Abiraterone

From WikiMD


Abiraterone, developmental code name CB-7598, also known as 17-(3-pyridyl)androsta-5,16-dien-3β-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.[1]

Abiraterone acetate

Abiraterone acetate (brand names Zytiga, Abiratas, Abretone, Abirapro) is used in the treatment of prostate cancer.[2][3] Prostate cancer cells are stimulated to grow and spread by circulating androgen hormones. The intended effect of the drug is to block both physiologic and tumor-related androgen (e.g. testosterone) production, in order to slow or stop the spread of cancer cells.[4] Since the drug blocks normal physiologic production of steroids by the adrenal glands, it is commonly prescribed with a low-dose steroid in order to prevent adrenal insufficiency.

In addition to acting as an irreversible inhibitor of CYP17A1 (17α-hydroxylase/17,20-lyase), abiraterone inhibits 3β-hydroxysteroid dehydrogenase (3β-HSD), steroid 11β-hydroxylase (CYP11B1), 5α-reductase (via a metabolite)[5] and certain hepatic cytochrome P450 enzymes (e.g., CYP1A2, CYP2C9, and CYP3A4).[6] The drug acts as a partial antagonist of the androgen receptor and as an agonist of the estrogen receptor.[6][7]

References

References



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