Obatoclax: Difference between revisions
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Obatoclax mesylate, also known as GX15-070, is an experimental drug for the treatment of various types of cancer. It was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals.<ref>Cephalon Announces Definitive Agreement to Acquire Gemin X, March 21, 2011</ref> Several Phase II clinical trials were completed that investigated use of Obatoclax in the treatment of leukemia, lymphoma, myelofibrosis, and mastocytosis.<ref>,
Phase II Study of Obatoclax Mesylate (GX15-070), a Small-Molecule BCL-2 Family Antagonist, for Patients with Myelofibrosis, Clinical Lymphoma, Myeloma & Leukemia, 2010, Vol. 10(Issue: 4), pp. 285–9, DOI: 10.3816/CLML.2010.n.059, PMID: 20709666,</ref><ref>Gemin X Presents New Data on Obatoclax at the American Society of Hematology Meeting, Dec 9, 2008</ref><ref>Obatoclax at ClinicalTrials.gov</ref>
Mechanism of action
Obatoclax is an inhibitor of the Bcl-2 family of proteins.<ref>,
Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax), Cancer Research, 2008, Vol. 68(Issue: 9), pp. 3413–20, DOI: 10.1158/0008-5472.CAN-07-1919, PMID: 18451169, PMC: 4096127,</ref> This inhibition induces apoptosis in cancer cells, preventing tumor growth. Solubility has been an issue in the development of the drug.<ref>, Obatoclax is a direct and potent antagonist of membrane-restricted Mcl-1 and is synthetic lethal with treatment that induces Bim, BMC Cancer, 2015, Vol. 15, DOI: 10.1186/s12885-015-1582-5, PMC: 4522062,</ref>
Clinical trials
Clinical trial results have been published for treatment of acute myeloid leukemia,<ref>,
A Multicenter Phase I/II Study of Obatoclax Mesylate Administered as a 3- or 24-Hour Infusion in Older Patients with Previously Untreated Acute Myeloid Leukemia, PLoS ONE, 2014, Vol. 9(Issue: 10), pp. e108694, DOI: 10.1371/journal.pone.0108694, PMID: 25285531, PMC: 4186779,</ref> small cell lung cancer,<ref>, Randomized phase II study of carboplatin and etoposide with or without obatoclax mesylate in extensive-stage small cell lung cancer, Lung Cancer, 2014, Vol. 85(Issue: 3), pp. 420–8, DOI: 10.1016/j.lungcan.2014.05.003, PMID: 24997137,</ref> Hodgkin's lymphoma,<ref>, Experience with obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist in patients with relapsed or refractory classical Hodgkin lymphoma, Blood, 2012, Vol. 119(Issue: 9), pp. 2171–2, DOI: 10.1182/blood-2011-11-391037, PMID: 22383790,</ref> myelodysplastic syndromes,<ref>, A Phase II, Multicenter, Open-Label Study of Obatoclax Mesylate in Patients with Previously Untreated Myelodysplastic Syndromes with Anemia or Thrombocytopenia, Clinical Lymphoma, Myeloma & Leukemia, 2014, Vol. 14(Issue: 6), pp. 534–9, DOI: 10.1016/j.clml.2014.04.007, PMID: 25052051,</ref>
Teva halted a phase III trial in patients with lung cancer before it had begun, citing "business decisions" as the reason.<ref>Clinical trial number NCT01563601 for "Efficacy and Safety of Obatoclax Mesylate in Combination With Carboplatin and Etoposide Compared With Carboplatin and Etoposide Alone in Chemotherapy-Naive Patients With Extensive-Stage Small Cell Lung Cancer" at ClinicalTrials.gov </ref>
See also
References
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