (K homology domain containing protein over-expressed in cancer) family of proteins. As an oncofetal protein, L523S is normally expressed in early embryonic tissues and certain normal adult tissues such as colon, fallopian tube, gall bladder, and ovary tissues but may be overexpressed in squamous cell cancers of the lung.
  • Recombinant adenovirus-p53 sch-58500 - A genetically-engineered adenovirus that contains the gene that encodes the human tumor-suppressor protein p53 with potential antineoplastic activity. Recombinant adenovirus-p53 SCH-58500 delivers p53 into tumor cells, which may result in p53-mediated cell cycle arrest and apoptosis.
  • Recombinant anti-wt1 immunotherapeutic gsk2302024a - An immunotherapeutic composed of the Wilms tumor 1 (WT1) and an as of yet undisclosed adjuvant, with potential antineoplastic activity. Upon administration, the immune system may be stimulated to exert a cytotoxic T-lymphocyte (CTL) response against WT1-expressing tumor cells. The adjuvant stimulates the immune system's response to WT1. WT1, a tumor-associated antigen (TAA) and transcription factor, is overexpressed in a variety of tumor cell types.
  • Recombinant attenuated salmonella typhimurium expressing il-2 - An orally available, genetically engineered Salmonella typhimurium strain expressing a truncated form of the human cytokine interleukin-2 (IL-2) gene, with antitumor activity. Upon administration of recombinant attenuated S. typhimurium expressing IL-2 (SalpIL2), this Salmonella strain may selectively accumulate and divide in a variety of tumor types, and express IL-2. In turn, IL-2 may induce natural killer (NK) cell proliferation thereby enhancing their activity. This may inhibit the growth of tumor cells.
  • Recombinant b. pertussis adenylate cyclase toxin-tyrosinase a2 epitope vaccine - A recombinant vaccine containing a genetically detoxified adenylate cyclase toxin (CyaA) of Bordetella pertussis coupled, through its catalytic site, to the melanoma tyrosinase A2 epitope YMDGTMSQV, with potential antineoplastic activity. Via the toxin moiety, the recombinant B. pertussis adenylate cyclase toxin-tyrosinase A2 epitope specifically binds to the alphaMbeta2 integrin (CD11b/CD18) located on CD11b-positive antigen-presenting cells (APC). Upon processing and presentation of the melanoma-specific epitope by MHC class I molecules to the surface of these APCs, a specific cytotoxic T-cell (CTL) response against tumor cells expressing tyrosinase may be initiated, resulting in decreased tumor growth and cell lysis.
  • Recombinant bacterial minicells vax014 - A population of recombinant bacterial minicells (rBMCs) engineered to express the alpha3beta1 (a3b1) and alpha5beta1 (a5b1) integrin-targeting invasion and that contain a bacterial protein toxin, perfringolysin O (PFO), with potential antineoplastic activity. Upon intravesical administration, VAX014 selectively targets and binds to tumor cells expressing un-ligated a3b1 and/or a5b1 integrins and delivers PFO, leading to destabilization of tumor cell membranes and tumor cell lysis. By targeting un-ligated a3b1 and/or a5b1 integrins, VAX014 selectively targets tumor cells over normal cells, with potentially less adverse effects in comparison with first generation integrin-targeted therapies.
  • Recombinant bispecific single-chain antibody rm28 - A recombinant, bispecific, single-chain antibody directed against both the T-cell surface-associated costimulatory molecule CD28 and a melanoma-associated proteoglycan (MAPG) with potential antitumor activity. By targeting both CD28 and MAPG, recombinant bispecific single-chain antibody rM28 enhances cytotoxic T-cell recognition of melanoma cells, which may result in immune effector cell-mediated tumor cell death and a decrease in distant metastases. This agent appears to have a long serum half-life secondary to the formation of dimers. When activated, CD28 facilitates interactions between T-cells and other immune effector cells resulting in cytotoxic T-lymphocyte responses; MAPG is a surface antigen expressed on the majority of melanomas, including primary cutaneous, ocular, and metastatic melanomas.
  • Recombinant cd40-ligand - A recombinant therapeutic agent which is chemically identical to or similar to CD40-ligand. CD40-ligand, also known as CD40L/TRAP and CD154, is a type II membrane protein which binds to CD40, a cell surface receptor that belongs to the tumor necrosis factor receptor family; CD40 is expressed on B lymphocytes, monocytes, dendritic cells (DC), hematopoietic progenitors, endothelial cells and epithelial cells. Recombinant CD40-ligand may be used to activate DC ex vivo via CD40 binding; CD40-ligand-activated DC may provide or augment a protective antitumor immunity when administered in dendritic cell cancer vaccines.
  • Recombinant dher2 vaccine - A cancer vaccine consisting of a truncated recombinant HER2 peptide (dHER2) with potential antineoplastic activity. Upon administration, recombinant dHER2 vaccine may stimulate the host immune response to mount a cytotoxic T-lymphocyte response against tumor cells that overexpress the HER2 protein, resulting in tumor cell lysis. The HER2 protein is a tumor-associated antigen (TAA) that is overexpressed in a variety of cancers. dHER2 includes the extracellular domain (ECD) and a part of the intracellular domain (ICD) of the HER2 protein.
  • Recombinant dna-l523s vaccine - A plasmid DNA encoding human L523S, an RNA-binding protein that belongs to the KOC (K homology domain containing protein overexpressed in cancer) family, with potential antineoplastic activity. Vaccination with L523S DNA may stimulate a cytotoxic T lymphocytes (CTL) response against tumor cells that express the L523S protein. As an oncofetal protein, L523S is normally expressed in early embryonic tissue, but is overexpressed in certain cancer cell types.
  • Recombinant ephb4-hsa fusion protein - A recombinant fusion protein composed of the full-length extracellular domain (soluble) of human receptor tyrosine kinase ephrin type-B receptor 4 (sEphB4) and fused, at its C-terminus, to full-length human serum albumin (HSA), with potential antineoplastic and anti-angiogenic activities. sEphB4-HSA functions as a decoy receptor for the membrane-bound ligand Ephrin-B2 (Efnb2) and interferes with the binding of Efnb2 to its native receptors, including EphB4 and EphA3. This may result in a reduction of angiogenesis and a reduction in cell growth of Efnb2 and/or EphB4 over-expressing tumor cells. In addition, this agent also prevents the angiogenic effects of numerous growth factors due to interactions between Efnb2 and EphB4. Efnb2 and EphB4 are overexpressed in a variety of tumor cell types; the bi-directional signaling of Efnb2-EphB4 plays an important role in angiogenesis and tumor cell migration, invasion, and proliferation. Albumin reduces this agent's degradation, improves circulation time and may thus improve efficacy.
  • Recombinant erwinia asparaginase jzp-458 - A recombinant form of asparaginase (Erwinia asparaginase; crisantaspase) derived from the bacterium Erwinia chrysanthemi, genetically engineered to be produced in Pseudomonas fluorescens, with potential antineoplastic activity. Upon administration of recombinant Erwinia asparaginase JZP-458, the recombinant asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia. This depletes cancer cells of asparagine, which blocks protein synthesis and tumor cell proliferation. Asparagine is critical to protein synthesis in cancer cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. JZP-458 can be used as an alternative in patients who are hypersensitive to Escherichia (E.) coli-derived asparaginase products.
  • Recombinant fas ligand - A recombinant agent, which is chemically identical to or similar to the endogenous protein Fas ligand, a protein related to tumor necrosis factor (TNF) with potential antineoplastic activity. Fas ligand binds to the Fas receptor, thereby activating caspases and inducing apoptosis.
  • Recombinant fowlpox gm-csf vaccine adjuvant - A cancer vaccine adjuvant consisting of a recombinant fowlpox virus encoding human granulocyte-macrophage colony-stimulating factor (GM-CSF). GM-CSF binds to specific cell surface receptors on various immuno-hematopoietic cell types, enhancing their proliferation and differentiation and stimulating macrophage and dendritic cell functions in antigen presentation and antitumor cell-mediated immunity. Administration of recombinant fowlpox GM-CSF vaccine adjuvant may induce an immune response against tumor cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
  • Recombinant fowlpox-b7.1 vaccine - A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the stimulatory molecule transgene B7-1. Recombinant fowlpox-B7.1 vaccine may enhance antigen presentation and activate antitumoral cytotoxic T-cells.
  • Recombinant fowlpox-cea(6d)/tricom vaccine - A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the carcinoembryonic antigen (CEA) and a TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3) (TRICOM). This agent may enhance CEA presentation to antigen presenting cells (APC) and activate cytotoxic T-cells against CEA-expressing tumors.
  • Recombinant fowlpox-mgp100 vaccine - A vaccine consisting of a replication-defective recombinant fowlpox virus that encodes for the murine melanoma antigen glycoprotein 100 (mgp100) with potential antineoplastic activity. Vaccination with recombinant fowlpox-mgp100 vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the gp100 antigen, resulting in decreased tumor growth.
  • Recombinant fowlpox-prostate specific antigen vaccine - A cancer vaccine consisting of a recombinant fowlpox virus encoding human prostate-specific antigen (PSA). Administration of this agent may stimulate a cytotoxic T cell response against PSA-expressing tumor cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
  • Recombinant fowlpox-tricom vaccine - A vaccine comprised of a recombinant fowlpox virus vector encoding a TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3) (TRICOM), which may enhance antigen presentation and activate cytotoxic T-cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
  • Recombinant fowlpox-tyrosinase vaccine - A recombinant fowlpox virus vaccine with potential antineoplastic activity. Binding to the melanoma antigen tyrosinase, recombinant fowlpox-tyrosinase vaccine generates cellular immune responses against melanoma cells expressing the tyrosinase antigen; this effect is enhanced by the co-administration of interleukin 2 (IL-2). Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
  • Recombinant fractalkine - A pro-inflammatory delta chemokine with potential antineoplastic activity. Fractalkine induces the adhesion and migration of T lymphocytes, monocytes and natural killer (NK) cells. In lymphomas, this agent may promote cell-mediated lympholysis by recruiting activated NK cells.
  • Recombinant human 6ckine - A therapeutic recombinant analogue of a member of the endogenous CC chemokines with potential antineoplastic activity. Expressed by various lymphoid tissues, endogenous 6Ckine is chemotactic for B and T lymphocytes and dendritic cells.
  • Recombinant human adenovirus type 5 h101 - A replication selective, recombinant, E1B and partial E3 gene deleted form of human adenovirus type 5, with potential antineoplastic activity. Upon intratumoral injection of recombinant human adenovirus type 5, the adenovirus selectively replicates in cancer cells while preventing viral replication in normal, healthy cells. This induces a selective adenovirus-mediated cytotoxicity in cancer cells, which leads to cancer cell lysis. In addition, viral spread to adjacent cells, following lysis of infected cells, may activate the immune system to kill the infected tumor cells. The E1B protein causes p53 inactivation, which promotes viral replication; deletion of E1B allows for p53 activation in normal cells, which prevents viral replication in normal, healthy cells. The mutation and subsequent inactivation of p53 in cancer cells enables the E1B-deleted adenovirus to selectively replicate in cancer cells. Partial deletion of E3, encoding the adenovirus death protein, enhances the safety profile of the administered adenovirus.
  • Recombinant human angiotensin converting enzyme 2 apn01 - A recombinant, soluble glycosylated form of human angiotensin converting enzyme 2 (rhACE2) with antihypertensive and potential antineoplastic activities. Recombinant human angiotensin converting enzyme 2 APN01 may normalize ACE2 levels, cleaving angiotensin II to create angiotensin-(1-7) and restoring the function of the renin-angiotensin system (RAS). ACE2, a homolog of ACE1, appears to function as a negative regulator of the RAS system by converting angiotensin II to angiotensin-(1-7), a peptide with actions that counteract the cardiovascular actions of angiotensin II. In addition, angiotensin-(1-7) may inhibit cyclooxygenase 2 (COX-2) and the production of proinflammatory prostaglandins and may activate the angiotensin-(1-7) G protein-coupled receptor Mas, resulting in diminished tumor cell proliferation. ACE2 levels may be reduced in malignancy and diabetes and in liver, cardiovascular and lung diseases.
  • Recombinant human anti-tgf-beta monoclonal antibody - A recombinant human IgG4 monoclonal antibody directed against transforming growth factor-beta (TGFb) with potential antineoplastic activity. Recombinant human anti-TGF-beta monoclonal antibody specifically targets and binds to all 3 isoforms of TGFb, thereby neutralizing TGFb isoforms 1, 2 and 3. This prevents activation of TGFb-mediated signaling pathways. TGFb, a pleiotropic cytokine, is often overexpressed in a number of cancer cell types and is involved in cancer cell proliferation, differentiation, migration, invasion and angiogenesis.
  • Recombinant human apolipoprotein(a) kringle v mg1102 - An 86 amino-acid long polypeptide fragment of a recombinant form of human apolipoprotein (a) (apo(a)) kringle V, with potential anti-angiogenic and antineoplastic activities. Although the exact mechanism of action has yet to be fully elucidated, upon administration, recombinant human apo(a) kringle V MG1102 inhibits the fibronectin-mediated migration of endothelial cells, binds to and blocks the activity of alpha 3 beta 1 integrin (a3b1 integrin), inhibits the activation of focal adhesion kinase (FAK) and FAK-mediated signaling, and leads to the inhibition of the p130 Crk-associated substrate (p130CAS)-c-Jun NH2-terminal kinase (JNK) pathway. This inhibits tumor angiogenesis, induces mitochondrial-mediated apoptosis of tumor cells and tumor-associated endothelial cells, and suppresses tumor growth and metastasis. Apo(a), a glycoprotein component of human lipoprotein(a), contains repeated kringle domains; certain kringle domains of apo(a), including the plasminogen kringle V homolog (KV), have anti-angiogenic effects.
  • Recombinant human egf-rp64k/montanide isa 51 vaccine - A peptide vaccine preparation, containing recombinant human epidermal growth factor (rEGF) linked to the Neisseria meningitidis-derived recombinant immunogenic carrier protein P64k (rP64k) and mixed with the immunoadjuvant Montanide ISA 51, with potential active immunotherapy activity. Recombinant human EGF-rP64K/Montanide ISA 51 vaccine may trigger a humoral immune response against vaccine rEGF and rP64K and, so, against endogenous EGF. Antibody-mediated inhibition of endogenous EGF binding to its receptor, epithelial growth factor receptor (EGFR), may result in the inhibition of tumor cell proliferation.
  • Recombinant human endostatin - A recombinant human proteolytic fragment of the C-terminal end of type XVIII collagen. Endostatin induces microvascular endothelial cell apoptosis and inhibits endothelial proliferation and angiogenesis, which may result in a reduction in tumor burden. This agent also may decrease hepatic metastasis by inhibiting proinflammatory cytokines and vascular cell adhesion molecule (VCAM)-dependent cell attachment to the hepatic microvasculature.
  • Recombinant human hsp110-gp100 chaperone complex vaccine - A recombinant chaperone-peptide complex-based vaccine composed of a complex between heat shock protein hsp110 and the human melanoma-associated antigen gp100, with potential antineoplastic activity. Upon vaccination, recombinant hsp110-gp100 chaperone complex activates the immune system to exert a cytotoxic T cell immune response and antigen-specific interferon-gamma production against gp100-overexpressing cancer cells. Gp100, is overexpressed in a variety of cancer cell types. Hsp110, binds to and chaperones full-length proteins during heat shock; as an immunoadjuvant it is able to enhance an immune response against antigen(s) and stimulate T-lymphocyte activation.
  • Recombinant human muc1-oxidized polymannose-pulsed autologous dendritic cell vaccine - A cancer vaccine containing autologous dendritic cells pulsed with a fusion product of an epitope of human tumor-associated epithelial mucin 1 (MUC1) antigen and the vaccine adjuvant mannan (oxidized mannose), with potential antineoplastic activity. When the modified dendritic cells are returned to the patient, they may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the MUC1 antigen, resulting in tumor cell lysis. Addition of manna in this vaccine, enhances immune recognition. MUC1 antigen, a high-molecular-weight transmembrane glycoprotein, is overexpressed on many tumor cells.
  • Recombinant human papillomavirus 11-valent vaccine - A recombinant, 11-valent, human papillomavirus (HPV) vaccine, produced in Hansenula polymorpha, with potential immunoprotective and antineoplastic properties. Upon administration, recombinant HPV 11-valent vaccine may generate humoral and cellular immunity against the 11 undisclosed types of HPV antigens, thereby preventing cervical infection upon exposure to these 11 types of HPV. In addition, this agent may stimulate an antitumoral cellular immune response against cervical cancer associated with HPV infection.
  • Recombinant human papillomavirus bivalent vaccine - A recombinant, bivalent, human papillomavirus (HPV) vaccine, containing virus-like particles for HPV types 16 and 18 linked to the adjuvant ASO4, with potential immunoprotective and antineoplastic properties. Upon administration, HPV 16/18 L1 virus-like particle/ASO4 vaccine may generate humoral and cellular immunity against HPV types-16 and -18 antigens, thereby preventing cervical infection upon exposure to HPV types 16 and 18. In addition, this agent may stimulate an antitumoral cellular immune response against cervical cancer associated with HPV infection.
  • Recombinant human papillomavirus nonavalent vaccine - A non-infectious, recombinant, nonavalent vaccine prepared from highly purified virus-like particles (VLPs) comprised of the major capsid (L1) proteins from human papillomavirus (HPV) types 6, 11, 16, 18, 31, 33, 45, 52, and 58, with active immunizing activity. Upon administration, the recombinant HPV nonavalent vaccine activates the immune system to produce antibodies against the 9 HPV types. This protects against HPV infection and HPV-related cancers. Altogether, HPV types 6, 11, 16, 18, 31, 33, 45, 52, and 58 account for the majority of the HPV types that cause cervical, vulvar, vaginal and anal cancers.
  • Recombinant human plasminogen kringle 5 domain abt 828 - A recombinant human plasminogen kringle 5 domain with potential antiangiogenic and antineoplastic activities. Upon administration, recombinant human plasminogen kringle 5 domain ABT 828 may promote caspase activity and apoptosis in proliferating endothelial cells, thereby inhibiting migration. Kringle 5 (K5), an internal proteolytic fragment of plasminogen specifically inhibits endothelial cell growth via its interaction with endothelial cell surface ATP synthase, which sequentially triggers the activation of caspases -8, -9, and -3.
  • Recombinant human trail-trimer fusion protein scb-313 - A recombinant fusion protein composed of the human C-propeptide of alpha1(I) collagen (Trimer-Tag) to the C-terminus of the mature human tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL; Apo2L), with potential pro-apoptotic and antineoplastic activities. The binding of TRAIL to the Trimer-Tag allows TRAIL to form a stable covalently-linked homotrimer. Upon administration of recombinant human TRAIL-trimer fusion protein SCB-313, this fusion protein targets, binds to and trimerizes the TRAIL-receptors, pro-apoptotic death receptors (DRs) TRAIL-R1 (death receptor 4; DR4) and TRAIL-R2 (death receptor 5; DR5), expressed on tumor cells, thereby activating caspases and inducing apoptosis in TRAIL-R1/R2-expressing tumor cells. TRAIL, a homotrimeric type II transmembrane protein and member of the TNF superfamily of cytokines, plays a key role in the induction of apoptosis through TRAIL-mediated death receptor pathways. The pro-apoptotic cell surface receptors TRAIL-R1 and -R2, members of the TNF receptor family, are overexpressed by a variety of cancer cell types; The induction of receptor trimerization is needed for the initiation of the apoptotic signaling pathway. The TRAIL-Trimer retains similar bioactivity and receptor binding kinetics as native TRAIL but has more favorable pharmacokinetics and antitumor activity than native TRAIL.
  • Recombinant humanized anti-her-2 bispecific monoclonal antibody mbs301 - A glyco-engineered heterodimeric bispecific monoclonal antibody, derived from trastuzumab and pertuzumab, directed against two distinct epitopes of the extracellular dimerization (ECD) domain of the tumor-associated antigen (TAA) human tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential immunomodulating and antineoplastic activities. Upon administration, recombinant humanized anti-HER-2 bispecific monoclonal antibody MBS301 simultaneously targets and binds to two separate, non-overlapping epitopes of HER-2. This prevents the activation of HER-2 signaling pathways. Also, by binding to HER-2, MBS301 induces an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER-2. This results in tumor cell apoptosis and inhibits tumor cell proliferation of HER-2-overexpressing tumor cells. HER-2, overexpressed on a variety of tumor cell types, plays an important role in tumor cell proliferation, differentiation and survival.
  • Recombinant interferon - One of a group of recombinant therapeutic glycoprotein cytokines with antiviral, anti-proliferative, and immunomodulating activities. Interferons bind to specific cell-surface receptors, leading to the transcription and translation of genes with interferon-specific response elements (ISREs). The resultant proteins mediate many complex effects, ultimately leading to inhibition of viral protein synthesis and cellular growth, alteration of cellular differentiation, interference with oncogene expression, activation of natural killer cells, alteration of cell surface antigen expression, and augmentation of lymphocyte and macrophage cytotoxicity. The production of endogenous interferons is induced in response to foreign agents such as bacteria, viruses and parasites and to tumor cells.
  • Recombinant interferon alfa - A class of naturally-isolated or recombinant therapeutic peptides used as antiviral and anti-tumor agents. Alpha interferons are cytokines produced by nucleated cells (predominantly natural killer (NK) leukocytes) upon exposure to live or inactivated virus, double-stranded RNA or bacterial products. These agents bind to specific cell-surface receptors, resulting in the transcription and translation of genes containing an interferon-specific response element. The proteins so produced mediate many complex effects, including antiviral effects (viral protein synthesis); antiproliferative effects (cellular growth inhibition and alteration of cellular differentiation); anticancer effects (interference with oncogene expression); and immune-modulating effects (natural killer cell activation, alteration of cell surface antigen expression, and augmentation of lymphocyte and macrophage cytotoxicity).
  • Recombinant interferon alfa-1b - The non-glycosylated recombinant interferon alpha, subtype 1b, with immunostimulatory and antineoplastic activities. Alpha interferon-1b binds to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects.
  • Recombinant interferon alfa-2a - A non-glycosylated recombinant human alpha interferon, subtype 2a, produced in the bacterium E. coli. Interferon alpha-2a binds to its specific cell-surface receptor, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune modulating effects.
  • Recombinant interferon alfa-2b - A non-glycosylated recombinant interferon with antiviral and antineoplastic activities. Alfa interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects.
  • Recombinant interferon alpha 2b-like protein - A proprietary recombinant protein highly resembling human interferon alpha 2b (IFN-a2b), with potential anti-tumor, anti-inflammatory, immunomodulating and antiviral activities. Upon injection, recombinant IFN alpha 2b-like protein binds to specific IFN alpha cell surface receptors. This activates interferon-mediated signal transduction pathways and induces the transcription and translation of genes with interferon-specific response elements (ISREs). This may activate the immune system, including the activation of natural killer cells (NKs) and may result in an inhibition of tumor cell proliferation, tumor angiogenesis, metastasis and an induction of apoptosis. Compared to human IFN-a2b (HuINF-a2b), this agent exhibits enhanced antiviral and antiproliferative activities. In addition, this agent exhibits antiviral activity against a variety of viruses, including hepatitis B and C viruses, human immunodeficiency virus (HIV) and Avian Influenza.
  • Recombinant interferon beta - A recombinant protein which is chemically identical to or similar to endogenous interferon beta with antiviral and anti-tumor activities. Endogenous interferons beta are cytokines produced by nucleated cells (predominantly natural killer cells) upon exposure to live or inactivated virus, double-stranded RNA or bacterial products. These agents bind to specific cell-surface receptors, resulting in the transcription and translation of genes with an interferon-specific response element. The proteins so produced mediate many complex effects, including antiviral (the most important being inhibition of viral protein synthesis), antiproliferative and immune modulating effects. The recombinant therapeutic forms of interferon beta are interferon beta 1-a and interferon beta 1-b. (NCI05)
  • Recombinant interferon gamma - A recombinant therapeutic agent which is chemically identical to or similar to the endogenous lymphokine interferon gamma (IFN-gamma) with antineoplastic, immunoregulatory, and antiviral activities. Therapeutic IFN-gamma binds to and activates the cell-surface IFN-gamma receptor, stimulating antibody-dependent cytotoxicity and enhances natural killer cell attachment to tumor cells. This agent also activates caspases, thereby inducing apoptosis in malignant cells.
  • Recombinant interleukin-13 - The recombinant analogue of an endogenous cytokine interleukin 13 with potential antineoplastic activity. Produced by lymphocytes and exhibiting a variety of functions, interleukin-13 (therapeutic) inhibits DNA synthesis and regulates inflammatory and immune responses. In animal models, this agent has been shown to kill tumor cells both directly and indirectly by activating the host immune system at the tumor site.
  • Recombinant interleukin-6 - A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-6 (IL-6) with antiapoptotic, proinflammatory, antiinflammatory, proproliferative and proangiogenic activities. IL-6 binds to its receptor (IL-6R), activating a receptor-CD130 receptor complex; the CD130 portion of the complex is a signal transduction protein that activates JAK kinases and Ras-mediated signaling pathways, which in turn activate downstream signaling pathways, resulting in the activation of various transcription factors (STAT, ELK-1, NF-IL-6, etc.) and gene transcription. The physiological effects of IL-6 are complex and varied and include hematopoietic, pyrogenic and thermogenic, proinflammatory, antiinflammatory, proproliferative (anti-apoptotic), and angiogenic effects.
  • Recombinant ksa glycoprotein co17-1a - A recombinant counterpart of tumor-associated KSA antigen (Ep-CAM), a type-I transmembrane glycoprotein cellular adhesion molecule with a molecular mass of 40 kDa, overexpressed on the majority of tumor cells of most human epithelia in a of variety of tumor tissues such as stomach, colon, pancreas, gall bladder, bile duct, mammary gland, breast, and lung carcinoma. It has been suggested to be involved in the differentiation, growth, and organization of epithelial cells within tissues under normal physiological conditions. The antigen has been used as a target for diagnosis and for passive and active immunotherapy of colorectal cancer. Immunization with KSA Glycoprotein elicits both humoral and Th1-associated cellular immune responses.
  • Recombinant leukocyte interleukin - A cocktail preparation of synthetic interleukin (IL) -1, IL-2, IL-6, tumor necrosis factor (TNF)-alpha, interferon gamma and other cytokines that are chemically identical to or similar to signaling molecules secreted by leukocyte cells. Leukocyte interleukins are essential in many immune responses, such as antibodies production, modulating secretion of other cytokines, and activation of bone marrow stem cells.
  • Recombinant leukoregulin - A formulated therapeutic analog of the endogenous lymphokine leukoregulin with potential antineoplastic activity. Leukoregulin displays direct and indirect cytotoxicity through tumor cell lysis and enhancing tumor cell susceptibility to natural killer cell-mediated cytotoxicity. This agent enhances membrane permeability and decreases p-glycoprotein expression, thereby promoting cytotoxic drug uptake into tumor cells. Leukoregulin also induces the synthesis of collagenase and hyaluronan, expression and secretion of interleukin-8, and upregulates stromelysin-1 gene expression in human fibroblasts, thereby regulating extracellular matrix degradation.
  • Recombinant macrophage colony-stimulating factor - A recombinant therapeutic agent which is chemically identical to or similar to the endogenous protein cytokine macrophage colony-stimulating factor (M-CSF). Synthesized endogenously by mesenchymal cells, M-CSF stimulates the survival, proliferation, and differentiation of hematopoietic cells of the monocyte-macrophage series and can reverse treatment-related neutropenias. Recombinant M-CSF may also enhance antigen presentation and activate antitumoral cytotoxic T-cells.
  • Recombinant mage-3.1 antigen - A recombinant tumor-specific melanoma antigen. Vaccination with recombinant MAGE-3.1 antigen may induce a host immune response against MAGE-expressing cells, resulting in antitumoral T cell-mediated cytotoxicity. MAGE-expressing cells are found in melanoma, non-small-cell lung carcinoma (NSCLC), head and neck squamous cell carcinoma, transitional cell carcinoma of the bladder, and esophageal carcinoma.
  • Recombinant modified vaccinia ankara-5t4 vaccine - A cancer vaccine comprised of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the 5T4 fetal oncoprotein (MVA-h5T4). Vaccination with recombinant modified vaccinia Ankara-5T4 vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing 5T4 fetal oncoprotein antigen, resulting in tumor cell lysis. The MVA viral vector, derived from the replication-competent strain Ankara, is a highly attenuated, replication-defective vaccinia strain incapable of virion assembly.
  • Recombinant nematode anticoagulant protein c2 - An 85-amino acid recombinant peptide derived from protein c2 of the hemophagocytic hookworm Ancylostoma caninum (a common canine parasite) with anticoagulant activity. Recombinant nematode anticoagulant protein c2 (rNAPc2) binds to circulating activated factor X (FXa) or zymogen factor X (FX) to form a binary complex which subsequently binds to and inhibits membrane-bound activated factor VII/tissue factor complex (FVIIa/TF). When administered prophylactically, this agent may reduce the incidence of deep venous thrombosis without hemostatic compromise. Because rNAPc2 inhibits the formation of the FVIIa/TF protease complex, which may play a role in the cellular signaling of both metastatic and angiogenic processes, it may impede tumor progression.
  • Recombinant oncolytic poliovirus pvs-ripo - A recombinant, live attenuated, nonpathogenic oncolytic virus containing the oral poliovirus Sabin type 1 in which the internal ribosomal entry site (IRES) is replaced with the IRES from human rhinovirus type 2 (HRV2), with potential antineoplastic activity. Upon intratumoral administration of recombinant oncolytic poliovirus PVS-RIPO, the poliovirus is selectively taken up by and replicates in tumor cells expressing CD155 (poliovirus receptor, PVR or NECL5) eventually causing tumor cell lysis. CD155, an oncofetal cell adhesion molecule and tumor antigen, is ectopically expressed in certain cancers, such as glioblastoma multiforme (GMB), and plays an important role in tumor cell migration, invasion, and metastasis. Due to the heterologous HRV2 IRES in this recombinant virus, PVS-RIPO only propagates in susceptible, nonneuronal cells (e.g., GBM).
  • Recombinant prame protein plus as15 adjuvant gsk2302025a - A recombinant form of the human PRAME (Preferentially Expressed Antigen of Melanoma) protein combined with the AS15 adjuvant, with potential immunostimulatory and antineoplastic activities. Upon intramuscular administration, GSK2302025A may stimulate the host immune response to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells that overexpress the PRAME protein, resulting in tumor cell lysis. The tumor-associated antigen PRAME is often overexpressed by a variety of tumor cell types. AS15 is an potent adjuvant liposomal formulation that contains CpG 7909, monophosphoryl lipid, and QS-21.
  • Recombinant saccharomyces cerevisia-cea(610d)-expressing vaccine gi-6207 - A whole, heat-killed, recombinant Saccharomyces cerevisiae yeast-based vaccine genetically altered to express the carcinoembryonic antigen (CEA) peptide 610D with potential immunostimulating and antineoplastic activities. Upon administration, recombinant Saccharomyces cerevisia-CEA(610D) vaccine GI-6207 may stimulate a host cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells, which may result in tumor cell lysis. CEA, a tumor associated antigen, is overexpressed on a wide variety of human cancer cells including colorectal, gastric, lung, breast and pancreatic cancer cells. CEA 610D encodes for 9 amino acids (605-613) in which aspartate is substituted for asparagine at position 610 (610D) in order to strengthen the induction of the CTL response against CEA-expressing tumor cells.
  • Recombinant super-compound interferon - A recombinant form of the naturally-occurring cytokine interferon-alpha (IFN-a) that has a modified spatial configuration, with immunomodulating, antiviral and antineoplastic activities. Upon administration of recombinant super-compound interferon (rSIFN-co), this agent binds to IFN-specific cell surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects. The 3-dimensional conformational change improves efficacy and causes less side effects compared to IFN-a.
  • Recombinant thyroglobulin - A recombinant form of thyroglobulin identical to or similar to the endogenous iodine-containing glycoprotein. Thyroglobulin is synthesized in the thyroid follicular cell, and is the precursor of thyroid hormones T3 and T4. Thyroglobulin levels can serve as a tumor marker for monitoring the status of differentiated thyroid carcinomas.
  • Recombinant thyrotropin alfa - A recombinant form of the human anterior pituitary glycoprotein thyroid stimulating hormone (TSH) with use in the diagnostic setting. With an amino acid sequence identical to that of human TSH, thyrotropin alfa binds to TSH receptors on normal thyroid epithelial cells or well-differentiated thyroid cancer cells, stimulating iodine uptake and organification, synthesis and secretion of thyroglobulin (Tg), triiodothyronine (T3), and thyroxine (T4).
  • Recombinant transforming growth factor-beta - A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine transforming growth factor-beta (TGF-beta) with proapoptotic and antineoplastic properties. TGF-beta may suppress tumor cell growth by decreasing the expression of cyclin D1, a cell cycle regulatory protein, and downregulating the expression of the oncogene c-myc. This agent is also involved in T cell-mediated immunosuppression by CD4+CD25+ T cells, which permits cancer cells to evade immune surveillance.
  • Recombinant transforming growth factor-beta-2 - A recombinant polypeptide chemically identical to or similar to the endogenous cytokine transforming growth factor-beta-2 (TGF-beta-2). TGF-beta-2 modulates cell growth and immune function and may promote or inhibit tumor growth, depending on the tumor cell type. TGF-beta-2 may also suppress host immune system recognition of and/or response to tumor cells.
  • Recombinant tumor necrosis factor family protein - A recombinant therapeutic agent which is chemically identical to or similar to one of a number of endogenous tumor necrosis factor (TNF) proteins. TNF family cytokines bind to and activate specific cell-surface receptors, thereby mediating inflammatory processes, cell proliferation, immunity, angiogenesis, and tumor cell cytotoxicity. One primary antitumor effect of TNFs involves stimulation of T cell-mediated antitumor cytotoxicity.
  • Recombinant tumor necrosis factor-alpha - A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine tumor necrosis factor-alpha with antineoplastic properties. Tumor necrosis factor-alpha binds to and activates "death receptors" on the cell surface, resulting in apoptosis and cell death by the p53-independent extrinsic pathway. This agent also disrupts tumor vascularization.
  • Recombinant tyrosinase-related protein-2 - A recombinant therapeutic agent which is chemically identical to or similar to an endogenous non-mutated melanocyte differentiation antigen expressed by both normal and malignant melanocytes. Vaccinations with recombinant tyrosinase-related protein-2 may elicit an antitumoral cytotoxic T-cell response against tumor cells and some normal cells that express tyrosinase-related protein-2.
  • Recombinant vaccinia df3/muc1 vaccine - A vaccinia virus based vaccine expressing human tumor associated epithelial mucin (DF3 antigen; MUC1). MUC1 antigen, a membrane bound glycoprotein expressed by most glandular and ductal epithelial cells, is overexpressed in various tumors such as breast, prostate, and ovarian cancers. This vaccine could be used in development of immunotherapeutics against cancers expressing MUC1.
  • Recombinant vaccinia psa vaccine - A vaccine consisting of recombinant vaccinia virus encoding prostate specific antigen (PSA). Vaccination with recombinant vaccinia prostate-specific antigen vaccine stimulates the host immune system to mount a cytotoxic T-cell response against tumor cells expressing PSA.
  • Recombinant vaccinia-b7.1 vaccine - A recombinant vaccinia virus encoding the T-cell co-stimulatory molecule B7-1. Co-administration of recombinant vaccinia-B7.1 and a tumor-associated antigen vaccine may enhance tumor-associated antigen-specific T-cell responses.
  • Recombinant vaccinia-cea(6d)-tricom vaccine - A vaccine consisting of recombinant vaccinia virus encoding the tumor-associated antigen carcinoembryonic antigen (CEA) and a TRIad of COstimulatory Molecules (B7-1, ICAM-1, and LFA-3; also called TRICOM). Vaccination with recombinant vaccinia-CEA(6D)-TRICOM vaccine stimulates the host immune system to mount a T-cell response against tumor cells expressing the CEA antigen. The use of TRICOM in the vaccine may elicit a greater antitumor cytotoxic T lymphocyte (CTL) immune response compared to the use of vaccinia-CEA alone.
  • Recombinant vaccinia-muc-1 vaccine - A vaccine containing a recombinant vaccinia virus that encodes the gene for human mucin-1, a tumor-associated antigen. Upon administration, recombinant vaccinia-MUC-1 vaccine may elicit a MUC-1-specific cytotoxic T cell response against tumor cells bearing MUC-1.
  • Recombinant vaccinia-multiepitope melanoma peptides-b7.1-b7.2 vaccine - A cancer vaccine consisting of an inactivated recombinant vaccinia virus encoding epitope peptides derived from melanoma-related HLA-A2-restricted tumor-associated antigens (TAAs), including Melan-A(27-35), gp100(280-288) and tyrosinase(1-9), and two co-stimulatory B7 proteins, B7.1 (CD80) and B7.2 (CD86). Upon administration, recombinant vaccinia-multiepitope melanoma peptides-B7.1-B7.2 vaccine may stimulate a cytotoxic T-lymphocyte response against melanoma cells that express TAAs which share epitopes with the epitope peptides expressed by the vaccine viral vector, resulting in tumor cell lysis; vaccine viral vector-expressed co-stimulatory proteins B7.1 and B7.2 may enhance the cytotoxic T-lymphocyte immune response to the TAAs.
  • Recombinant vaccinia-ny-eso-1 vaccine - A cancer vaccine consisting of a recombinant vaccinia viral vector encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1, an antigen found in normal testis and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. Vaccination with recombinant vaccinia NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis. (NCI05)
  • Recombinant vaccinia-tricom vaccine - A vaccine consisting of recombinant vaccinia virus encoding a TRIad of COstimulatory Molecules (B7-1, ICAM-1, and LFA-3; also called TRICOM). Vaccination with recombinant vaccinia-TRICOM vaccine stimulates the host immune system to mount a non-specific T-cell response. With the addition of a tumor-associated antigen peptide, this vaccine may enhance a tumor-specific immune response.
  • Recombinant vesicular stomatitis virus-expressing human interferon beta and sodium-iodide symporter - A recombinant, replication competent form of the oncolytic RNA virus vesicular stomatitis virus (VSV), based on the Indiana strain of VSV, that is genetically engineered to express the genes for the human cytokine interferon beta (IFNbeta) and the human thyroidal sodium-iodide symporter (NIS), with potential oncolytic and imaging activities. Upon intravenous administration, VSV-hIFNbeta-NIS is preferentially taken up by tumor cells, resulting in tumor cell infection, viral replication and a direct virus-mediated cytolytic effect against the infected tumor cells. IFN-mediated signaling is defective in tumor cells and tumor cells are unable to exert an anti-viral response against VSV. As normal, healthy cells secrete and respond normally to IFNbeta and are able to activate IFN-mediated anti-viral pathways, the expressed IFNbeta from the VSV-infected tumor cells helps protect normal cells from VSV infection. Upon subsequent administration of certain isotope-containing imaging agents, NIS expression by the infected tumor cells allows visualization and tracking of VSV biodistribution, and analysis and quantification of VSV-infected tumor cells by positron emission tomography (PET). Also, upon subsequent administration of the radioisotope iodine I 131 (I131), I131 can be taken up by NIS and allows for a cytotoxic dose of radiation to accumulate in the NIS-expressing VSV-infected tumor cells, which also leads to tumor cell death.
  • Recombinant vesicular stomatitis virus-expressing interferon-beta - A recombinant, replicating oncolytic vesicular stomatitis virus (VSV) carrying the human interferon-beta (IFN-b) gene, with potential immunomodulating and antineoplastic activities. Upon intratumoral administration, recombinant VSV expressing IFN-b replicates in the tumor environment specifically, partially due to defective innate antiviral host defense mechanisms in tumor cells, involving type I IFNs, and exerts its cytolytic activity towards the tumor cells. By expressing human IFN-b, an INF-b-mediated antiviral immune response in surrounding normal cells is activated which protects normal cells against virus replication and VSV-mediated cell lysis. However, tumor cells have a defective IFN-b-mediated innate antiviral immune response allowing for VSV to replicate in these cells without interference. In addition, the IFN-b produced by VSV may activate an immune response in surrounding normal cells and may activate T-lymphocytes, dendritic cells and natural killer cells; thus, inducing an anti-tumor immune response against the tumor cells. VSV, a single-stranded RNA virus belonging to the genus Vesiculovirus of the family Rhabdoviridae, is relatively nonpathogenic to healthy humans.
  • Recombinant vesicular stomatitis virus-expressing interferon-beta and tyrosinase related protein 1 - A recombinant, replicating oncolytic vesicular stomatitis virus (VSV) carrying the human interferon-beta (IFN-b) gene and the tyrosinase related protein 1 (TYRP1) gene, with potential immunomodulating and antineoplastic activities. Upon intratumoral and intravenous administration, recombinant VSV-expressing IFN-b/TYRP1 preferentially replicates in tumor cells. Due to defective IFN-b-mediated innate antiviral host defense mechanisms in tumor cells, VSV is able to replicate in these cells without interference. This induces VSV-mediated cytolytic activity towards the tumor cells. By expressing human IFN-b, an IFN-b-mediated antiviral immune response in surrounding normal cells is activated which protects normal cells against virus replication and the associated VSV-mediated cell lysis. Also, the IFN-b produced by VSV may activate an immune response in surrounding normal cells, involving the activation of cytotoxic T-lymphocytes (CTL), dendritic cells (DCs) and natural killer (NK) cells. This induces an anti-tumor immune response against the tumor cells. In addition, the expression of TYRP1 further activates the immune system to induce a CTL-mediated immune response against the TYRP1-expressing tumor cells, thereby further killing TYRP1-expressing tumor cells. VSV, a single-stranded RNA virus belonging to the genus Vesiculovirus of the family Rhabdoviridae, is relatively nonpathogenic to healthy humans but is able to rapidly replicate in and induce apoptosis of tumor cells. TYRP1, a tumor-associated antigen (TAA), is primarily expressed in melanocytes and melanomas.
  • Redaporfin - A bacteriochlorin-based photosensitizer, with antineoplastic activity upon photodynamic therapy (PDT). Following intravenous administration, redaporfin preferentially accumulates in hyperproliferative tissues, such as tumors. Local application of laser light at the tumor site results in the absorption of light by this agent and a photodynamic reaction between LUZ 11 and oxygen. This results in the production of reactive oxygen species (ROS), which includes singlet oxygen molecules, the superoxide ion, and other cytotoxic free radicals. The formation of ROS induces free radical-mediated DNA damage and cell death.
  • Refametinib - An orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Refametinib specifically inhibits mitogen-activated protein kinase kinase 1 (MAP2K1 or MAPK/ERK kinase 1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers.
  • Regorafenib - An orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling.
  • Relacorilant - An orally available antagonist of the glucocorticoid receptor (GR), with potential antineoplastic activity. Upon administration, relacorilant competitively binds to and blocks GRs. This inhibits the activity of GRs, and prevents both the translocation of the ligand-GR complexes to the nucleus and gene expression of GR-associated genes. This decreases the negative effects that result from excess levels of endogenous glucocorticoids, like those seen when tumors overproduce glucocorticoids. In addition, by binding to GRs and preventing their activity, inhibition with CORT125134 also inhibits the proliferation of GR-overexpressing cancer cells. GRs are overexpressed in certain tumor cell types and promote tumor cell proliferation.
  • Relatlimab - A monoclonal antibody directed against the inhibitor receptor lymphocyte activation gene-3 (LAG-3), with potential immunomodulating and antineoplastic activities. Upon administration, relatlimab binds to LAG-3 on tumor infiltrating lymphocytes (TILs). This may activate antigen-specific T-lymphocytes and enhance cytotoxic T cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG-3 is a member of the immunoglobulin superfamily (IgSF) and binds to major histocompatibility complex (MHC) class II. LAG-3 expression on TILs is associated with tumor-mediated immune suppression.
  • Relugolix - An orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.
  • Remetinostat - A topical formulation containing the histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Upon cutaneous administration, SHP-141 selectively binds to and inhibits HDAC, resulting in an accumulation of highly acetylated histones in the skin (dermis and epidermis), the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes. These events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins. Topical administration of SHP-141 allows for high concentrations of this agent locally while minimizing systemic toxicity.
  • Renal cell carcinoma peptides vaccine ima901 - A multipeptide cancer vaccine targeting renal cell carcinoma with potential immunopotentiating activity. Renal cell carcinoma peptides vaccine IMA901 consists of 10 different synthetic tumor-associated peptide (TUMAP) antigens (9 HLA-class I-binding and 1 HLA class II-binding); endogenously, these TUMAPs are expressed by the majority of renal cell carcinomas. Vaccination with this agent may significantly increase host cytotoxic T-lymphocyte (CTL) immune responses against tumor cells expressing these peptide antigens.
  • Reparixin - An orally available inhibitor of CXC chemokine receptor types 1 (CXCR1) and 2 (CXCR2), with potential antineoplastic activity. Upon administration, reparixin allosterically binds to CXCR1 and prevents CXCR1 activation by its ligand interleukin 8 (IL-8 or CXCL8). This may cause cancer stem cell (CSC) apoptosis and may inhibit tumor cell progression and metastasis. CXCR1, overexpressed on CSCs, plays a key role in CSC survival and the ability of CSC to self-renew; it is also linked to tumor resistance to chemotherapy. Inhibition of the IL-8/CXCR1 interaction also potentiates the cytotoxic effect of chemotherapeutic agents. In addition, reparixin inhibits CXCR2 activation and may reduce both neutrophil recruitment and vascular permeability during inflammation or injury.
  • Repotrectinib - An orally available inhibitor of multiple kinases, including the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, the proto-oncogene SRC, and focal adhesion kinase (FAK), with potential antineoplastic activity. Upon oral administration, repotrectinib binds to and inhibits wild-type, point mutants and fusion proteins of ALK, ROS1, NTRK1-3, SRC, FAK and, to a lesser extent, other kinases. Inhibition of these kinases leads to the disruption of downstream signaling pathways and the inhibition of cell growth of tumors in which these kinases are overexpressed, rearranged or mutated.
  • Resiquimod - An imidazoquinolinamine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes. Due to its immunostimulatory activity, this agent may potentially be useful as a vaccine adjuvant.
  • Resiquimod topical gel - A topical gel containing the Toll-like receptor (TLR) agonist resiquimod, an imidazoquinolinamine and with potential immunomodulating activity. Resiquimod binds toTLR7 and 8, mainly on dendritic cells, macrophages, and B-lymphocytes, and activates the TLR signaling pathway, resulting in the induction of the nuclear translocation of transcription activator NF-kB and activation of other transcription factors; subsequently, gene expression increases and the production of cytokines increases, especially interferon-alpha (INF-a), resulting in the enhancement of T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate epidermal Langerhans cells, leading to an enhanced activation of T-lymphocytes.
  • Resistant starch - A form of dietary fiber that resists degradation by gastrointestinal (GI) enzymes in the small intestine with potential chemopreventive and prebiotic activity. Upon consumption of resistant starch, the fiber is not metabolized or absorbed in the small intestine and enters the colon unaltered. Once in the colon, the starch is fermented by anaerobic colonic bacteria and produces short-chain fatty acids (SCFA), including butyrate, which has anti-inflammatory and immunoregulatory activities. In addition, butyrate appears to exert antitumor effects by inhibiting tumor cell proliferation, inducing tumor cell differentiation and promoting apoptosis in colorectal cancer cells.
  • Resminostat - An orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, inhibition of the transcription of tumor suppressor genes, inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins.
  • Resveratrol - A phytoalexin derived from grapes and other food products with antioxidant and potential chemopreventive activities. Resveratrol induces phase II drug-metabolizing enzymes (anti-initiation activity); mediates anti-inflammatory effects and inhibits cyclooxygenase and hydroperoxidase functions (anti-promotion activity); and induces promyelocytic leukemia cell differentiation (anti-progression activity), thereby exhibiting activities in three major steps of carcinogenesis. This agent may inhibit TNF-induced activation of NF-kappaB in a dose- and time-dependent manner. (NCI05)
  • Resveratrol formulation srt501 - A proprietary formulation of resveratrol, a polyphenolic phytoalexin derived from grapes and other food products with potential antioxidant, anti-obesity, antidiabetic and chemopreventive activities. Resveratrol may activate sirtuin subtype 1 (SIRT-1). SIRT1 activation has been reported to inhibit tumorigenesis and tumor cell proliferation. SIRT-1 is a member of the silent information regulator 2 (SIR2) (or sirtuin) family of enzymes that plays an important role in mitochondrial activity and acts as a protein deacetylase. SIRT1 appears to be involved in the regulation of numerous transcription factors such as NF-kB and p53.
  • Ret inhibitor ds-5010 - An orally bioavailable selective inhibitor of wild-type, fusion products and mutated forms, including gatekeeper mutations, of the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, DS-5010 selectively binds to and inhibits the activity of RET. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.
  • Ret/src inhibitor tpx-0046 - An orally bioavailable selective dual inhibitor of fusions and mutations involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (ret) and the src family tyrosine kinases, with potential antineoplastic activity. Upon oral administration, the RET/SRC inhibitor TPX-0046 specifically targets and binds to ret mutants and ret-containing fusion products. This results in an inhibition of cell growth of tumor cells that exhibit increased ret activity. By inhibiting src kinase-mediated signaling and reducing the src-initiated recruitment of multiple receptor tyrosine kinases involved in bypass resistance, TPX-0046 may be able to overcome tumor resistance which may increase its therapeutic effect. Ret overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of ret tyrosine kinase activity in various cancer cell types; dysregulation of ret activity plays a key role in the development and progression of these cancers. Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation, survival, migration, invasion and angiogenesis. Src upregulation is seen in tumors with acquired resistance to RET inhibitors.
  • Retaspimycin - A small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis.
  • Retaspimycin hydrochloride - The hydrochloride salt of a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis.
  • Retelliptine - An ellipticine derivative and topoisomerase II inhibitor with antineoplastic activity. Retelliptine intercalates with DNA and inhibits topoisomerase II during DNA replication. In addition, this agent appears to induce cell cycle arrest at G2/M phase and apoptosis mediated through the Fas/Fas ligand death receptor and the mitochondrial pathway.
  • Retifanlimab - A proprietary humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, retifanlimab binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T-cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T-cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
  • Retinoic acid agent ro 16-9100 - A synthetic retinoid with differentiation inducing and potential antineoplastic activities. Like other retinoic acid agents, Ro 16-9100 binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells.
  • Retinoid 9cuab30 - A synthetic analogue of 9-cis retinoic acid with potential antineoplastic and chemopreventive activities. Retinoid 9cUAB30 binds to and activates retinoid X receptor (RXR) homodimers and/or and retinoic acid receptor (RAR)/RXR heterodimers, which may result in the dissociation of corepressor protein and the recruitment of coactivator protein, followed by transcription of downstream target genes into mRNAs and protein translation. Gene transcription regulated by these transcription factors may result in inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells.
  • Retinol - The fat soluble vitamin retinol. Vitamin A binds to and activates retinoid receptors (RARs), thereby inducing cell differentiation and apoptosis of some cancer cell types and inhibiting carcinogenesis. Vitamin A plays an essential role in many physiologic processes, including proper functioning of the retina, growth and differentiation of target tissues, proper functioning of the reproductive organs, and modulation of immune function.
  • Retinyl acetate - A naturally-occurring fatty acid ester form of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Retinyl acetate binds to and activates retinoid receptors, inducing cell differentiation and decreasing cell proliferation. This agent also inhibits carcinogen-induced neoplastic transformation in some cancer cell types and exhibits immunomodulatory properties.
  • Retinyl palmitate - A naturally-occurring phenyl analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. As the most common form of vitamin A taken for dietary supplementation, retinyl palmitate binds to and activates retinoid receptors, thereby inducing cell differentiation and decreasing cell proliferation. This agent also inhibits carcinogen-induced neoplastic transformation, induces apoptosis in some cancer cell types, and exhibits immunomodulatory properties.
  • Retrovector encoding mutant anti-cyclin g1 - A replication-incompetent, pathotropic, tumor matrix (collagen)-targeted, retroviral vector encoding an N-terminal deletion mutant form of the cyclin G1 gene with potential antineoplastic activity. Under the control of a hybrid long-terminal repeat/cytomegalovirus (CMV) promoter, retrovector encoding mutant anti-cyclin G expresses the mutant cyclin G1 construct, resulting in disruption of tumor cell cyclin G1 activity and decreased cellular proliferation and angiogenesis. This agent preferentially targets collagen of the tumor matrix because of the incorporation of the collagen-binding domain of von Willebrand factor (vWF) on the retrovector surface. Exploiting the collagen-targeting mechanism of vWF permits delivery of the retrovector to tumor sites where angiogenesis and collagen matrix exposure occur.
  • Revdofilimab - An agonistic humanized IgG1 monoclonal antibody that recognizes the co-stimulatory receptor OX40 (CD134; tumor necrosis factor receptor superfamily member 4; TNFRSF4), with potential immunostimulatory activity. Upon administration, revdofilimab selectively binds to and activates OX40. This may induce the proliferation of memory and effector T-lymphocytes and inhibit the function of T-regulatory cells (Tregs) in the tumor microenvironment (TME). OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes and plays an essential role in T-cell activation and differentiation.
  • Rexinoid nrx 194204 - An orally bioavailable synthetic retinoid X receptor (RXR) agonist with potential antineoplastic and anti-inflammatory activities. Rexinoid NRX 194204 selectively binds to and activates RXRs. Because RXRs can form heterodimers with several nuclear receptors (NRs), RXR activation by this agent may result in a broad range of gene expression depending on the effector DNA response elements activated. Rexinoid NRX 194204 may inhibit the tumor-necrosis factor (TNF)-mediated release of nitric oxide (NO) and interleukin 6 (IL6) and may inhibit tumor cell proliferation. This agent appears to be less toxic than RAR-selective ligands.
  • Rezivertinib - An orally available third-generation and selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations, including the resistance mutations T790M and L858R, as well as exon 19 deletion, with potential antineoplastic activity. Upon administration, rezivertinib specifically and covalently binds to and inhibits selective EGFR mutations, with particularly high selectivity against the T790M mutation, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, BPI-7711 may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity against wild-type EGFR (wt EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit wt EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • Rft5-dga immunotoxin imtox25 - A recombinant immunotoxin consisting of the anti-CD25 monoclonal antibody RFT5 fused to the deglycosylated ricin A-chain (dgA) with potential antitumor activity. The monoclonal antibody moiety of RFT5-dgA immunotoxin attaches to CD25 (the alpha chain of the IL-2 receptor complex) on the cell membrane; after internalization, the dgA moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. CD25 is expressed on activated normal T and B cells and macrophages and is frequently upregulated in many hematologic malignancies.
  • Rhenium re 188 bmeda-labeled liposomes - A liposome-based preparation consisting of the beta- and gamma-emitting radionuclide rhenium Re 188 (Re 188) linked to the chelator N,N-bis (2-mercaptoethyl)-N',N'-diethylethylenediamine (BMEDA) and encapsulated in liposomes, with potential tumor imaging and antineoplastic activities. Upon intravenous infusion of rhenium Re 188 BMEDA-labeled liposomes, the liposomes selectively target tumor cells, facilitate the retention of the radioisotope by those cells, and cause localized antitumor radiocytotoxicity while sparing surrounding normal, healthy cells. In addition, Re 188 BMEDA-labeled liposomes can be used for imaging purposes. Re 188 has a short half-life and a short path length, which further contribute to limiting the radiotoxicity to the tumor cells.
  • Rhenium re-186 hydroxyethylidene diphosphonate - An synthetic compound containing the organic phosphonate hydroxyethylidene diphosphonate (HEDP) labeled with the radioisotope rhenium Re 186. Re-186 hydroxyethylidene diphosphonate binds to hydroxyapatite in bone, delivering a cytotoxic dose of beta radiation to primary and metastatic bone tumors. Re-186 is a beta emitter with a short half-life, a radioisotope profile that provides localized antitumor radiocytotoxicity while sparing extramedullary bone marrow tissues.
  • Rhenium re-188 ethiodized oil - A rhenium (Re) 188 conjugate of ethiodized oil (lipiodol), an iodinated ethyl ester derived from poppy seed oil, with potential antineoplastic activity. Upon hepatic intra-arterial injection rhenium Re 188 ethiodized oil accumulates in hepatocellular carcinoma (HCC) tumor cells, thereby delivering a cytotoxic dose of radiation through Re 188 directly to the tumor cells. This may kill tumor cells while sparing surrounding normal cells and tissues. Compared to iodine I 131, Re 188 has a shorter half-life.
  • Rhenium re-188 etidronate - A synthetic compound containing the bisphosphonate etidronate (hydroxyethylidene diphosphonate, HEDP) labeled with rhenium Re188, a beta-emitting radioisotope with potential antineoplastic activity. Upon administration, Re-188 etidronate binds to hydroxyapatite in bone, delivering a cytotoxic dose of beta radiation to primary and metastatic bone tumors. The beta-radiation may provide localized anti-tumor radiotoxicity while sparing extramedullary bone marrow tissues.
  • Rhizoxin - A macrocyclic lactone. Rhizoxin binds to tubulin and inhibits microtubule assembly, thereby inducing cytotoxicity. This agent also may inhibit endothelial cell-induced angiogenic activity, which may result in decreased tumor cell proliferation.
  • Rhoc peptide vaccine rv001v - A cancer vaccine composed of an immunogenic peptide derived from the Ras homolog family member C (RhoC; Rho-related GTP-binding protein RhoC) that is emulsified in the immunoadjuvant montanide ISA-51, with potential immunomodulating and antineoplastic activities. Upon subcutaneous administration, RhoC peptide vaccine RV001V may stimulate the host immune system to mount a humoral and cytotoxic T-lymphocyte (CTL) response against tumor cells expressing RhoC, which results in tumor cell lysis. RhoC, a tumor-associated antigen (TAA) that is overexpressed in a variety of tumor cell types, is associated with increased metastatic potential.
  • Ribociclib - An orally available cyclin-dependent kinase (CDK) inhibitor targets at cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. Ribociclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.
  • Ribociclib/letrozole - An orally available co-packaged agent combination of ribociclib, a cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6, and letrozole, a nonsteroidal inhibitor of estrogen synthesis, with antineoplastic activity. Ribociclib specifically inhibits CDK4 and CDK6, thereby inhibiting retinoblastoma (Rb) phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Letrozole selectively and reversibly inhibits aromatase, which may result in growth inhibition of estrogen-dependent cancer cells.
  • Ribonuclease qbi-139 - A nuclease of mammalian origin that cleaves the phosphodiester bond between nucleotides of ribonucleic acids with potential antineoplastic activity. Ribonuclease QBI-139 catalyzes the hydrolysis and degradation of RNA leading to the inhibition of protein synthesis and cell death.
  • Ribozyme rpi.4610 - A nuclease-stabilized synthetic ribozyme (ribonucleic acid enzyme) with potential anti-angiogenesis activity. Ribozyme RPI.4610 specifically recognizes the mRNA for FLT1 (vascular endothelial growth factor receptor 1; VEGFR1), and hydrolyzes the mRNA, thereby preventing VEGFR1 proteins from being made. This may prevent VEGF-stimulated angiogenesis in cancerous tissue and metastasis.
  • Rice bran - The nutrient-rich hard outer layer of the rice cereal grain, with potential chemopreventive, antioxidant, iron chelating, anticholesterol and anti-inflammatory activities. Rice bran is rich in fiber, such as beta-glucan, pectin and gum; it also comprises vitamins and minerals, such as iron, magnesium and phosphorus, and essential fatty acids. In addition, Rice bran contains various bioactive components, including ferulic acid, tricin, beta-sitosterol, gamma-oryzanol, phytic acid, and inositol hexaphosphate (IP6). The potential anticancer activity of rice bran may be due to the synergistic effects of these phytochemicals on their ability to induce apoptosis, inhibit cell proliferation, and alter cell cycle progression in cancer cells. Rice bran's bioactive components also protect against tissue damage by scavenging free radicals and blocking chronic inflammatory responses. In addition, they are able to modulate the gut microflora and carcinogen-metabolizing enzymes, thereby further exerting a chemopreventive effect.
  • Ricolinostat - An orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. Ricolinostat selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. This leads to an accumulation of unfolded and misfolded ubiquitinated proteins and may eventually induce cancer cell apoptosis, and inhibition of cancer cell growth. HDAC6, a class II HDAC deacetylase located in the cytoplasm, appears to play a key role in the formation and activation of the aggresomes needed for degradation of misfolded proteins. Compared to non-selective HDAC inhibitor, ACY-1215 is able to reduce the toxic effects on normal, healthy cells.
  • Ridaforolimus - A small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.
  • Rigosertib sodium - The sodium salt form of rigosertib, a synthetic benzyl styryl sulfone analogue and Ras mimetic, with potential antineoplastic activity. Upon administration, rigosertib targets and binds to Ras-binding domain (RBD) found in many Ras effector proteins, including Raf kinase and phosphatidylinositol 3-kinase (PI3K). This prevents Ras from binding to its targets and inhibits Ras-mediated signaling pathways, including Ras/Raf/Erk, Ras/CRAF/polo-like kinase1 (Plk1), and Ras/ PI3K/Akt signaling pathways. This induces cell cycle arrest and apoptosis and inhibits proliferation in a variety of susceptible tumor cells.
  • Rilimogene galvacirepvec - A vaccine formulation consisting of recombinant vaccinia virus encoding prostate specific antigen (PSA) and recombinant vaccinia virus encoding three co-stimulatory molecule transgenes B7.1, ICAM-1, and LFA-3 (TRICOM). Vaccination with PSA in combination with TRICOM may enhance antigen presentation, resulting in the augmentation of a cytotoxic T cell (CTL) immune response against tumor cells expressing PSA.
  • Rilimogene galvacirepvec/rilimogene glafolivec - A vaccine formulation consisting of rilimogene galvacirepvec (V-PSA-TRICOM; PROSTVAC-V), a recombinant vaccinia virus, and rilimogene glafolivec (F-PSA-TRICOM; PROSTVAC-F), a recombinant fowlpox virus, with potential immunostimulating and antineoplastic activities. Both viruses encode modified forms of human prostate specific antigen (PSA) and the three co-stimulatory molecule transgenes (TRIad of COstimulatory Molecules; TRICOM), B7.1 (CD80), intercellular adhesion molecule-1 (ICAM-1), and lymphocyte function-associated antigen-3 (LFA-3). Using a prime-boost vaccine regimen, with a primary vaccination of rilimogene galvacirepvec followed by multiple booster vaccinations of rilimogene glafolivec, the PSA-TRICOM vaccines infect antigen-presenting cells (APCs), such as dendritic cells (DCs). Upon processing and expression of the PSA and TRICOM proteins on their surfaces, the DCs are able to initiate cytotoxic T-lymphocyte (CTL) responses against PSA-expressing cancer cells. The combination of PSA and TRICOM greatly enhances T-cell activation and T-cell-mediated tumor cell killing.
  • Rilimogene glafolivec - A cancer vaccine consisting of a recombinant fowlpox virus encoding fragment of human prostate-specific antigen (PSA), PSA:154-163 (155L), and a TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3) (TRICOM). Administration of this agent may induce a cytotoxic T cell response against PSA-expressing tumor cells. Dendritic cells infected with TRICOM vectors greatly enhance naive T-cell activation and peptide-specific T-cell stimulation. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
  • Rilotumumab - A fully human IgG2 monoclonal antibody directed against the human hepatocyte growth factor (HGF) with potential antineoplastic activity. Anti-HGF monoclonal antibody AMG 102 binds to and neutralizes HGF, preventing the binding of HGF to its receptor c-Met and so c-Met activation; inhibition of c-Met-mediated signal transduction may result in the induction of apoptosis in cells expressing c-Met. c-Met (HGF receptor or HGFR), a receptor tyrosine kinase overexpressed or mutated in a variety of epithelial cancer cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.
  • Rindopepimut - A cancer vaccine consisting of a human epidermal growth factor receptor variant III (EGFRvIIi)-specific peptide conjugated to the non-specific immunomodulator keyhole limpet hemocyanin (KLH) with potential antineoplastic activity. Vaccination with rindopepimut may elicit a cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing EGFRvIII. EGFRvIII, a functional variant of EGFR that is not expressed in normal tissues, was originally discovered in glioblastoma multiforme (GBM) and has also been found in various other cancers such as breast, ovarian, metastatic prostate, colorectal, and head and neck cancers. EGFRvIII contains an 83 amino acid deletion in its extracellular domain and has been shown to transform NIH/3T3 mouse embryonic fibroblast cells in vitro.
  • Ripertamab - A chimeric monoclonal antibody directed against human CD20, with potential antineoplastic activity. Ripertamab binds to the B-cell-specific cell surface antigen CD20, which triggers an immune response against CD20-positive B-cells, leading to apoptosis. CD20, a non-glycosylated cell surface phosphoprotein, is exclusively expressed on B-cells during most stages of B-cell development and is often overexpressed in B-cell malignancies.
  • Ripk1 inhibitor gsk3145095 - An orally available, small-molecule inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1; receptor-interacting protein 1; RIP1) with potential antineoplastic and immunomodulatory activities. Upon administration, GSK3145095 disrupts RIPK1-mediated signaling, which may reduce C-X-C motif chemokine ligand 1 (CXCL1)-driven recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment (TME). This allows effector cells, such as natural killer (NK) cells and cytotoxic T-lymphocytes (CTLs), to kill and eliminate cancer cells. RIPK1, a serine-threonine kinase that normally plays a key role in inflammation and cell death in response to tissue damage and pathogen recognition, is overexpressed in certain cancer types and may be associated with oncogenesis and promotion of the immunosuppressive nature of the TME.
  • Ripretinib - An orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) KIT and platelet-derived growth factor receptor alpha (PDGFR-alpha; PDGFRa), with potential antineoplastic activity. Upon oral administration, ripretinib targets and binds to both wild-type and mutant forms of KIT and PDGFRa specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. This abrogates KIT/PDGFRa-mediated tumor cell signaling and prevents proliferation in KIT/PDGFRa-driven cancers. DCC-2618 also inhibits several other kinases, including vascular endothelial growth factor receptor type 2 (VEGFR2; KDR), angiopoietin-1 receptor (TIE2; TEK), PDGFR-beta and macrophage colony-stimulating factor 1 receptor (FMS; CSF1R), thereby further inhibiting tumor cell growth. KIT and PDGFRa are tyrosine kinase receptors that are upregulated or mutated in a variety of cancer cell types; mutated forms play a key role in the regulation of tumor cell proliferation and resistance to chemotherapy.
  • Risperidone formulation in rumenic acid - An orally bioavailable capsule formulation containing the antipsychotic agent risperidone suspended in the lipid rumenic acid, with potential antineoplastic activity. Upon administration of VAL401, risperidone may, through an as of yet not elucidated mechanism of action, reduce cellular activity and tumor cell proliferation in multiple cancers.
  • Ritrosulfan - A sulfonate-based alkylation agent with potential antineoplastic activity. Ritrosulfan appears to alkylate DNA, thereby producing DNA crosslinks, resulting in cell cycle arrest.
  • Rituximab - A recombinant chimeric murine/human antibody directed against the CD20 antigen, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes. Following binding, rituximab triggers a host cytotoxic immune response against CD20-positive cells.
  • Rituximab and hyaluronidase human - A combination preparation of rituximab, a genetically engineered chimeric murine/human immunoglobulin (Ig) G1 kappa monoclonal antibody directed against the CD20 antigen, and the recombinant form of the human enzyme hyaluronidase, with antineoplastic activity. Upon subcutaneous administration of rituximab and hyaluronidase human, the hyaluronidase reversibly depolymerizes the polysaccharide hyaluronan in the subcutaneous tissue. This increases the permeability of the subcutaneous tissue and enhances the absorption of rituximab into the systemic circulation. In turn, rituximab targets and binds to CD20 expressed on tumor cells, and induces tumor cell lysis primarily through the induction of complement dependent cytotoxicity (CDC) and antibody-dependent cell mediated cytotoxicity (ADCC). When administered subcutaneously, hyaluronidase, an endoglycosidase, increases the dispersion and absorption of co-administered drugs. CD20 is expressed on the surface of pre-B and mature B-lymphocytes, and is overexpressed in a variety of B-cell malignancies.
  • Rituximab conjugate con-4619 - A proprietary conjugate of rituximab, a recombinant chimeric murine/human antibody directed against the CD20 antigen, with potential antineoplastic activity. Upon administration of the rituximab conjugate CON-4619, the rituximab moiety targets and binds to CD20, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes. Following binding, rituximab triggers a host cytotoxic immune response against CD20-positive cells.
  • Riviciclib - A flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. Riviciclib selectively binds to and inhibits Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation.
  • Rivoceranib mesylate - The mesylate salt of rivoceranib, an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Rivoceranib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.
  • Rna electroporated cd19car-cd3zeta-4-1bb-expressing autologous t-lymphocytes - Autologous, genetically engineered T-lymphocytes that have been electroporated with an mRNA encoding for an anti-CD19 chimeric antigen receptor (CAR) consisting of an anti-CD19 single chain variable fragment (scFv) coupled to the co-stimulatory signaling domain of 4-1BB (CD137) and the zeta chain of the T-cell receptor CD3 complex (CD3-zeta), with potential immunomodulating and antineoplastic activities. Upon transfusion, the RNA electroporated CD19CAR-CD3zeta-4-1BB-expressing autologous T-lymphocytes attach to cancer cells expressing CD19. This induces selective toxicity against CD19-expressing tumor cells and causes tumor cell lysis. The 4-1BB co-stimulatory molecule signaling domain enhances T-cell activation and signaling after recognition of CD19. CD19 antigen is a B-cell specific cell surface antigen, which is expressed in all B-cell lineage malignancies.
  • Rnr inhibitor coh29 - An orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity. Upon oral administration, the RNR inhibitor COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail. This blocks the interaction between the hRRM1 and hRRM2 subunits and interferes with the assembly of the active hRRM1/hRRM2 complex of RNR. Inhibition of RNR activity decreases the pool of deoxyribonucleotide triphosphates available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, which prevents the repair of damaged DNA, and causes both the accumulation of single and double strand DNA breaks and the induction of apoptosis. RNR, an enzyme that catalyzes the conversion of ribonucleoside diphosphate to deoxyribonucleoside diphosphate, is essential for de novo DNA synthesis and plays an important role in cell growth; it is overexpressed in many cancer cell types and is associated with increased drug resistance, cancer cell growth and metastasis.
  • Robatumumab - A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R fully human monoclonal antibody SCH 717454 binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; downregulation of this survival pathway may result in the induction of apoptosis and decreased cellular proliferation. The activation of IGF-1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis.
  • Roblitinib - An inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, roblitinib binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.
  • Robo1-targeted bicar-nkt cells - A preparation of natural killer T (NKT) cells engineered to express a chimeric antigen receptor (CAR) specific for roundabout homolog 1 (ROBO1, Robo1), with potential immunostimulating and antineoplastic activities. Upon administration, the ROBO1-targeted BiCAR-NK/T cells target and bind to ROBO1 expressed on the surface of tumor cells. This induces selective toxicity in ROBO1-expressing tumor cells. ROBO1, a member of the axon guidance receptor family, is often overexpressed in a variety of tumor types. It is involved in axon guidance, cell proliferation, cell motility and angiogenesis.
  • Rocakinogene sifuplasmid - A plasmid DNA vaccine encoding the human pro-inflammatory cytokine interleukin-12 (IL-12) with potential immunoactivating activity. Upon intramuscular delivery by electroporation of rocakinogene sifuplasmid, IL-12 is translated in cells and activates the immune system by promoting the activation of natural killer cells (NK cells), inducing secretion of interferon-gamma and promoting cytotoxic T-cell responses against tumor cells. This may result in both immune-mediated tumor cell death and the inhibition of tumor cell proliferation.
  • Rocapuldencel-t - A cancer vaccine in which autologous dendritic cells are transfected with patient-specific renal cell carcinoma (RCC) RNA and a synthetic, truncated human CD40 ligand (CD40L) RNA with potential immunostimulatory and antineoplastic activities. Individual RCC-specific RNA, encoding a unique repertoire of tumor-associated antigens (TAAs) (including telomerase reverse transcriptase, G250, and oncofetal antigen) is electroporated into autologous dendritic cells (DCs), transfected with synthetic RNA that encodes a truncated version of the T-cell protein CD40L; the transfected autologous DCs express and process both patient-specific RCC TAAs and the truncated CD40L protein. When reintroduced back to the patient, rocapuldencel-T may elicit a highly specific cytotoxic T-cell (CTL) response against RCC cells expressing the patient-specific RCC TAA repertoire. The signal cascade initiated by stimulation of the truncated, ectopically expressed co-stimulatory molecule CD40L results in the secretion of the inflammatory cytokine IL-12 downstream.
  • Rociletinib - An orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Rociletinib binds to and inhibits mutant forms of EGFR, including T790M, thereby leading to cell death of resistant tumor cells. Compared to other EGFR inhibitors, CO-1686 inhibits T790M, a secondary acquired resistance mutation, as well as other mutant EGFRs and may have therapeutic benefits in tumors with T790M-mediated resistance to other EGFR tyrosine kinase inhibitors. This agent shows minimal activity against wild-type EGFR, hence does not cause certain dose-limiting toxicities.
  • Rodorubicin - A synthetic tetraglycosidic anthracycline antibiotic with antineoplastic activity. Rodorubicin appears to intercalate DNA and causes cell death. Due to its severe cardiotoxic effects, this agent was never marketed.
  • Roducitabine - An orally available small molecule and nucleoside antimetabolite with potential antineoplastic activity. Upon administration, tRoducitabine is taken up by cells through a carrier-mediated transporter, phosphorylated by uridine cytidine kinase (UCK) and then further phosphorylated to its diphosphate (RX-DP) and triphosphate forms (RX-TP). The triphosphate form is incorporated into RNA and inhibits RNA synthesis. The diphosphate RX-DP is reduced by ribonucleotide reductase (RR) to dRX-DP; its triphosphate form (dRX-TP) is incorporated into DNA. In addition, RX-3117 also inhibits DNA methyltransferase 1 (DNMT1). This eventually leads to cell cycle arrest and the induction of apoptosis. UCK is the rate-limiting enzyme in the pyrimidine-nucleotide salvage pathway.
  • Rofecoxib - A synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.
  • Roflumilast - An orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3',5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling. cAMP prevents phosphorylation of spleen tyrosine kinase (SYK) and abrogates activation of the PI3K/AKT/mTOR signaling pathway, which may result in the induction of apoptosis. PDE4, a member of the PDE superfamily that hydrolyses cAMP and 3',5'-cyclic guanosine monophosphate (cGMP) to their inactive 5' monophosphates, is upregulated in a variety of cancers and may contribute to chemoresistance; it also plays a key role in inflammation, especially in inflammatory airway diseases.
  • Rogaratinib - A pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. Rogaratinib inhibits the activities of FGFRs, which may result in the inhibition of both tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases, which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival.
  • Rogletimide - An orally active aminoglutethimide derivative with potential antineoplastic activity. Rogletimide reversibly inhibits the activity of aromatase, a cytochrome P450 family enzyme found in many tissues and the key enzyme in the oxidative aromatization process of androgens to estrogens. In estrogen-dependent cancers, the inhibition of aromatase by this agent leads to a reduction in the synthesis of estrogen, thereby inhibiting estrogen-mediated signal transduction and consequently reducing tumor cell growth. In addition, rogletimide also inhibits enzymes that catalyzing conversion of cholesterol to corticosteroids.
  • Rolinsatamab talirine - An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against the prolactin receptor (PRLR) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration of rolinsatamab talirine, rolinsatamab targets and binds to PRLR expressed on tumor cells. Upon binding and internalization, talirine is released and kills the PRLR-expressing tumor cells, through an as of yet unknown mechanism of action. PRLR, a tumor-associated antigen (TAA), is overexpressed by a variety of tumor cell types.
  • Romidepsin - A bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several heat shock protein 90 (Hsp90)-dependent oncoproteins.
  • Roneparstat - An N-acetylated, glycol-split form of heparin that is devoid of anticoagulant activity and is an inhibitor of heparanase with antineoplastic and antiangiogenic activities. Upon subcutaneous administration, roneparstat inhibits the activity of heparanase. This prevents the heparanase-mediated cleavage of heparan sulfate (HS) proteoglycans on cell surfaces and within the extracellular matrix. In addition, this agent prevents the heparanase-induced production of a number of angiogenic growth factors, including matrix metalloproteinase-9, hepatocyte growth factor and vascular endothelial growth factor. Altogether, this leads to an inhibition of both tumor cell growth and angiogenesis. Heparanase, an enzyme that is responsible for the proteolytic cleavage of proteoglycans, is upregulated in a variety of tumor cell types and promotes tumor cell growth; it plays a key role in tumor cell invasion, metastasis and angiogenesis.
  • Roniciclib - An orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. Roniciclib selectively binds to and inhibits the activity of CDK1/Cyclin B, CDK2/Cyclin E, CDK4/Cyclin D1, and CDK9/Cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle progression and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are often dysregulated in cancerous cells.
  • Ropeginterferon alfa-2b - A long-acting formulation of recombinant interferon alpha subtype 2b (IFN-a2b), in which IFN-a2b is coupled, via proline, to polyethylene glycol (PEG), with antiviral, immunomodulating and antineoplastic activities. Upon administration of ropeginterferon alfa-2b, IFN-a2b targets and binds to specific IFN cell-surface receptors. This activates IFN-mediated signal transduction pathways and induces the transcription and translation of genes with IFN-specific response elements (ISREs). Their protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects. The PEG moiety inhibits proteolytic breakdown and clearance of IFN-a2b, which prolongs its half-life, extends the duration of its therapeutic effects and allows less frequent dosing. The proline linker facilitates the synthesis of a single positional isomer which further increases its stability and half-life.
  • Ropidoxuridine - An orally available 5-substituted 2-pyrimidinone-2'-deoxyribonucleoside analogue and prodrug of 5-iododeoxyuridine (IUdR), an iodinated analogue of deoxyuridine, with radiosensitizing activity. Upon oral administration, ropidoxuridine (IPdR) is efficiently converted to idoxuridine (IUdR) by a hepatic aldehyde oxidase. In turn, IUdR is incorporated into DNA during replication, thereby sensitizing cells to ionizing radiation by increasing DNA strand breaks. Compared to IUdR, ropidoxuridine is associated with a lower toxicity profile and improved anti-tumor activity.
  • Ropocamptide - A synthetic form of a human antimicrobial peptide (37 amino acids), belonging to the cathelicidin family, with antimicrobial, anti-inflammatory, immunostimulating and potential antineoplastic activities. Upon intratumoral injection of the ropocamptide, this peptide increases p53 expression, and induces phosphatidylserine externalization, DNA fragmentation, cell cycle arrest and caspase-independent apoptosis-inducing factor (AIF)/ endonuclease G (EndoG)-mediated apoptotic cell death in susceptible cancer cells. This suppresses tumor cell proliferation. LL-37, a protein secreted by bone marrow cells, circulating leukocytes, and various epithelial tissues, plays a crucial role in the innate host immune defense via the regulation of leukocyte chemotaxis and cytokine production; it also promotes wound healing.
  • Roquinimex - A quinoline-3-carboxamide with potential antineoplastic activity. Roquinimex inhibits endothelial cell proliferation, migration, and basement membrane invasion; reduces the secretion of the angiogenic factor tumor necrosis factor alpha by tumor-associated macrophages (TAMs); and inhibits angiogenesis. This agent is also an immune modulator that appears to alter cytokine profiles and enhance the activity of T cells, natural killer cells, and macrophages.
  • Ror1 car-specific autologous t-lymphocytes - A mixture of two T-lymphocyte preparations expressing a chimeric antigen receptor (CAR) consisting of an anti-receptor tyrosine kinase-like orphan receptor 1 (ROR1) single chain variable fragment (scFv) fused to either the co-stimulatory signaling domain cluster of differentiation 28 (CD28), and the zeta chain of the T-cell receptor (TCR)/CD3 complex (CD3-zeta) (ROR1CD28zeta), or the co-stimulatory signaling domain cluster of differentiation 137 (CD137; 4-1BB), and the zeta chain of the T-cell receptor (TCR)/CD3 complex (CD3-zeta) (ROR1CD137zeta), with potential immunomodulating and antineoplastic activities. Upon simultaneous administration of the two T-lymphocyte populations ROR1CD28zeta and ROR1CD137zeta , the ROR1 CAR-specific autologous T-lymphocytes are directed to tumor cells expressing ROR1, which may result in a selective toxicity against, and lysis of ROR1-expressing tumor cells. CD28, a T-cell surface-associated co-stimulatory molecule, is required for full T-cell activation, proliferation, and survival. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of ROR1. ROR1, also known as neurotrophic tyrosine kinase, receptor-related 1, is expressed during embryogenesis and by certain leukemias.
  • Rosabulin - A small molecule vascular disrupting agent, with potential antimitotic and antineoplastic activities. Rosabulin binds to tubulin in a similar manner as colchicine and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells, ultimately leading to cell cycle arrest and blockage of cell division. By destroying proliferating vascular cells, blood flow to the tumor is reduced and eventually leads to a decrease in tumor cell proliferation.
  • Rose bengal solution pv-10 - An injectable ten percent solution of rose bengal disodium, an iodinated fluorescein derivative, with potential antineoplastic and radiosensitizing activities. When injected into tumor tissue, PV-10 specifically targets and concentrates in tumor cells, producing cytotoxic singlet oxygen when exposed to ionizing radiation. In addition, PV-10 may stimulate an anti-tumor immune response.
  • Rosiglitazone maleate - The maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. Rosiglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation.
  • Rosmantuzumab - An immunoglobulin (Ig) G1 humanized monoclonal antibody targeting human R-spondin 3 (RSPO3), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, rosmantuzumab targets and binds to RSPO3 expressed on tumor cells. This prevents the activation of RSPO3, and inhibits both the binding of RSPO3 to leucine-rich repeat-containing G-coupled receptors (LGRs) and the activation of the RSPO-LGR pathway. This may result in an inhibition of both cancer stem cell (CSC) survival and the proliferation of cancer cells in which this pathway is overactivated. The RSPO-LGR pathway is a CSC pathway activated in a variety of cancer cell types.
  • Rosopatamab - A humanized monoclonal antibody (MoAb) against the external domain of the Prostate-specific membrane antigen (PSMA), overexpressed in the malignant prostate and its metastases. Although PSMA is not a biomarker of disease progression, over-expression indicates an aggressive phenotype of the prostate cancer. Rosopatamab was generated by replacing murine Ig sequences with human ones, thereby MoAb huJ591can be administered to patients on multiple occasions over long time periods without inducing an immune response. Radiolabelled MoAb huJ591 may be used in immunotherapy of prostate cancer.
  • Rosuvastatin - A statin with antilipidemic and potential antineoplastic activities. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. In addition, rosuvastatin, like other statins, exhibits pro-apoptotic, growth inhibitory, and pro-differentiation activities in a variety of tumor cell types; these antineoplastic activities may be due, in part, to inhibition of the isoprenylation of Ras and Rho GTPases and related signaling cascades.
  • Rovalpituzumab tesirine - An antibody-drug conjugate (ADC) containing a humanized IgG1 monoclonal antibody (MAb) directed against the delta-like protein 3 (DLL3), conjugated to the cytotoxic pyrrolobenzodiazepine (PBD) dimer D6.5 (SC-DR002) via a maleimide-containing linker with an eight-carbon polyethylene glycol spacer and a cathepsin B-cleavable valine-alanine dipeptide, with potential antineoplastic activity. The MAb moiety of rovalpituzumab tesirine selectively binds to DLL3 on tumor cell surfaces. Upon internalization of the ADC, the dipeptide linker is cleaved and D6.5 is released. Then the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of DLL3-overexpressing tumor cells. DLL3, a membrane protein that binds to Notch receptors and regulates Notch-mediated signaling and gene transcription, is overexpressed by certain cancers but is rarely expressed by normal, healthy cells.
  • Rsk1-4 inhibitor pmd-026 - An orally bioavailable inhibitor of the serine/threonine kinase p90 ribosomal S6 kinase (p90RSK; RSK) subtypes 1-4, with high selectivity for RSK subtype 2 (RSK2), with potential antineoplastic activity. Upon administration of the RSK1-4 inhibitor PMD-026, this agent targets and inhibits the RSK subtypes, thereby inhibiting RSK-mediated signaling. This prevents the phosphorylation and activation of the transcription factor Y-box binding protein-1 (YB-1) and leads to cell cycle arrest, an induction of apoptosis, and an inhibition of tumor cell proliferation in RSK-expressing tumor cells. RSK is overexpressed in a variety of cancers, especially in triple negative breast cancer (TNBC). It plays a key role in tumor cell proliferation, differentiation, survival, and metastasis.
  • Rubitecan - A semisynthetic agent related to camptothecin with potent antitumor and antiviral properties. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
  • Rucaparib - An orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types.
  • Rucaparib camsylate - The camsylate salt form of rucaparib, an orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types.
  • Rucaparib phosphate - The phosphate salt form of rucaparib, an orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types.
  • Ruthenium ru-106 - A radioactive isotope of the rare element ruthenium, a member of the light platinum group. A radioactive plaque containing ruthenium 106 may be inserted into the eye to irradiate ophthalmic tumors.
  • Ruthenium-based small molecule therapeutic bold-100 - A ruthenium-based, small molecule that selectively inhibits stress-induced upregulation of GRP78, with potential antineoplastic activity. Although the exact mechanisms(s) through which this agent exerts its effects have yet to be fully elucidated, upon administration, BOLD-100 may selectively inhibit stress-induced upregulation of GRP78, thereby preventing the activation of multiple GRP78-mediated pathways and blocking GRP78-induced suppression of apoptotic pathways. This may lead to the induction of tumor cell apoptosis and slow tumor cell proliferation. GRP78, the endoplasmic reticulum (ER) chaperone and unfolded protein response (UPR) regulator, is overexpressed on the surface of a variety of cancer cell types. Its expression is associated with increased tumor cell survival and proliferation, as well as angiogenesis and resistance to chemotherapy.
  • Ruthenium-based transferrin targeting agent nkp-1339 - A ruthenium-containing cancer agent targeting transferrin with potential antineoplastic activity. Upon intravenous administration, NKP-1339 (Ru3+) binds to transferrin (Tf) and is taken up via Tf receptors (TfR), which are overexpressed on cancer cells. Once inside the cell, NKP-1339 is released from Tf and is reduced, within the acidic environment of the endosomes, to its active form NKP-119 (Ru2+). In turn, the active form induces a redox reaction, thereby leading to the formation of reactive oxygen species (ROS) which inhibits GRP78 and SOD, endoplasmic reticulum-stress modulating molecules as well as BAG4 and ERK, program cell death regulating molecules. This eventually induces caspase-dependent apoptosis.
  • Ruxolitinib - An orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.
  • Ruxolitinib phosphate - The phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.
  • Ruxotemitide - A peptide derived from human lactoferrin, with potential lytic and immunostimulating activities. Upon transdermal injection directly into the tumor, ruxotemitide may bind to the tumor cell membranes and subsequently lyse tumor cells, thereby inducing tumor cell necrosis. In turn, presentation of the tumor antigens to the immune system may induce systemic innate and adaptive immune responses mediated by anti-tumor natural killer (NK) cells, cytotoxic T lymphocytes, and natural killer T (NKT) cells. This may trigger an immune response against tumor associated antigens on tumors distant from the primary tumor. Human lactoferrin, a 692 amino acid glycoprotein, belongs to the transferrin family of metal-binding proteins.

Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ

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