Abiraterone acetate (AA) is a selective inhibitor of cytochrom p450 (CYP)17 which is required for androgen biosynthesis, and can block the androgens synthesis by testicles, surrenals and intratumoral secretion. In phase I and II studies in patients with prostate cancer, therapy with AA 250-2000 mg once daily demonstrated reductions in prostate specific antigen (PSA), and/or circulating tumor cells (CTCs). In two large phase III trials in patients with metastatic castration resistant prostate cancer (CRPC) in post-docetaxel and pre-docetaxel setting, AA plus prednisone compared with placebo plus prednisone demonstrated a significant superior overall survival in post-docetaxel setting, and a superior radiological PFS in pre-docetaxel setting. Based of these results, AA is approved in metastatic CRPC patients in post-docetaxel setting or pre-docetaxel setting in 2013.
Keywords: abiraterone acetate; castration-resistance prostate cancer; cytochrome CYP17; steroidogenosis.