Galeterone

Galeterone (TOK-001, VN/124-1) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively. Galeterone is effective at preventing binding of [3H]-R1881 (methyltrienolone, a stable synthetic androgen) to both the mutant AR (T877A) in LNCaP cells and the wild-type AR in PC-3AR cells. Galeterone potently inhibits the AR-mediated transcription in LNCaP cells transiently transfected with a probasin luciferase reporter construct AARZ-Luc in a concentration-dependent manner. Galeterone inhibits the growth of DHT-stimulated LNCaP and LAPC4 prostate cancer cells with IC50 of