Obatoclax

Chemical Compound
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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

• Navitoclax

References

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