3D model (JSmol)
|Molar mass||317.39 g·mol−1|
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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. Several Phase II clinical trials were completed that investigated use of Obatoclax in the treatment of leukemia, lymphoma, myelofibrosis, and mastocytosis.
Mechanism of action
Obatoclax is an inhibitor of the Bcl-2 family of proteins. This inhibition induces apoptosis in cancer cells, preventing tumor growth. Solubility has been an issue in the development of the drug.
Teva halted a phase III trial in patients with lung cancer before it had begun, citing "business decisions" as the reason.
- Cephalon Announces Definitive Agreement to Acquire Gemin X, March 21, 2011
- Parikh, Sameer A.; Kantarjian, Hagop; Schimmer, Aaron; Walsh, William; Asatiani, Ekatherine; El-Shami, Khaled; Winton, Elliott; Verstovsek, Srdan (2010). "Phase II Study of Obatoclax Mesylate (GX15-070), a Small-Molecule BCL-2 Family Antagonist, for Patients with Myelofibrosis". Clinical Lymphoma Myeloma and Leukemia. 10 (4): 285–9. PMID 20709666. doi:10.3816/CLML.2010.n.059.
- Gemin X Presents New Data on Obatoclax at the American Society of Hematology Meeting, Dec 9, 2008
- Obatoclax at ClinicalTrials.gov
- Konopleva, M.; Watt, J.; Contractor, R.; Tsao, T.; Harris, D.; Estrov, Z.; Bornmann, W.; Kantarjian, H.; Viallet, J.; Samudio, I.; Andreeff, M. (2008). "Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax)". Cancer Research. 68 (9): 3413–20. PMC . PMID 18451169. doi:10.1158/0008-5472.CAN-07-1919.
- Nguyen, Mai; Cencic, Regina; Ertel, Franziska; Bernier, Cynthia; Pelletier, Jerry; Roulston, Anne; Silvius, John R.; Shore, Gordon C. (2015). "Obatoclax is a direct and potent antagonist of membrane-restricted Mcl-1 and is synthetic lethal with treatment that induces Bim". BMC Cancer. 15. doi:10.1186/s12885-015-1582-5.
- Schimmer, Aaron D.; Raza, Azra; Carter, Thomas H.; Claxton, David; Erba, Harry; Deangelo, Daniel J.; Tallman, Martin S.; Goard, Carolyn; Borthakur, Gautam (2014). "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. 9 (10): e108694. Bibcode:2014PLoSO...9j8694S. PMC . PMID 25285531. doi:10.1371/journal.pone.0108694.
- Langer, Corey J.; Albert, Istvan; Ross, Helen J.; Kovacs, Peter; Blakely, L. Johnetta; Pajkos, Gabor; Somfay, Attila; Zatloukal, Petr; Kazarnowicz, Andrzej; Moezi, Mehdi M.; Schreeder, Marshall T.; Schnyder, Judy; Ao-Baslock, Ada; Pathak, Ashutosh K.; Berger, Mark S. (2014). "Randomized phase II study of carboplatin and etoposide with or without obatoclax mesylate in extensive-stage small cell lung cancer". Lung Cancer. 85 (3): 420–8. PMID 24997137. doi:10.1016/j.lungcan.2014.05.003.
- Oki, Y.; Copeland, A.; Hagemeister, F.; Fayad, L. E.; Fanale, M.; Romaguera, J.; Younes, A. (2012). "Experience with obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist in patients with relapsed or refractory classical Hodgkin lymphoma". Blood. 119 (9): 2171–2. PMID 22383790. doi:10.1182/blood-2011-11-391037.
- Arellano, Martha L.; Borthakur, Gautam; Berger, Mark; Luer, Jill; Raza, Azra (2014). "A Phase II, Multicenter, Open-Label Study of Obatoclax Mesylate in Patients with Previously Untreated Myelodysplastic Syndromes with Anemia or Thrombocytopenia". Clinical Lymphoma Myeloma and Leukemia. 14 (6): 534–9. PMID 25052051. doi:10.1016/j.clml.2014.04.007.
- 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
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