abiraterone + ketoconazole

Abiraterone and ketoconazole are both small molecule inhibitors that target androgen biosynthesis by inhibiting the enzyme cytochrome P450 17A1 (CYP17), which is crucial for androgen production. Abiraterone is a potent, selective, and irreversible inhibitor of CYP17 and is primarily used in combination with prednisone to treat metastatic castration-resistant prostate cancer (mCRPC) and high-risk metastatic castration-sensitive prostate cancer. Ketoconazole, originally developed as an antifungal agent under the brand name Nizoral, also inhibits CYP17 but is less potent and less specific than abiraterone. In some settings where abiraterone is unavailable or unaffordable, ketoconazole has been used off-label as an alternative for androgen deprivation in prostate cancer[2][5][8]. Both drugs suppress androgen synthesis but differ significantly in potency; abiraterone is tenfold to thirtyfold more potent than ketoconazole[5][8]. The combination of these two drugs together as a therapy regimen does not represent standard clinical practice due to overlapping mechanisms of action and potential for increased toxicity; rather they are considered alternatives or sequential options in treatment-resistant cases[6][8].

Other names

abiraterone acetateNizoral (for ketoconazole)