Obatoclax
| Chemical Compound | |
|---|---|
| Identifiers | |
| CAS Number | |
| PubChem CID | |
| ChemSpider ID | |
| UNII | |
| ChEBI | |
| ChEMBL | |
| Properties | |
| Chemical Formula | |
| Molar Mass | |
| Appearance | |
| Density | |
| Melting Point | |
| Boiling Point | |
| Hazards | |
| GHS Pictograms | [[File:|50px]] |
| GHS Signal Word | |
| GHS Hazard Statements | |
| NFPA 704 | [[File:|50px]] |
| References | |
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.[1] Several Phase II clinical trials were completed that investigated use of Obatoclax in the treatment of leukemia, lymphoma, myelofibrosis, and mastocytosis.[2][3][4]
Mechanism of action[edit | edit source]
Obatoclax is an inhibitor of the Bcl-2 family of proteins.[5] This inhibition induces apoptosis in cancer cells, preventing tumor growth. Solubility has been an issue in the development of the drug.[6]
Clinical trials[edit | edit source]
Clinical trial results have been published for treatment of acute myeloid leukemia,[7] small cell lung cancer,[8] Hodgkin's lymphoma,[9] myelodysplastic syndromes,[10]
Teva halted a phase III trial in patients with lung cancer before it had begun, citing "business decisions" as the reason.[11]
See also[edit | edit source]
References[edit | edit source]
- ↑ Cephalon Announces Definitive Agreement to Acquire Gemin X, March 21, 2011
- ↑ , 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,
- ↑ Gemin X Presents New Data on Obatoclax at the American Society of Hematology Meeting, Dec 9, 2008
- ↑ Obatoclax at ClinicalTrials.gov
- ↑ , 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,
- ↑ , 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,
- ↑ , 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,
- ↑ , 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,
- ↑ , 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,
- ↑ , 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,
- ↑ 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
| Obatoclax Resources | |
|---|---|
 |
 |
Search WikiMD
Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD
|
WikiMD's Wellness Encyclopedia |
| Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Translate this page: - East Asian
中文,
日本,
한국어,
South Asian
हिन्दी,
தமிழ்,
తెలుగు,
Urdu,
ಕನ್ನಡ,
Southeast Asian
Indonesian,
Vietnamese,
Thai,
မြန်မာဘာသာ,
বাংলা
European
español,
Deutsch,
français,
Greek,
português do Brasil,
polski,
română,
русский,
Nederlands,
norsk,
svenska,
suomi,
Italian
Middle Eastern & African
عربى,
Turkish,
Persian,
Hebrew,
Afrikaans,
isiZulu,
Kiswahili,
Other
Bulgarian,
Hungarian,
Czech,
Swedish,
മലയാളം,
मराठी,
ਪੰਜਾਬੀ,
ગુજરાતી,
Portuguese,
Ukrainian
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates, categories Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD
