CYP17A1 inhibitor

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CYP17A1 inhibitor
Drug class
Abiraterone acetate.svg
Abiraterone acetate, a steroidal CYP17A1 inhibitor that is used in the treatment of prostate cancer.
Class identifiers
Synonyms Androgen synthesis inhibitors
Use Prostate cancer, precocious puberty, breast cancer, others
ATC code L02BX
Biological target CYP17A1
Chemical class Steroidal; Nonsteroidal
In Wikidata

A CYP17A1 inhibitor is a type of drug which inhibits the enzyme CYP17A1. It may inhibit both of the functions of the enzyme, 17α-hydroxylase and 17,20-lyase, or may be selective for inhibition of one of these two functions (generally 17,20-lyase), these drugs prevent the conversion of pregnane steroids into androgens like testosterone and therefore are androgen biosynthesis inhibitors and functional antiandrogens. Examples of CYP17A1 inhibitors include the older drug ketoconazole and the newer drugs abiraterone acetate, orteronel, galeterone, and seviteronel. The CYP17A1 inhibitors that have been marketed, like abiraterone acetate, are used mainly in the treatment of prostate cancer. CYP17A1 inhibitors that are not selective for inhibition of 17,20-lyase must be combined with a glucocorticoid such as prednisone in order to avoid adrenal insufficiency and mineralocorticoid excess caused by prevention of cortisol production.

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