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Abiraterone is an orally administered small molecule antiandrogen used in combination with prednisone to treat metastatic castration-resistant prostate cancer (mCRPC) and metastatic high-risk castration-sensitive prostate cancer (CSPC). It acts as a potent, irreversible, and selective inhibitor of the enzyme 17α-hydroxylase/C17,20-lyase (CYP17), which is crucial for androgen biosynthesis in testicular, adrenal, and prostatic tumor tissues. By inhibiting CYP17, abiraterone reduces androgen production—male hormones that can promote tumor growth in the prostate gland. Abiraterone acetate is a prodrug developed to improve oral bioavailability and stability. The drug was first approved by regulatory agencies such as the FDA and EMA in 2011 for use in advanced prostate cancer settings. Developed and manufactured by Janssen.
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