Obatoclax

Chemical compound From Wikipedia, the free encyclopedia

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]

Quick facts Names, Identifiers ...
Obatoclax
Names
IUPAC name
2-(2-((3,5-Dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-1H-indole
Other names
GX15-070
Identifiers
3D model (JSmol)
ChemSpider
UNII
  • InChI=1S/C20H19N3O/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17/h4-11,21-22H,1-3H3/b19-10+
  • Cc1cc([nH]c1/C=C/2\C(=CC(=N2)c3cc4ccccc4[nH]3)OC)C
Properties
C20H19N3O
Molar mass 317.392 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Mechanism of action

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

Clinical trial results have been published for treatment of acute myeloid leukemia,[7] small cell lung cancer,[8] Hodgkin's lymphoma,[9] and 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

References

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