Directing abiraterone metabolism: balancing the scales between clinical relevance and experimental observation

In their recent report published in Nature, Li and colleagues investigate the feasibility of exploiting drug metabolism pathways to improve abiraterone treatment for castration resistant prostate cancer (CRPC). Abiraterone is a 17α-hydroxylase/17,20-lyase (CYP17A1) inhibitor, and is used in the context of androgen deprivation therapy to prevent the de novo generation of androgens by the tumor from cholesterol or adrenal precursor molecules. While abiraterone initially blocks androgen synthesis and prolongs survival, the disease will ultimately progress despite treatment (1,2).