Abiraterone

Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17, 20 lyase (CYP17A1) with an IC50 of 4 nM, an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues. Abiraterone was recently approved for the treatment of docetaxel-treated castration-resistant prostate cancer (CRPC), is often effective, but requires coadministration with glucocorticoids to curtail side effects. Abiraterone inhibited 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.