Obatoclax

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]

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
CAS Number	803712-67-6 Y 803712-79-0 (mesylate) Y
3D model (JSmol)	Interactive image
ChemSpider	24539359
PubChem CID	11404337 16681698 (mesylate)
UNII	QN4128B52A Y 39200FJ43J (mesylate) Y
InChI 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+
SMILES Cc1cc([nH]c1/C=C/2\C(=CC(=N2)c3cc4ccccc4[nH]3)OC)C
Properties
Chemical formula	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). Infobox references

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

• Navitoclax