[CAS NO. 154229-18-2]  Abiraterone Acetate (CB7630)

Abiraterone shows a good complexation with the heme iron only in SM1. Abiraterone blocks the synthesis of androgens by inhibiting CYP17A1. Abiraterone also blocks 3β-hydroxysteroid dehydrogenase (3βHSD), an enzyme that is absolutely required for the synthesis of biologically active androgens. Abiraterone inhibits conversion of DHEA to Δ-androstenedione. Abiraterone inhibition of 3βHSD blocks DHT synthesis and the androgen receptor response. Abiraterone inhibits the conversion of Δ-androstenediol to testosterone. Abiraterone inhibits C-lyase, with an IC50 of 5.8 nM, in rat testis microsomes. Abiraterone significantly inhibits testosterone secretion (−48%) and in turn increases LH concentration (192%). Abiraterone inhibits in vitro proliferation and AR-regulated gene expression of AR-positive prostate cancer cells, which could be explained by AR antagonism in addition to inhibition of steroidogenesis.