Abiraterone, developmental code name CB-7598, also known as 17-(3-pyridyl)androsta-5,16-dien-3?-ol, is a synthetic, steroidal CYP17A1 inhibitor. It is the active metabolite of abiraterone acetate, an ester and prodrug of abiraterone.
A metabolite of abiraterone has been found to act as an agonist of the androgen receptor, and may antagonize the clinical effectiveness of abiraterone acetate.
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Abiraterone acetate
Abiraterone acetate (brand names Zytiga, Abiratas, Abretone, Abirapro) is used in the treatment of prostate cancer. In addition to acting as an irreversible inhibitor of CYP17A1 (17?-hydroxylase/17,20-lyase), abiraterone inhibits 3?-hydroxysteroid dehydrogenase (3?-HSD), steroid 11?-hydroxylase (CYP11B1), 5?-reductase (via a metabolite) and certain hepatic cytochrome P450 enzymes (e.g., CYP1A2, CYP2C9, and CYP3A4). The drug acts as a partial antagonist of the androgen receptor and as an agonist of the estrogen receptor.
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