abiraterone + enzalutamide

Abiraterone and enzalutamide are two distinct oral small molecule drugs used in the treatment of metastatic castration-resistant prostate cancer (mCRPC). Abiraterone acetate is a selective inhibitor of Cytochrome P450 17A1 (CYP17A1), an enzyme critical for androgen biosynthesis, thereby reducing androgen production from all sources. Enzalutamide is a direct androgen receptor inhibitor that blocks the AR pathway at multiple points: it prevents ligand binding, inhibits AR nuclear translocation, and blocks DNA transactivation. Both drugs disrupt androgen receptor signaling but through different mechanisms. The combination has been studied to overcome resistance mechanisms; however, clinical trials have not shown significant added benefit over monotherapy and have reported increased toxicity with the combination[4][8]. Abiraterone was developed by Janssen (a Johnson & Johnson company), while enzalutamide was developed by Medivation/Astellas.

Brand names

XtandiZytigaYonsa

Other names

abiraterone acetate