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Antineoplastic agents g

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  • G protein-coupled estrogen receptor agonist lns8801 - An orally bioavailable selective agonist of the G protein-coupled estrogen receptor (G protein-coupled estrogen receptor 1; GPER; GPER1; GPR30), with potential immunomodulating and antineoplastic activities. Upon oral administration, LNS8801 targets, binds to and activates GPER. This activates GPER-mediated signaling and suppresses the expression of various tumor-associated genes, such as c-Myc and programmed cell death-ligand 1 (PD-L1). This leads to an inhibition of tumor cell proliferation. GPER activation may also induce immune memory. GPER is a membrane protein and a member of the G-protein coupled receptors (GPCRs) that are widely distributed in various tissues. GPER is a tumor suppressor in a wide range of cell cancer types.
  • G250 peptide vaccine - A cancer vaccine containing of a synthetic form of the renal cell carcinoma (RCC)-associated antigen G250 with potential antineoplastic activity. Vaccination with G250 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the G250 antigen, resulting in decreased tumor growth. Found in the majority of renal cell carcinomas, G250 is a cell surface tumor-associated antigen (TAA) that contains an HLA-A2.1-restricted epitope that is recognized by CTLs.
  • Gadopiclenol - A gadolinium-based paramagnetic contrast agent, with potential imaging enhancing activity upon magnetic resonance imaging (MRI). Upon administration of gadopiclenol and placement in a magnetic field, this agent produces a large magnetic moment and creates a large local magnetic field, which can enhance the relaxation rate of nearby protons. This change in proton relaxation dynamics, increases the MRI signal intensity of tissues in which this agent has accumulated; therefore, contrast and visualization of those tissues is enhanced compared to unenhanced MRI.
  • Gag:267-274 peptide vaccine - A peptide vaccine containing the amino acids 267 through 274 of the human immunodeficiency virus type 1 (HIV-1) gag core protein (gag:267-274), with potential immunostimulating activity. Upon vaccination, the immune system may exert a potent cytotoxic T-lymphocyte (CTL) response against the xenoantigen gag:267-274 and produces pro-inflammatory cytokines. The concomitant administration of a cancer peptide vaccine may benefit from an already activated immune system and may augment an immune response against the administered tumor associated antigen(s). Gag:267-274 peptide is highly immunogenic and may potentially be used as a cancer immunoadjuvant.
  • Galamustine - A galactose mustard compound, an alkylating agent, with antineoplastic activity.
  • Galarubicin - An anthracycline derivative with antineoplastic activity developed to circumvent doxorubicin resistance.
  • Galectin-1 inhibitor otx008 - A calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteasomal degradation, through an as of yet not fully elucidated mechanism, and eventually downregulation of Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses.
  • Galeterone - An orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.
  • Galinpepimut-s - A peptide cancer vaccine comprised of four peptide chains derived from the Wilms' tumor gene 1 (WT1) protein, with potential immunomodulating and antineoplastic activities. Upon administration, galinpepimut-S, which is comprised of one WT1-derived peptide (WT-A1) that may stimulate CD8-positive T-cell responses; two WT1 peptides (WT1-427 long, WT1-331 long) that may stimulate CD4-positive T-cell responses; and one modified peptide (WT1-122A1 long) that may stimulate both CD4-positive and CD8-positive T-cells, may elicit a targeted innate immune response against WT1-expressing tumor cells. WT1 protein, a zinc finger DNA-binding protein and transcription factor, is overexpressed in leukemic cells and in many non-hematological solid tumors.
  • Galiximab - A chimeric IgG1 monoclonal antibody directed against CD80, the natural ligand for the T-cell antigen CD28 which mediates T-cell and B-cell adhesion. Galiximab binds to CD80 expressed on the cell surfaces of follicular lymphomas, resulting in antibody-dependent cell-mediated cytotoxicity (ADCC). CD80 is expressed on activated B-cells and gamma-interferon-stimulated monocytes and is often expressed at low levels on the surfaces of follicular lymphoma cells and other lymphoid malignancies.
  • Gallium ga 68-psma-617 - A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET)/computed tomography (CT). Upon intravenous administration of 68Ga-PSMA-617, the PSMA-617 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells can be detected during PET/CT imaging. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
  • Gallium-based bone resorption inhibitor ap-002 - An orally bioavailable gallium (Ga)-based small molecule agent with potential anti-bone resorption and antineoplastic activities. Upon oral administration, AP-002 selectively inhibits osteoclast differentiation and bone resorption, and may promote the growth of osteoblasts thereby improving the skeletal sequelae of bony metastases which include pain, spinal cord compression, fractures and hypercalcemia of malignancy. Additionally, AP-002 may, through an as of yet undescribed mechanism of action, directly target and kill bone tumor cells.
  • Galocitabine - An orally available 5-fluorouracil (5-FU) prodrug with potential antineoplastic activity. Upon administration, galocitabine is converted into 5'-deoxy-5-fluorocytidine, 5'-deoxy-fluorouridine, and 5-FU. 5-FU is further metabolized into other cytotoxic metabolites that interfere with RNA and DNA synthesis via inhibition of thymidylate synthase. As a result, this agent eventually inhibits tumor cell growth.
  • Galunisertib - An orally available, small molecule antagonist of the tyrosine kinase transforming growth factor-beta (TGF-b) receptor type 1 (TGFBR1), with potential antineoplastic activity. Upon administration, galunisertib specifically targets and binds to the kinase domain of TGFBR1, thereby preventing the activation of TGF-b-mediated signaling pathways. This may inhibit the proliferation of TGF-b-overexpressing tumor cells. Dysregulation of the TGF-b signaling pathway is seen in a number of cancers and is associated with increased cancer cell proliferation, migration, invasion and tumor progression.
  • Gamboge resin extract tsb-9-w1 - An orally bioavailable extract from the yellow to brown gum-resin of the gamboge tree (genus Garcinia) belonging to the Clusiaceae (or Guttiferae) family, with potential anti-inflammatory and antineoplastic activities. Gamboge resin extract TSB-9-W1 contains various active ingredients, including gambogic acid, formoxanthone A, betulin, betulinic acid, morellic acid, isomorellic acid, isogambogic acid, isomorellinol and desoxymorellin. Upon oral administration, the various active components of the gamboge resin extract TSB-9-W1 may bind to and inhibit the activity of a variety of cancer-related proteins, may induce apoptosis, and may exert cytotoxic activity on tumor cells, thereby inhibiting tumor cell proliferation. TSB-9 is derived from TSB-14, which is the acetone-extract of gamboge resin, and pulverized into powder form; TSB-9 is 90% extract and 10% brown sugar. TSB-9-W1 is a milled form of TSB-9 with a particle size of 5 micrometers.
  • Gamma-delta tocotrienol - An orally available nutritional supplement containing the gamma and delta forms of the vitamin E family member tocotrienol, with hypocholesterolemic, antithrombotic, antioxidant, and potential antineoplastic activity. Upon oral administration, gamma-delta tocotrienol accumulates in cancer cells and may exert their anti-cancer activity in part through 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase downregulation and/or degradation, cell cycle arrest, and induction of caspase-mediated apoptosis. In addition, this agent may inhibit angiogenesis partially through the blockage of vascular endothelial growth factor receptor (VEGFR) and the inhibition of tumor cell-induced vessel formation. Altogether, this may result in the inhibition of tumor cell growth. Further, this agent prevents free radical formation and inhibits lipid peroxidation. Tocotrienols contain 3 double bonds, absent in tocopherols, on its farnesyl isoprenoid side chain that likely contribute to its anti-cancer activities.
  • Gamma-secretase inhibitor ly3039478 - An orally available inhibitor of the integral membrane protein gamma-secretase (GS), with potential antineoplastic activity. Upon administration, gamma-secretase inhibitor LY3039478 binds to the GS protease complex, thereby blocking the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth in tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival.
  • Gamma-secretase inhibitor ro4929097 - An orally bioavailable, small-molecule gamma secretase (GS) inhibitor with potential antitumor activity. Gamma secretase inhibitor RO4929097 binds to GS and blocks activation of Notch receptors, which may inhibit tumor cell proliferation. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth.
  • Gandotinib - An orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. JAK2V617F has a substitution of phenylalanine for valine at amino acid position 617 and plays a key role in tumor cell proliferation and survival.
  • Ganetespib - A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Ganetespib binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.
  • Ganglioside gd2 - A cell surface antigen expressed on all tumors of neuroectodermal origin, including melanoma, neuroblastomas, sarcoma, astrocytomas, and small cell lung cancer. GD2, an O-acetylated disialoganglioside, belongs to the group of glycosphingolipids that are widely expressed in many tissues and organs in vertebrates and have been suggested to be involved in the regulation of development and differentiation as recognition molecules or signal modulators. Due to its high level of expression in neuroblastoma, GD2 has the potential to be used as a component of anti-neuroblastoma vaccines, in addition to being used in polyvalent anti-melanoma vaccines.
  • Ganglioside gm2 - A glycosphingolipid antigen expressed by a variety of human cancer cells. GM2 containing vaccines have been shown to elicit antibodies production in melanoma patients without deleterious effects associated with an immune response to GM2. Mutations in at least 1 of 3 recessive genes: HEXA, HEXB, and GM2A cause defects in GM2 catabolism, leading to lysosomal lipid storage disorders that manifest primarily as neurodegenerative diseases, including Tay-Sachs and Sandhoff Disease.
  • Ganitumab - A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Ganitumab binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R is a tyrosine kinase and a member of the insulin receptor family. IGF-1R activation stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis.
  • Ganoderma lucidum spores powder capsule - An orally available powder-based nutritional supplement containing the spores of the mushroom Ganoderma lucidum (Ganoderma l.), a traditional Chinese medicine, with potential protective, sedative, anti-oxidant, immunomodulating, and antineoplastic activities. The spores contain various bioactive components including polysaccharides, triterpenoids, peptidoglycans, amino acids, fatty acids, vitamins, and minerals. Upon oral administration of the Ganoderma lucidum spores powder capsule, the active ingredients may modulate the immune system, may activate dendritic cells, natural killer cells, and macrophages and may modulate the production of certain cytokines, such as tumor necrosis factor-alpha (TNFa), interleukin (IL) 1-beta (IL-1b), IL-2, IL-6 and IL-8. This supplement may improve cancer-related fatigue and may be used as a sleep aid; it may also have a beneficial effect on the heart, lung, liver, pancreas, kidney, and the central nervous system.
  • Garlic - A bulbous herb isolated from the plant Allium sativum with potential antineoplastic activity. Garlic contains a number of different organosulfur compounds, some of which have displayed antineoplastic activity.
  • Garlic extract - The alcoholic extract of the bulb or whole garlic plant Allium sativum (Liliaceae) with potential antineoplastic activity. The garlic plant has long been considered a beneficial plant for health and has been used as an antihelmintic, a rubefacient, an anti-infective, and an antihypertensive. Fresh or aged, garlic extracts contain compounds such as diallyl and allyl propyl disulfides with potent antioxidant, cholesterol-lowering properties; regular ingestion may be preventative for atherosclerosis and cardiovascular diseases.
  • Gastrin immunotoxin - An immunotoxin containing an epitope of human gastrin conjugated to diphtheria toxin, with antineoplastic activity. The gastrin epitope in this vaccine is chemically identical or similar to the endogenous gastrin-17 (G-17), a 17-amino acid peptide hormone that stimulates secretion of gastric acid by the stomach. Diphtheria toxin inhibits protein synthesis via modifying translation elongation factor 2 (EF-2). Vaccination with this immunotoxin may elicit production of antibodies against gastrinoma cells overexpressing gastrin, in addition to the toxic effects on protein synthesis exerted by the diphtheria toxin moiety.
  • Gastrin/cholecystokinin type b receptor inhibitor z-360 - A selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells.
  • Gataparsen sodium - A second-generation antisense oligonucleotide against survivin mRNA with potential antitumor activity. Gataparsen hybridizes to survivin mRNA, thereby blocking translation of survivin protein, a member of the inhibitor of apoptosis (IAP) family. Survivin, expressed during embryonal development, is upregulated in a variety of human cancers while absent in most normal adult cells; its expression in tumors is associated with a more aggressive phenotype, shorter survival times, and a decreased response to chemotherapy. Silencing expression of survivin potentially leads to restoration of the apoptotic process in cancer cells, thereby facilitating chemotherapeutic treatments.
  • Gatipotuzumab - A humanized monoclonal antibody recognizing the tumor-specific epitope of mucin-1 (TA-MUC1), with potential antineoplastic activity. Gatipotuzumab targets and binds to the TA-MUC1 epitopes expressed on the cell surface of tumor cells, thereby potentially activating the immune system to induce an antibody-dependent cellular cytotoxicity (ADCC) against the TA-MUC1-expressing tumor cells. TA-MUC1 is designated to MUC1 epitopes with O-glycosylated carbohydrate-induced conformational structures that are tumor-specific, thereby enabling gatipotuzumab to differentiate between tumor MUC1 and non-tumor MUC1 epitopes.
  • Gbm antigens and alloantigens immunotherapeutic vaccine - An orally bioavailable, immunotherapeutic vaccine composed of hydrolyzed and formulated glioblastoma multiforme (GBM) antigens and alloantigens derived from a pool of patients' cancer cells in the blood and samples of tumor tissues, with potential immunomodulating and antineoplastic activities. Upon oral administration of the GBM antigens and alloantigens immunotherapeutic vaccine, the GBM antigens and alloantigens may stimulate the host immune system via antigen-presenting cells (APCs) lining the gut to mount an immune response against tumor cells expressing these antigens. This may lead to tumor cell death.
  • Gd2 lactone/gd3 lactone-klh conjugate bivalent vaccine - A cancer vaccine, containing epitopes of the gangliosides GD2 and GD3 conjugated with the immunostimulant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with GD2 lactone/GD3 lactone-KLH conjugate bivalent vaccine may elicit antibodies against tumor cells expressing either epitope, resulting in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC). Located primarily in the nervous system, gangliosides, such as GD2 and GD3, are cell membrane components involved in cellular recognition and cell-cell communication.
  • Gd2-car-expressing autologous t-lymphocytes - Genetically modified, autologous T-lymphocytes transduced with a retroviral vector encoding a 14g2a.zeta chimeric antigen receptor (CAR) directed against the disialoganglioside GD2, with potential immunomodulating and antineoplastic activities. Upon intravenous administration, the activated T-lymphocytes target the GD2 antigen on tumor cells and selectively kill those cells. The tumor-associated antigen GD2 is overexpressed on the surface of almost all tumors of neuroectodermal origin.
  • Gd2-klh vaccine - A cancer vaccine containing an epitope of glycosphingolipid GD2 conjugated with the immunostimulant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. The disialoganglioside GD2 is a tumor-associated antigen expressed on the surface of several cancers, including neuroblastoma medulloblastomas, astrocytomas, melanomas, small-cell lung cancer, osteosarcomas, and other soft tissue sarcomas. Vaccination with GD2-KLH vaccine may elicit antibody production against cells expressing GD2 ganglioside, thereby reducing tumor cell growth.
  • Gedatolisib - An agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Upon intravenous administration, gedatolisib inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K.
  • Gefitinib - An anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis.
  • Geldanamycin - A benzoquinone antineoplastic antibiotic isolated from the bacterium Streptomyces hygroscopicus. Geldanamycin binds to and inhibits the cytosolic chaperone functions of heat shock protein 90 (HSP90). HSP90 maintains the stability and functional shape of many oncogenic signaling proteins; the inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins that may be over-expressed or overactive in tumor cells.
  • Gelonin - A class I ribosome-inactivating protein (RIP) and toxin derived from the seeds of the plant Gelonium multiflorum. Gelonin (rGel) exerts N-glycosidase activity on the 28S ribosomal RNA (rRNA) unit of eukaryotic ribosomes by cleaving out adenine at the 4324 site, which depurinates rRNA, inactivates ribosomes, inhibits protein synthesis, and results in cell death. Used as the toxin moiety of certain immunotoxins and linked to antibodies specific for a tumor-associated antigen (TAA), gelonin can be targeted to and induce specific cytotoxicity in tumor cells expressing the TAA.
  • Gemcitabine - A broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA. This locks DNA polymerase thereby resulting in "masked termination" during DNA replication. On the other hand, dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis. The reduction in the intracellular concentration of dCTP potentiates the incorporation of dFdCTP into DNA.
  • Gemcitabine elaidate - A lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. Due to its lipophilicity, gemcitabine 5'-elaidic acid ester exhibits an increased cellular uptake and accumulation, resulting in an increased conversion to active metabolites, compared to gemcitabine. In addition, this formulation of gemcitabine may be less susceptible to deamination and deactivation by deoxycytidine deaminase.
  • Gemcitabine hydrochloride - The hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
  • Gemcitabine hydrochloride emulsion - An orally available nanoparticle-based formulation containing the hydrochloride salt form of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue, with antineoplastic activity. The formulation consists of an oil-in-water emulsion in which gemicitabine is solubilized in the excipient matrix containing a mixture of oil and (co)surfactants. Upon oral administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA, resulting in premature termination of DNA replication and the induction of apoptosis. Further, dFdCDP inhibits ribonucleotide reductase and reduces the deoxynucleotide pool available for DNA synthesis. Compared to gemcitabine alone, the emulsion allows for increased oral bioavailability and decreases its susceptibility to deamination and deactivation by cytidine deaminase.
  • Gemcitabine prodrug ly2334737 - An orally available valproic acid prodrug of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon administration, gemcitabine prodrug LY2334737 is hydrolyzed by carboxylesterase 2 (CES2) and releases gemcitabine systemically over a period of time consistent with formation rate-limited kinetics. In turn, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate and triphosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP is incorporated into DNA, resulting in premature termination of DNA replication and eventually the induction of apoptosis. Compared to gemcitabine, this prodrug is able to avoid hydrolysis in enterocytes and the portal circulation thus avoiding first pass metabolism and increasing systemic gemcitabine availability. In addition, the slow release of gemcitabine may enhance efficacy while lowering toxicity. CES2, a serine ester hydrolase, is expressed in certain tumors which may allow for increased conversion of gemcitabine at the tumor site thus increases cytotoxicity.
  • Gemcitabine-releasing intravesical system - A controlled-release intravesical system consisting of a small flexible tube-like device with a solid core composed of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue, with antineoplastic activity. Upon placement of the gemcitabine-releasing intravesical system (GemRIS) into the bladder, gemcitabine is gradually and continuously released from the system over an extended period of time before being removed from the bladder. Upon release, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA, resulting in premature termination of DNA replication and the induction of apoptosis of bladder tumor cells. In addition, dFdCDP inhibits ribonucleotide reductase (RNR) and reduces the deoxynucleotide pool available for DNA synthesis.
  • Gemtuzumab ozogamicin - A recombinant, humanized anti-CD33 monoclonal antibody attached to the cytotoxic antitumor antibiotic calicheamicin. In this conjugate, the antibody binds to and is internalized by tumor cells expressing CD33 antigen (a sialic acid-dependent glycoprotein commonly found on the surface of leukemic blasts), thereby delivering the attached calicheamicin to CD33-expressing tumor cells. Calicheamicin binds to the minor groove of DNA, causing double strand DNA breaks and resulting in inhibition of DNA synthesis.
  • Gene-edited autologous neoantigen-targeted neotcr-p1 t-cells - A preparation of autologous CD4- and CD8-positive T-lymphocytes that have been engineered with site-specific nucleases to suppress the expression of most endogenous forms of the T-cell receptor (TCR) and promote expression of a single, native TCR targeting a neoepitope that is presented on the surface of a patient's tumor cells, with potential immunostimulating and antineoplastic activities. Upon reintroduction into the patient, the gene-edited autologous neoantigen-targeted NeoTCR-P1 T-cells recognize and bind to tumor cells expressing the targeted neoantigen, resulting in a cytotoxic T-lymphocyte (CTL)-mediated immune response against the patient's tumor cells.
  • Genetically engineered ny-eso-1-specific t lymphocytes - A preparation of human T-lymphocytes recognizing the tumor-associated antigen (TAA), cancer/testis antigen 1 (NY-ESO-1), with potential immunostimulating and antineoplastic activities. Genetically engineered NY-ESO-1-specific T-lymphocytes target tumor cells expressing the NY-ESO-1 antigen, resulting in tumor cell lysis. NY-ESO-1, an antigen found in normal testis, is overexpressed on the surface of various tumor cell types.
  • Genetically modified interleukin-12 transgene-encoding bifidobacterium longum - A live, genetically modified probiotic bacteria Bifidobacterium longum (B. longum) engineered to deliver genetic material encoding the human pro-inflammatory transgene interleukin-12 (IL-12), with potential immunoactivating activity. Upon administration of genetically modified IL-12 transgene-encoding B. longum, the bacteria selectively colonize hypoxic tumor tissues and deliver plasmid DNA encoding the IL-12 transgene within the tumor microenvironment (TME). 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.
  • Genetically-modified anti-her2-car-cd28zeta-expressing allogeneic nk-92/5.28.z cells - A preparation of genetically-modified natural killer (NK) cells derived from the allogeneic NK-92 cell line that are transduced with a lentiviral vector expressing a codon-optimized chimeric antigen receptor (CAR) consisting of a single chain variable fragment (scFv) of the anti-human epidermal growth factor 2 (HER2; ErbB2) monoclonal antibody FRP5, and fused, via hinge and transmembrane regions, to the intracellular domain of the costimulatory molecule CD28, and the intracellular signaling domain of the T-cell antigen receptor complex zeta chain (CD3-zeta), with potential cytolytic, immunomodulating and antineoplastic activities. Upon infusion of the genetically modified anti-HER2-CAR-CD28zeta-expressing allogeneic NK-92/5.28.z cells, the NK cells recognize and bind to HER2 expressed on tumor cells. This leads to the secretion and release of perforins, granzymes, cytokines and chemokines, which results in selective tumor cell lysis in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase (RTK) mutated or overexpressed in many tumor cell types, plays a significant role in tumor cell proliferation and tumor vascularization. The NK-92 cells are derived from a human cytotoxic cell line composed of allogeneic, activated, interleukin-2-(IL-2) dependent-NK cells from a 50-year old male patient with rapidly progressive non-Hodgkin's lymphoma. As NK-92 cells are devoid of killer inhibitory receptors (KIRs; also called killer cell immunoglobulin-like receptors), which are negative regulators of NK cell activity, cancer cells are unable to suppress the cancer cell killing ability of the NK-92 cells.
  • Genetically-modified mage-a3-expressing mg1 maraba virus vaccine - A vaccine consisting of the attenuated, genetically-modified, oncolytic form of the Maraba virus, MG1, which has been engineered to express a gene encoding the cancer testis antigen melanoma antigen family A3 (MAGE-A3), with potential antineoplastic activity. Upon administration of genetically-modified MAGE-A3-expressing MG1 Maraba virus vaccine, the attenuated Maraba virus selectively and rapidly replicates in cancer cells; however, it is unable to replicate in normal, healthy cells. This induces a selective Maraba virus-mediated cytotoxicity in those cancer cells, and leads to cancer cell lysis. In addition, the expression of MAGE-A3 further stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing MAGE-A3. The tumor-associated antigen MAGE-A3 is overexpressed by a variety of cancer cell types. The attenuated virus is a double mutant strain with single amino acid substitutions occurring in both G protein (Q242R) and M protein (L123W).
  • Genistein - A soy-derived isoflavone and phytoestrogen with antineoplastic activity. Genistein binds to and inhibits protein-tyrosine kinase, thereby disrupting signal transduction and inducing cell differentiation. This agent also inhibits topoisomerase-II, leading to DNA fragmentation and apoptosis, and induces G2/M cell cycle arrest. Genistein exhibits antioxidant, antiangiogenic, and immunosuppressive activities.
  • Gentuximab - A recombinant, humanized monoclonal antibody directed against the vascular endothelial growth factor receptor 2 (VEGFR-2), with potential anti-angiogenic and antineoplastic activities. Upon intravenous injection, gentuximab specifically binds to VEGFR-2, preventing the binding of its ligand, vascular endothelial growth factor (VEGF). Inhibition of VEGFR-2 signaling may potentially inhibit tumor angiogenesis and decrease nutrient supply to tumor cells, resulting in tumor cell death. VEGFR-2 is a type V receptor tyrosine kinase (RTK) expressed on endothelial cells and some tumor cells that regulates endothelial migration and proliferation.
  • Geranylgeranyltransferase i inhibitor - A substance that inhibits protein geranylgeranyltransferase type 1 (GGTase-I), with potential antineoplastic activity. GGTase-I is involved in the posttranslational modification of a number of oncogenic GTPases, including K-Ras, N-Ras, RhoA, RhoC, Cdc42, RalA, RalB and Rac1. Inhibition of the prenylation of these oncogenic proteins inhibits both their oncogenic activity and membrane localization. This may result in cell cycle arrest and apoptosis. Protein geranylgeranylation, catayzed by GGTase-I, plays a critical role in malignant transformation and cancer cell proliferation, migration and invasion.
  • Gi-4000 vaccine - A vaccine containing a heat-killed recombinant Saccharomyces cerevisiae yeast transfected with mutated forms of Ras, an oncogene frequently found in solid tumors, with potential immunostimulant and antitumor activity. Upon administration, GI-4000 vaccine elicits an immune response by stimulating a specific cytotoxic T-cell response against the mutated forms of Ras. This may lead to a destruction of cancer cells expressing a Ras mutation.
  • Giloralimab - An agonistic monoclonal antibody directed against the B-cell surface antigen CD40, with potential antineoplastic activity. Upon administration, giloralimab binds to CD40 on a variety of immune cell types. This induces CD40-dependent signaling pathways, triggers the proliferation and activation of antigen-presenting cells (APCs), and activates T-cells. This results in an enhanced cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. CD40, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on various immune cells and plays a key role in the activation of the immune system.
  • Gilteritinib - An orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-related tyrosine kinase 3 (FLT3, STK1, or FLK2), AXL (UFO or JTK11) and anaplastic lymphoma kinase (ALK or CD246), with potential antineoplastic activity. Gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL and ALK. This may result in an inhibition of FLT3, AXL, and ALK-mediated signal transduction pathways and reduces tumor cell proliferation in cancer cell types that overexpress these RTKs. FLT3, AXL and ALK, overexpressed or mutated in a variety of cancer cell types, play a key role in tumor cell growth and survival.
  • Gilteritinib fumarate - The fumarate salt form of gilteritinib, an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-like tyrosine kinase 3 (FLT3; STK1; FLK2), AXL (UFO; JTK11), anaplastic lymphoma kinase (ALK; CD246), and leukocyte receptor tyrosine kinase (LTK), with potential antineoplastic activity. Upon administration, gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL, ALK and LTK. This may result in an inhibition of FLT3-, AXL-, ALK-, and LTK-mediated signal transduction pathways and reduced proliferation in cancer cells that overexpress these RTKs. FLT3, AXL, ALK, and LTK, which are overexpressed or mutated in a variety of cancer cell types, play key roles in tumor cell growth and survival.
  • Gimatecan - An orally bioavailable, semi-synthetic lipophilic analogue of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic and antiangiogenic activities. Gimatecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Although the mechanism of its antiangiogenic activity has yet to be full elucidated, this agent may inhibit endothelial cell migration, tumor neovascularization, and the expression of proangiogenic basic fibroblast growth factor (bFGF).
  • Gimeracil - A pyridine derivative with antitumor activity. Gimeracil enhances the antitumor activity of fluoropyrimidines by competitively and reversibly inhibiting the enzyme dihydropyrimidine dehydrogenase causing decreased degradation of the fluoropyrimidines.
  • Ginger extract - An extract of the rhizome of the perennial plant Zingiber officinale with potential antineoplastic activity. Ginger extract contains a number of different phenolic compounds, some of which have displayed antineoplastic, anti-inflammatory, and antioxidant activities. This agent also exhibits antiemetic properties.
  • Ginseng compound - A compound containing the traditional Chinese medicine (TCM) ginseng, a herb belonging to the Araliaceae family, with potential antioxidant, chemopreventive, anti-inflammatory and antineoplastic activities. Upon administration of the ginseng compound, the active ingredients, mainly ginsenosides, inhibit various signal transduction pathways that play key roles in carcinogenesis and inflammation. This leads to the induction of apoptosis in and inhibits proliferation of tumor cells. In addition, ginsenosides enhance the activity of various antioxidant enzymes, induce nitric oxide (NO) formation, inhibit the formation of reactive oxygen species (ROS) and protect against free radical-induced DNA damage. Ginseng also modulates various components of the immune system, including the activation of dendritic cells (DCs).
  • Ginseng/lingzhi mushroom/cordyceps sinensis/rose oral liquid - An orally available supplement containing ginseng, lingzhi mushroom, Cordyceps sinensis, and rose with potential immunostimulating activities. Upon oral administration, ginseng/lingzhi mushroom/Cordyceps sinensis/rose oral liquid may, through a not yet elucidated mechanism, enhance immune responses and relieve fatigue.
  • Ginsenoside rg3 capsule - A capsule containing the steroidal saponin ginsenoside Rg3 isolated from the root of Panax ginseng, with potential cancer preventive and anti-angiogenic activities. Upon oral administration, ginsenoside Rg3 appears to inhibit endothelial cell proliferation, migration and tubular formation, and promotes cancer cell apoptosis. This agent also modulates the activities of certain growth factors, such as vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), and matrix metalloproteinases (MMPs), on tumor angiogenesis. In addition, ginsenoside Rg3 may be able to sensitize cancer cells to some chemotherapeutic agents.
  • Giredestrant - An orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, giredestrant specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells.
  • Girentuximab - A chimeric monoclonal antibody directed against G250, a cell surface antigen found in the majority of renal cell carcinomas. Following binding, monoclonal antibody G250 (mAb G250) may be internalized by G250 antigen-expressing renal carcinoma cells; mAb G250 may be useful as a carrier for radioisotopes and other antineoplastic therapeutic agents. (NCI05)
  • Girodazole - A compound isolated from the marine sponge Pseudaxinyssa cantharella exhibiting anti-tumor activity. Studies indicate girodazole acts during the elongation/termination steps of protein synthesis, resulting in protein synthesis inhibition. (NCI)
  • Gitr agonist medi1873 - An agonist of human glucocorticoid-induced tumor necrosis factor receptor (tumor necrosis factor superfamily, member 18; TNFRSF18; GITR), with potential immunomodulating and antineoplastic activities. Upon administration, GITR agonist MEDI1873 binds to GITR found on multiple types of T-cells, thereby inducing both the activation and proliferation of tumor antigen-specific T effector cells. This abrogates the suppression of T effector cells which is induced by inappropriately activated T regulatory cells (Tregs), and activates the immune system to help eradicate tumor cells. GITR, a member of the TNF receptor superfamily, is expressed on the surface of multiple types of immune cells, including regulatory T-cells, effector T-cells, B-cells, dendritic cells (DCs) and natural killer (NK) cells.
  • Gitrl rna-transfected autologous dendritic cell vaccine - An autologous dendritic cell (DC) cancer vaccine with potential immunostimulatory activity. GITRL RNA-transfected autologous DC vaccine is prepared by transfecting DCs with RNAs encoding tumor necrosis factor (ligand) superfamily, member 18 (TNFSF18 or GlTRL); expression of GlTRL results in modulating T lymphocyte survival in peripheral tissues. Co-vaccination of this vaccine with melanoma antigen specific vaccine may eliminate the adverse effects associated with systemic administration of immune modulators, while also enhancing vaccine-induced immune responses.
  • Givinostat - An orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Givinostat inhibits class I and class II HDACs, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. Givinostat has also been shown to activate the intrinsic apoptotic pathway, inducing apoptosis in hepatoma cells and leukemic cells. This agent may also exhibit anti-angiogenic activity, inhibiting the production of angiogenic factors such as IL-6 and vascular endothelial cell growth factor (VEGF) by bone marrow stromal cells.
  • Glasdegib - An orally bioavailable small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. Glasdegib appears to inhibit Hh pathway signaling. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies.
  • Glasdegib maleate - The maleate salt form of glasdegib, an orally bioavailable small-molecule, smoothened (SMO) receptor inhibitor, with potential antineoplastic activity. Upon oral administration, glasdegib targets, binds to and inhibits the activity of SMO. This inhibits the activity of the Hedgehog (Hh) signaling pathway and inhibits the growth of tumor cells in which this pathway is aberrantly activated. SMO, a transmembrane protein, is involved in Hh signal transduction. The Hh signaling pathway plays an important role in cellular growth, differentiation, repair, and cancer stem cell (CSC) survival. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies and is associated with uncontrolled cellular proliferation in a variety of cancers.
  • Glaucarubolone - A polycyclic lactone quassinoid phytochemical isolated from the seeds of Hannoa undulata and other plant species with potential antineoplastic activity. This agent also has antiviral and antitumor properties.
  • Glembatumumab vedotin - An antibody-drug conjugate, consisting of the fully human monoclonal antibody CR011 directed against glycoprotein NMB (GPNMB) and conjugated via a cathepsin B-sensitive valine-citrulline (vc) linkage to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the monoclonal antibody CR011 moiety binds to glycoprotein nmb (GPNMB), expressed on the surfaces of a variety of cancer cell types; upon endocytosis, the synthetic dolastin analogue MMAE is released via enzymatic cleavage into the tumor cell cytosol, where it binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and apoptosis. The vc linkage system is highly stable in serum, rendering the cytotoxicity of glembatumumab vedotin specific for GPNMB-positive cells. GPNMB is a transmembrane protein overexpressed on the surfaces of various cancer cell types, including melanoma, breast, and prostate cancer cells.
  • Glesatinib - An orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. Glesatinib binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON). Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs.
  • Glioblastoma cancer vaccine erc1671 - A cancer vaccine composed of a combination of autologous glioblastoma (GBM) tumor cells, allogeneic GBM tumor cells, generated from three different GBM donor cancer patients, and the lysates of all of these cells, with potential antineoplastic activity. Upon intradermal administration of GBM cancer vaccine ERC1671, the mixture of the autologous and allogeneic cells and lysates stimulates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GBM-associated antigens, which leads to the destruction of glioblastoma cells.
  • Glioblastoma multiforme multipeptide vaccine ima950 - A cancer vaccine comprised of 11 peptides associated with glioblastoma multiforme (GBM), with potential immunomodulating and antineoplastic activities. Vaccination with glioblastoma multiforme multi-antigen vaccine IMA950 stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response as well as a T-helper (Th) immune response against tumor cells expressing these peptides, potentially resulting in decreased tumor growth of GBM. Peptides in IMA950 consist of the following: brevican (BCAN); chondroitin sulfate proteoglycan 4 (CSPG4); fatty acid binding protein 7, brain (FABP7); insulin-like growth factor 2 mRNA binding protein 3 (IGF2BP3); neuroligin 4, X-linked (NLGN4X); neuronal cell adhesion molecule (NRCAM); protein tyrosine phosphatase, receptor-type, Z polypeptide 1 (PTPRZ1); tenascin C (TNC); Met proto-oncogene (MET); baculoviral IAP repeat-containing 5 (BIRC5); and hepatitis B virus core antigen.
  • Glioma lysate vaccine gbm6-ad - An allogeneic cell lysate-based vaccine derived from the glioma stem cell line GBM6-AD, which was isolated from the brain tumor of a patient diagnosed with glioblastoma multiforme (GBM), with potential immunostimulatory and antineoplastic activities. Upon subcutaneous administration, the glioma lysate vaccine GBM6-AD exposes the immune system to an undefined amount of glioma-associated antigens (GAAs), and stimulates the immune system to mount a specific anti-tumoral, cytotoxic T-lymphocyte (CTL)-mediated response against the GAA-expressing cells, resulting in glioma cell lysis.
  • Glioma-associated antigen peptide-pulsed autologous dendritic cell vaccine - A cancer vaccine comprised of autologous dendritic cells pulsed with synthetic glioma-associated antigen (GAA) peptides with potential antineoplastic activity. Upon administration, this vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against GAA peptide-expressing glioma cells, resulting in tumor cell lysis.
  • Glioma-associated peptide-loaded dendritic cell vaccine sl-701 - A cell-based cancer vaccine comprised of dendritic cells (DCs) pulsed with various, synthetic glioma-associated antigen (GAA) peptides, with potential antineoplastic activity. Upon subcutaneous administration, the glioma-associated peptide-loaded DC vaccine SL-701 exposes the immune system to various GAA peptides. This may stimulate both anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against the GAA-expressing glioma cells, which may result in tumor cell lysis.
  • Globo h-dt vaccine obi-833 - A carbohydrate-based vaccine comprised of the Globo H hexasaccharide 1 (Globo H) antigen conjugated to DT-CRM197, a non-toxic, mutated form of diphtheria toxin (DT), with potential immunostimulating and antineoplastic activities. Upon administration of Globo H-DT vaccine OBI-833, the carbohydrate antigen Globo H may stimulate a cytotoxic T-lymphocyte (CTL) response against Globo H-expressing tumor cells, thereby decreasing tumor cell proliferation. The hexasaccharide Globo H is a tumor-associated antigen (TAA) commonly found on a variety of tumor cells. DT-CRM197, also called diphtheria toxin cross-reacting material 197, is used to increase the immunogenicity of the Globo H carbohydrate antigen.
  • Globo h-gm2-lewis-y-muc1-32-mer-tf(c)-tn(c)-klh conjugate vaccine - A multivalent vaccine comprised of the epitope antigens of Globo H hexasaccharide 1 (Globo H), GM2 ganglioside, Lewis-Y, MUC1-32-mer, TF(c), and Tn(c) conjugated with keyhole limpet hemocyanin, with potential antineoplastic activity. The antigens included in this vaccine are associated various cancer cells. Vaccination with this multivalent vaccine may induce production of IgG and IgM antibodies as well as an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumors expressing these antigens.
  • Globo-h-gm2-lewis-y-muc1-32(aa)-stn(c)-tf(c)-tn(c)-klh conjugate vaccine - A heptavalent vaccine consisting of the tumor-associated carbohydrate antigens globohexaosylceramide (globo-H), GM2, Lewis-y, MUC1-32(aa), sTn(c), TF(c), and Tn(c) conjugated with keyhole limpet hemocyanin (KLH), an immunomodulator. This vaccine may induce the production of IgG and IgM antibodies and an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumors expressing these antigens.
  • Glucarpidase - A zinc-dependent enzyme isolated from a strain of the bacterium Pseudomonas. Because glucarpidase rapidly hydrolyzes methotrexate into inactive metabolites, it may be useful as a rescue agent for methotrexate-induced nephrotoxicity. In antibody-directed enzyme prodrug therapy (ADEPT), this agent is conjugated with an antibody that binds to a specific tumor cell type, allowing for glucarpidase-catalyzed activation of a co-administered prodrug at the site of the tumor.
  • Glucocorticoid receptor antagonist oric-101 - A mifepristone-based steroidal glucocorticoid receptor (GR) antagonist with potential antineoplastic activity. Upon oral administration, ORIC-101 selectively binds to GRs, thereby inhibiting the activation of GR-mediated proliferative and anti-apoptotic gene expression pathways. The GR, a member of the nuclear receptor superfamily of ligand-dependent transcription factors, is overexpressed in certain tumor types and may be associated with tumor cell proliferation and treatment resistance. Inhibition of GR activity may potentially slow tumor cell growth and disease progression in certain cancers. Due to its reduced androgen receptor (AR) agonistic activity and improved cytochrome P450 2C8 (CYP2C8) and 2C9 (CYP2C9) inhibition profile, ORIC-101 may be useful in the treatment of AR-positive tumors with reduced potential for drug-drug interactions.
  • Glufosfamide - A compound consisting of the mustard agent ifosforamide conjugated to glucose, with potential alkylating activity. Glufosfamide is cleaved by glucosidases in tumor cells and forms ifosforamide. In turn, ifosforamide alkylates and forms DNA crosslinks, thereby inhibiting DNA replication and subsequent cell growth. The glucose moiety may enhance this agent's uptake by tumor cells.
  • Glumetinib - An orally bioavailable, small molecule inhibitor of the oncoprotein c-Met (hepatocyte growth factor receptor; HGFR), with potential antineoplastic activity. Upon oral administration, glumetinib targets and binds to the c-Met protein, thereby disrupting c-Met-dependent signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.
  • Glutaminase inhibitor ipn60090 - An orally bioavailable inhibitor of glutaminase, with potential antineoplastic and immunostimulating activities. Upon oral administration, IPN60090 selectively targets, binds to and inhibits human glutaminase, an enzyme that is essential for the conversion of the amino acid glutamine into glutamate. Blocking glutamine metabolism inhibits proliferation in rapidly growing tumor cells and leads to an induction of cell death. Unlike normal healthy cells, glutamine-dependent tumors heavily rely on the intracellular conversion of exogenous glutamine into glutamate and glutamate metabolites to provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival.
  • Glutamine antagonist drp-104 - A broad acting glutamine antagonist, with potential immunomodulatory and antineoplastic activities. Upon administration, DON (6-Diazo-5-oxo-L-norleucine), the active moiety of DRP-104, irreversibly inhibits multiple enzymes involved in glutamine metabolism. Blocking glutamine metabolism inhibits proliferation in rapidly growing tumor cells and leads to an induction of cell death. Unlike normal healthy cells, glutamine-dependent tumors rely heavily on the intracellular conversion of exogenous glutamine into glutamate and glutamate metabolites to both provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival. In addition, blocking glutamine metabolism leads to the accumulation of glutamine in tumor cells and increases glutamine concentration in the tumor microenvironment (TME) upon tumor cell death. As glutamine is essential for T-cell generation, DON may also enhance T-cell proliferation and activation in the TME, which may lead to further killing of tumor cells. The conversion of DRP-104 to the active moiety DON occurs primarily in tumor cells, allowing glutamine metabolism in healthy cells which may lessen adverse effects.
  • Glutathione pegylated liposomal doxorubicin hydrochloride formulation 2b3-101 - A glutathione (GSH) pegylated, liposome-encapsulated preparation of the hydrochloride salt form of the anthracycline antineoplastic antibiotic doxorubicin, with potential anetineoplastic activity. Upon administration, the glutathione pegylated liposomal formulation 2B3-101 specifically delivers doxorubicin into the brain. Doxorubicin intercalates between DNA base pairs and interferes with topoisomerase II activity, which inhibits both DNA replication and RNA synthesis, resulting in cancer cell death and tumor regression. Doxorubicin also generates reactive oxygen species, which causes cell membrane lipid peroxidation leading to cytotoxicity. The pegylated liposomal delivery of doxorubicin improves drug penetration into tumors and prolongs circulation time, thereby increasing doxorubicin's efficacy and decreasing its toxicity. Conjugation of GSH to the PEG molecules directs the liposomes to the GSH transporters on the blood brain barrier (BBB) and improves the delivery of doxorubicin into the brain.
  • Glyco-engineered anti-cd20 monoclonal antibody cho h01 - A glyco-engineered monoclonal antibody directed against the human B-cell-specific cell surface antigen CD20, with potential antineoplastic and immunomodulating activities. Upon administration of glyco-engineered anti-CD20 monoclonal antibody CHO H01, the antibody specifically targets and binds to CD20. This induces antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B-cells, which leads to B-cell apoptosis and the inhibition of tumor cell proliferation. In addition, CHO H01 inhibits CD20-mediated signaling which further induces apoptosis in and inhibits proliferation of CD20-expressing tumor cells. CD20, a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B-cells during most stages of B-cell development, is often overexpressed in B-cell malignancies. The Fc-glycans are homogenously engineered onto the antibody and increase ADCC, anti-tumor activity and the half-life of the antibody.
  • Glycooptimized trastuzumab-gex - A glycoengineered form of a monoclonal antibody directed against the human epidermal growth factor receptor-2 (HER2), with potential antineoplastic activity. Glycooptimized trastuzumab-GEX specifically binds to the extracellular domain of HER2, thereby inducing an antibody-dependent cell-mediated cytotoxicity (ADCC) against HER2-expressing tumor cells. This eventually results in apoptosis and growth inhibition of tumor cells. HER2, a member of the receptor tyrosine kinase EGFR superfamily, is overexpressed on the cell surfaces of various solid tumors. This agent has a specific glycosylation profile that may enhance its ADCC response against HER2-expressing tumor cells.
  • Gm.cd40l cell vaccine - A cell-based vaccine composed of irradiated tumor cells transduced with granulocyte-macrophage colony-stimulating factor (GM-CSF) and CD40-ligand (CD40L) genes. Upon administration, this vaccine may stimulate an anti-tumoral dendritic cell-mediated host immune response. (NCI05)
  • Gm2/gd2/gd3 lactone-klh conjugate trivalent vaccine - A trivalent cancer vaccine containing the ganglioside lactones GM2, GD2 and GD3 conjugated with the immunostimulant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with GM2 lactone/GD2 lactone/GD3 lactone-KLH conjugate trivalent vaccine may elicit antibodies against tumor cells expressing any of these epitopes, resulting in an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing these gangliosides. GM2, GD2 and GD3 are tumor associated antigens (TAAs) that are overexpressed in a variety of tumor cell membranes.
  • Gm2-klh vaccine - A cancer vaccine consisting of GM2 ganglioside, a melanoma-specific antigen, conjugated with the immunostimulant keyhole limpet hemocyanin. Vaccination with GM2-KLH vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against GM2 ganglioside-expressing melanoma cells, resulting in tumor growth inhibition.
  • Gm2-klh vaccine/qs21 - A cancer vaccine based on the immunogenic ganglioside GM2, The GM2-KLH Vaccine/QS21 vaccine consists of GM2 conjugated with KLH keyhole limpet hemocyanin (KLH), a potent immunostimulant, and is admixed with the adjuvant QS21, a saponin fraction extracted from the bark of the South American tree Quillaja saponaria Molina. GM2 is a cell surface carbohydrate antigen expressed by most melanoma cells and various other tumor cell types.
  • Gm-csf dna - DNA that encodes granulocyte-macrophage colony stimulating factor (GM-CSF). GM-CSF enhances the host immune response to poorly immunogenic tumors, possibly by activating T-cell and macrophage anti-tumor responses, and, so, decreasing tumor growth.
  • Gm-csf-encoding oncolytic adenovirus cgtg-102 - A recombinant, oncolytic serotype 5/3 capsid-modified adenovirus encoding the immunostimulatory cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF) with potential antineoplastic activity. Upon administration, the oncolytic adenovirus selectively infects and replicates in tumor cells, which may result in tumor cell lysis. Synergistically, GM-CSF (sargramostim) expressed by the oncolytic adenovirus enhances antigen presentation, promotes natural killer (NK) cell-mediated killing and causes a cytotoxic T cell (CTL) response against tumor cells harboring the oncolytic adenovirus, resulting in an immune-mediated tumor cell death. CGTG-102 is designed to replicate only in cells with defects in the p16/Rb/E2F pathway, attributed to a mutation common in many solid tumors. Replacement of the Ad5 capsid protein knob with a knob domain from serotype 3 causes higher transduction in cancer cells as compared to normal cells.
  • Gm-k562 cell vaccine - A cell-based vaccine comprised of K562 cells transfected with the granulocyte macrophage-colony stimulating factor (GM-CSF) gene with potential immunopotentiating properties. Vaccination with GM-K562 cells may stimulate the host immune system to produce an antitumoral T-lymphocyte response, thereby inhibiting tumor growth. K562 cells are derived from the human erythroleukemia cell line K562. GM-CSF (also known as sagramostim) expressed by vaccine cells binds to specific cell surface receptors, modulating the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production. GM-CSF also promotes antigen presentation, up-regulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function; it may also augment host antitumoral immunity.
  • Gold sodium thiomalate - The sodium salt of gold thiomalic acid, an organogold compound with antirheumatic and potential antineoplastic activities. Gold sodium thiomalate (GST) appears to inhibit the activity of atypical protein kinase C iota (PKCiota) by forming a cysteinyl-aurothiomalate adduct with the cysteine residue Cys-69 within the PB1 binding domain of PKCiota. This prevents the binding of Par6 (Partitioning defective protein 6) to PKCiota, thereby inhibiting PKCiota-mediated oncogenic signaling, which may result in the inhibition of tumor cell proliferation, the promotion of tumor cell differentiation, and the induction of tumor cell apoptosis. Atypical PKCiota, a serine/threonine kinase overexpressed in numerous cancer cell types, plays an important role in cancer proliferation, invasion, and survival; Par6 is a scaffold protein that facilitates atypical PKC-mediated phosphorylation of cytoplasmic proteins involved in epithelial and neuronal cell polarization.
  • Golnerminogene pradenovec - A recombinant agent consisting of a genetically-modified adenovirus 5 vector encoding the protein cytokine tumor necrosis factor (TNF) alpha. TNF exhibits potent anti-tumor cytolytic properties; the adenovirus 5 vector efficiently infects tumor cells, delivering tumor-specific TNF.
  • Golotimod - An orally bioavailable synthetic peptide containing the amino acids D-glutamine and L-tryptophan connected by a gamma-glutamyl linkage with potential immunostimulating, antimicrobial and antineoplastic activities. Although the exact mechanism of action is unknown, golotimod appears to inhibit the expression of STAT-3, reversing immunosuppression and stimulating an anti-tumor immune response. This agent may stimulate the production of T-lymphocytes, in particular the helper T (Th1) cells, activate macrophages, and increase levels of interleukin 2 and interferon gamma. STAT-3, a transcription factor upregulated in many cancer cell types, is involved in tumor cell growth and survival and immunosuppression.
  • Golvatinib - An orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of tumor cell types and play important roles in tumor cell growth, migration and angiogenesis.
  • Gonadotropin-releasing hormone analog - A synthetic analogue of the endogenous hormone gonadotropin-releasing hormone (GnRH), with potential antineoplastic activity. Upon administration, GnRH analogue mimics endogenous GnRH and strongly binds to and activates pituitary GnRH receptors, which stimulates the synthesis and secretion of the gonadotropic hormones, follicle stimulating hormone (FSH) and luteinizing hormone (LH). Continuous, prolonged activation by the GnRH analogue results in pituitary GnRH receptor desensitization and receptor downregulation. This causes inhibition of pituitary gonadotropin secretion of LH and FSH. In males, the inhibition of LH secretion prevents the production and release of testosterone from Leydig cells in the testes and causes a significant decline in testosterone production that is near the levels seen after castration. This may inhibit androgen receptor-positive tumor progression. In females, this results in a decrease in estradiol production. GnRH, also called luteinizing hormone-releasing hormone (LH-RH), is normally synthesized in and secreted by the hypothalamus. Synthetic analogues of GnRH have a stronger receptor binding affinity than the endogenous form.
  • Gorilla-derived adenovirus-expressing hpv-16/18 e6/e7 vaccine - An off-the-shelf (OTS) cancer vaccine comprised of a genetically engineered, replication-deficient gorilla-derived adenovirus encoding human papillomavirus (HPV) types 16 and 18 E6/E7 antigens, with potential immunostimulating and antineoplastic activities. Upon administration of gorilla-derived adenovirus expressing HPV-16/18 E6/E7 vaccine PRGN-2009, the adenovirus infects and expresses the HPV-16/18 E6/E7 proteins. The expressed proteins stimulate the host immune system to produce antigen-specific neutralizing antibodies and to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing HPV-16/18 E6/E7 antigens, thereby inducing tumor cell lysis. HPV oncoproteins play a key role in the development of cervical intraepithelial neoplasia (CIN) and cervical carcinoma.
  • Goserelin - A synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. Goserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of goserelin inhibits the secretion of pituitary gonadotropin, thereby decreasing levels of testosterone (in males) and estradiol (in females). Administration of this agent in a depot formulation may result in the regression of sex hormone-sensitive tumors and a reduction in sex organ size and function.
  • Goserelin acetate - The acetate salt of a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH). Continuous, prolonged administration of goserelin in males results in inhibition of pituitary gonadotropin secretion, leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
  • Goserelin acetate extended-release microspheres ly01005 - A long-acting, extended-release microsphere formulation of the acetate form of goserelin, a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH), with potential antineoplastic activity. Upon administration, goserelin binds to and activates pituitary gonadotropin-releasing hormone (GnRH) receptors. Prolonged administration of goserelin inhibits the secretion of pituitary gonadotropin, thereby decreasing levels of testosterone (in males) and estradiol (in females). Administration of this agent in an extended-release formulation may result in the regression of sex hormone-sensitive tumors and a reduction in sex organ size and function.
  • Gossypol - An orally-active polyphenolic aldehyde with potential antineoplastic activity. Derived primarily from unrefined cottonseed oil, gossypol induces cell cycle arrest at the G0/G1 phase, thereby inhibiting DNA replication and inducing apoptosis. This agent also inhibits cell-signaling enzymes, resulting in inhibition of cell growth, and may act as a male contraceptive.
  • Gossypol acetic acid - The naturally occurring acetic acid form of gossypol, and an orally available polyphenolic aldehyde derived mostly from cottonseed with potential antineoplastic activity. The biologic activities of gossypol acetic acid are similar to those of gossypol and include suppression of DNA replication, inhibition of tumor cell proliferation, and male contraceptive effects.
  • Gp100 adenovirus vaccine - A vaccine consisting of a replication-defective recombinant adenovirus that encodes the melanoma antigen glycoprotein 100 (gp100) with potential antineoplastic activity. Vaccination with gp100 adenovirus 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.
  • Gp100 antigen - A melanoma-associated antigen. When administered in a vaccine formulation, gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumors that express this antigen, which may result in a reduction in tumor size.
  • Gp100 human melanoma peptide vaccine with incomplete freund's adjuvant - A vaccine consisting of synthetic glycoprotein 100 (gp100) melanoma antigen and incomplete Freund's adjuvant (IFA), an emulsifying agent and immune system stimulant, with antineoplastic activity. Vaccination with gp100 human melanoma peptide vaccine with IFA may stimulate the host immune system to direct cytotoxic T lymphocytes (CTL) against gp100 positive melanoma cells, resulting in decreased tumor growth.
  • Gp100:154-162 peptide vaccine - A peptide consisting of amino acid residues 154 through 162 of the melanoma-melanocyte antigen gp100. Vaccination with gp100:154-162 peptide may enhance tumor-specific T-cell immunity. gp100 antigen is a self-antigen expressed by melanocytes, pigmented retinal cells, and most melanoma lesions and is recognized via class I and II HLA-restricted mechanisms.
  • Gp100:209-217(210m) peptide vaccine - A synthetic peptide cancer vaccine consisting of amino acid residues 209 through 217 of the glycoprotein 100 (gp100) melanoma antigen, with a methionine substitution at position 210 designed to improve immunogenicity. Vaccination with gp100:209-217(210M) peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing gp100.
  • Gp100:280-288 peptide vaccine - A vaccine consisting of the amino acids 280 through 288 of the melanoma antigen glycoprotein 100 (gp100) with potential antineoplastic activity. Vaccination with gp100:280-288 peptide 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.
  • Gp100:280-288(288v) peptide vaccine - A peptide vaccine consisting of the amino acids 280 through 288 of the melanoma antigen glycoprotein 100 (gp100) with potential antineoplastic activity. gp100:280-288(288V) peptide has a valine substitution at amino acid position 288 to improve immunogenicity. Vaccination with gp100:280-288(288V) peptide 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.
  • Gp100-fowlpox vaccine - A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the melanoma antigen glycoprotein 100 (gp 100) with potential antineoplastic activity. The expression of gp100 may generate a cellular immune response to melanoma cells; this effect is enhanced by the co-administration of interleukin 2 (IL-2).
  • Gp2 peptide/gm-csf vaccine - A vaccine containing a HER2/Neu-derived epitope (amino acids 654-662) (GP2), and combined with granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential antineoplastic and immunoadjuvant activity. Upon vaccination, GP2 may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against HER2/Neu expressing cancer cells. GM-CSF may potentiate a tumor-specific cytotoxic T-lymphocyte (CTL) response against cancer cells expressing the HER2/Neu antigen. HER2/neu, a tumor associated antigen (TAA), is overexpressed in a variety of tumor cell types and is highly immunogenic.
  • Gp209-2m antigen - A modified peptide antigen derived from gp209, with potential immunomodulatory and antineoplastic activities. gp209-2M antigen (IMDQVPFSV) has a methionine substitution of threonine at position 2 of gp209 peptide (ITDQVPFSV), which is the immunogenic epitope of human melanoma tumor glycoprotein gp100. Vaccination with this peptide may evoke a cytotoxic T lymphocyte (CTL) response against tumor cells expression of the gp100 antigen.
  • G-quadruplex stabilizer bmvc - A carbazole derivative (3,6-bis[2-(1-methylpyridinium)vinyl]carbazole diiodide) that selectively targets to the G-quadruplex DNA structure, used as a fluorescent probe for cancer cytological diagnosis and with potential antitumor activity. G-quadruplex stabilizer BMVC, preferentially uptaken by cancer cells, binds to and stabilize the telomeric G-quadruplex structure at the end of DNA; when visualized with fluorescent imaging device, BMVC emits bright fluorescent light and can be used to differentiate tumor cells from normal cells. The BMVC/G-quadruplex complexes also interfere with the activity of telomerase, which is highly active in tumor cells and plays a key role in tumorigenesis while expressed at very low levels in most somatic cells.
  • Grapiprant - An orally bioavailable antagonist of the prostaglandin E receptor subtype 4 (EP4), with potential analgesic, immunomodulating and antineoplastic activities. Upon administration of grapiprant, this agent selectively binds to and inhibits the binding of prostaglandin E2 (PGE2) and prevents the activation of the EP4 receptor. This inhibits PGE2-EP4 receptor-mediated signaling and prevents proliferation in tumor cells in which the PGE2-EP4 signaling pathway is over-activated. In addition, EP4 receptor inhibition modulates the immune system by preventing both interleukin-23 (IL-23) production and the IL-23-mediated expansion of Th17 cells. As EP4 is expressed by peripheral sensory neurons, blockade of EP4-mediated signaling may induce an analgesic effect. EP4, a prostanoid receptor subtype, is a G protein-coupled receptor that is expressed in certain types of cancers; it promotes tumor cell proliferation and invasion.
  • Green tea - Tea derived from the dried leaves of the plant Camellia sinensis with potential antioxidant, chemopreventive, and lipid-lowering activities. Green tea contains polyphenols that are believed to be responsible for its chemopreventive effect. The polyphenol fraction contains mainly Epigallocatechin-3-gallate (EGCG) and other catechins, such as epicatechin (EC), gallocatechin gallate (GCG), epigallocatechin (EGC), and epicatechin gallate (ECG). Green tea polyphenols act as antioxidants and free radical scavengers and may affect enzymes involved in cellular replication and tumor angiogenesis by modulating angiogenic factors, such as vascular endothelial growth factor (VEGF).
  • Green tea extract - A defined, decaffeinated green tea polyphenol mixture isolated from Camellia sinensis, a plant native to Asia, with antiviral and antioxidant activities and potential chemopreventive activity. Green tea extract contains antioxidant compounds, including flavonoids, vitamins and polyphenols such as epigallocatechin-3-gallate (EGCG), which may have antineoplastic properties. Consumption of green tea extract may confer chemopreventive protection against various cancers including those of the prostate, stomach, and esophagus.
  • Green tea extract-based antioxidant supplement - A dietary supplement containing a green tea extract including the catechin epigallocatechin gallate and other vitamins and antioxidants, with potential antineoplastic and chemopreventive activities. The polyphenols in green tea act as antioxidants and scavenge free radicals which may inhibit cellular oxidation and prevent free radical damage to cells. In addition, polyphenols may affect enzymes involved in cellular reproduction and tumor angiogenesis by modulating angiogenic factors. Other ingredients in green tea extract-based antioxidant supplement include dry cinnamon extract, germanium, zinc sulfate, manganese sulfate, arginine, cysteine, malic acid, ascorbic acid (vitamin c), glycyrrhizinic acid, glycine, glucosamine, pyridoxal (vitamin B6), calcium pantothenate (vitamin B5), folic acid, cyanocobalamin (vitamin B12).
  • Green tea/licorice extract-based antioxidant solution - A nutritional supplement containing a variety of antioxidants, vitamins, minerals and amino acids, including glycyrrhizic acid, epigallocatechin gallate (EGCG), zinc, vitamins B5, B6 and B12, vitamin C (ascorbic acid), folic acid, malic acid, glucosamine, arginine, and glycine, with potential immunomodulating, anti-inflammatory, protective, and antineoplastic activities. Upon oral administration, the antioxidants in the solution modulate certain enzymes involved in inflammation and oxidative stress and downregulate certain pro-inflammatory mediators. They also scavenge free radicals. This protects against inflammation- and reactive oxygen species (ROS)-induced cellular damage. In addition, this formulation may also inhibit various signal transduction pathways involved in inflammation and cancer, may suppress the growth of susceptible tumor cells, induce tumor cell cycle arrest, induce apoptosis and reduce angiogenesis and metastasis.
  • Gs/pan-notch inhibitor al101 - A small-molecule gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon intravenous administration, GS/pan-Notch inhibitor AL101 binds to GS and blocks activation of Notch receptors, which may inhibit the proliferation of tumor cells with an overly-active Notch pathway. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains that lead to their activation. Overactivation of the Notch signaling pathway, often triggered by activating mutations, has been correlated with increased cellular proliferation and poor prognosis in certain tumor types.
  • Gs/pan-notch inhibitor bms-986115 - An orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, GS/pan-Notch inhibitor BMS 986115 binds to GS and blocks the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth of tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains and leads to their activation.
  • Gsk-3 inhibitor 9-ing-41 - A maleimide-based, small molecule inhibitor of glycogen synthase kinase-3 (GSK-3; serine/threonine-protein kinase GSK3) with potential antineoplastic activity. Upon intravenous administration, 9-ING-41 binds to and competitively inhibits GSK-3, which may lead to downregulation of nuclear factor kappa B (NF-kappaB) and decreased expression of NF-kappaB target genes including cyclin D1, B-cell lymphoma 2 (Bcl-2), anti-apoptotic protein XIAP, and B-cell lymphoma extra-large (Bcl-XL). This may inhibit NF-kappaB-mediated survival and chemoresistance in certain tumor types. GSK-3, a constitutively active serine/threonine kinase that plays a role in numerous pathways involved in protein synthesis, cellular proliferation, differentiation, and metabolism, is aberrantly overexpressed in certain tumor types and may promote tumor cell survival and resistance to chemotherapy and radiotherapy.
  • Gsk-3 inhibitor ly2090314 - An inhibitor of glycogen synthase kinase-3 (GSK-3), with potential antineoplastic activity. Upon administration, LY2090314 binds to and inhibits GSK-3 in an ATP-competitive manner. This prevents GSK-3-mediated phosphorylation of beta-catenin, which inhibits the subsequent ubiquitination and proteasomal degradation of beta-catenin. This leads to the activation of the Wnt/beta-catenin pathway and the induction of apoptosis in susceptible tumor cells. GSK-3, a serine/threonine kinase, plays a key role in numerous pathways involved in protein synthesis, cellular proliferation, differentiation, and apoptosis. The Wnt/beta-catenin signaling pathway plays key roles in both cellular proliferation and differentiation. The increased expression of beta-catenin, a transcriptional activator, correlates with decreased cellular proliferation and improved prognosis in select cancers.
  • Guadecitabine - A dinucleotide antimetabolite of a decitabine linked via phosphodiester bond to a guanosine, with potential antineoplastic activity. Following metabolic activation by phosphorylation and incorporation into DNA, guadecitabine inhibits DNA methyltransferase, thereby causing genome-wide and non-specific hypomethylation, and inducing cell cycle arrest at S-phase. This agent is resistant to cytidine deaminase, hence may result in gradual release of decitabine both extra and intracellularly, leading to more prolonged exposures to decitabine.
  • Guanabenz acetate - The orally bioavailable, acetate salt form of guanabenz, a centrally-acting alpha-2 adrenergic receptor agonist, with anti-hypertensive and potential antineoplastic, cytoprotective and bone resorption inhibitory activities. Upon oral administration, guanabenz suppresses endoplasmic reticulum (ER) stress by inhibiting the stress-induced dephosphorylation of eukaryotic translation initiation factor 2 alpha (eIF2a), thereby enhancing the phosphorylation level of eIF2a. This causes elF2a-mediated downregulation of the Rac1 pathway, upregulates the expression of activating transcription factor 4 (ATF4), which plays a key role in osteoblastogenesis, and downregulates the expression of nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1), which is a transcription factor that plays a key role in osteoclastogenesis. This enhances osteoblastogenesis and suppresses osteoclastogenesis. Altogether, this promotes new bone formation and prevents bone degradation. In addition, guanabenz blocks the proliferation, survival, motility and invasiveness of tumor cells through the eIF2a-mediated downregulation of Rac1 signaling. Rac1, a Ras-related small GTPase belonging to the Rho family, plays a key role in tumor cell proliferation, survival and motility.
  • Guarana supplement - An herbal supplement containing an extract from guarana (Paullinia cupana), a climbing plant of the Sapindaceae family which is native to the Amazon basin, with stimulant, antioxidant and potential chemoprotective activities. Guarana supplement contains various phytochemicals, including caffeine, theobromine, theophylline, tannins, saponins, catechins, epicatechins, proanthocyanidols and other compounds in minor concentrations. Caffeine is a central nervous system stimulant and may reduce chemotherapy-related fatigue. Tannins and other polyphenols may have chemopreventive activity. Intake of the guarana supplement may prevent cancer-related anorexia. In addition, animal studies have demonstrated that the ingestion of guarana resulted in decreased proliferation and increased apoptosis of tumor cells.
  • Guselkumab - An orally available, human, immunoglobulin G1 (IgG1) kappa, monoclonal antibody directed against the p19 protein subunit of interleukin-23 (IL-23), with immunomodulating activity. Upon administration, guselkumab binds to the p19 subunit of IL-23, thereby blocking the binding of IL-23 to the IL-23 receptor. This inhibits IL-23-mediated signaling and the differentiation of CD4-positive T-cells into Th1 and Th17 cells. This prevents Th1- and Th17-mediated immune responses and inhibits the production of pro-inflammatory cytokines. This may prevent or reduce symptoms and severity of immune-mediated inflammatory disorders. IL-23 plays a key role in the regulation of inflammation and the immune system, and modulates the release of various pro-inflammatory cytokines and chemokines. It is upregulated in various immune-mediated inflammatory disorders.
  • Gusperimus trihydrochloride - A derivative of the antitumor antibiotic spergualin with immunosuppressant activity. Gusperimus inhibits the interleukin-2-stimulated maturation of T cells to the S and G2/M phases and the polarization of the T cells into IFN-gamma-secreting Th1 effector T cells, resulting in the inhibition of growth of activated naive CD4 T cells; this agent may suppress growth of certain T-cell leukemia cell lines.
  • Gutolactone - A quassinoid phytochemical isolated from the plant Simaba guianensis with potential antineoplastic and antimalarial activities.

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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