Abiraterone (CB-7598) is a potent and irreversible CYP17A1 inhibitor with IC50 of 4 nM for 17α-hydroxylase.
Abiraterone shows 6-fold more selective for inhibition of 17α-hydroxylase over 17,20-lyase.
Abiraterone also acts as a partial antagonist of the AR, and as an inhibitor of the 3β-HSD, CYP11B1, and other CYP450s (e.g., CYP1A2, CYP2C9, and CYP3A4).
Abiraterone is highly active in the treatment of castration-resistant prostate cancer; the active agent of prodrug abiraterone acetate.
