Clinical data
Routes of
CAS Number 851983-85-2
PubChem (CID) 11188409
ChemSpider 9363493
KEGG D10125 YesY
Chemical and physical data
Formula C26H32N2O
Molar mass 388.25
3D model (Jmol) Interactive image

Galeterone (TOK-001 or VN/124-1) is a novel steroidal antiandrogen under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique dual mechanism of action, acting as both an androgen receptor antagonist and an inhibitor of CYP17A1, an enzyme required for the biosynthesis of the androgens.[1] It shows selectivity for 17,20-lyase over 17-hydroxylase.[2]

Galeterone was being compared to enzalutamide in a phase III clinical trial (ARMOR3-SV) for AR-V7-expressing metastatic castration-resistant prostate cancer.[3][4] Tokai announced the discontinuation of ARMOR3-SV on July 26, 2016, after a data monitoring committee determined that the trial was unlikely to meet its endpoint.[5] On August 22, 2016, the company announced the discontinuation of their phase II expansion (ARMOR2) as well.[6]

See also


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