CYP17A1 inhibitor
Drug class
Abiraterone acetate, a steroidal CYP17A1 inhibitor that is used in the treatment of prostate cancer.
Class identifiers
SynonymsAndrogen synthesis inhibitors
UseProstate cancer, precocious puberty, breast cancer, others
ATC codeL02BX
Biological targetCYP17A1
Chemical classSteroidal; Nonsteroidal
Legal status
In Wikidata

A CYP17A1 inhibitor is a type of drug which inhibits the enzyme CYP17A1.[1] 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).[2] 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.[3] 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.[4]

See also

References

  1. ^ Malikova, Jana; Brixius-Anderko, Simone; Udhane, Sameer S.; Parween, Shaheena; Dick, Bernhard; Bernhardt, Rita; Pandey, Amit V. (2017-09-08). "CYP17A1 inhibitor abiraterone, an anti-prostate cancer drug, also inhibits the 21-hydroxylase activity of CYP21A2". The Journal of Steroid Biochemistry and Molecular Biology. 174: 192–200. doi:10.1016/j.jsbmb.2017.09.007. ISSN 1879-1220. PMID 28893623. S2CID 6270824.
  2. ^ Küçükemre-Aydın, Banu; Öğrendil-Yanar, Özlem; Bilge, Ilmay; Baş, Firdevs; Poyrazoğlu, Şükran; Yılmaz, Alev; Emre, Sevinç; Bundak, Rüveyde; Saka, Nurçin; Darendeliler, Feyza (2015). "An easily missed diagnosis: 17-alpha-hydroxylase/17,20-lyase deficiency". The Turkish Journal of Pediatrics. 57 (3): 277–281. ISSN 2791-6421. PMID 26701948.
  3. ^ Arth, G. E.; Patchett, A. A.; Jefopoulus, T.; Bugianesi, R. L.; Peterson, L. H.; Ham, E. A.; Kuehl, F. A.; Brink, N. G. (1971-08-01). "Steroidal androgen biosynthesis inhibitors". Journal of Medicinal Chemistry. 14 (8): 675–679. doi:10.1021/jm00290a003. ISSN 0022-2623. PMID 5114062.
  4. ^ Gomez, Lissette; Kovac, Jason R.; Lamb, Dolores J. (2014-12-22). "CYP17A1 inhibitors in castration-resistant prostate cancer". Steroids. 95: 80–87. doi:10.1016/j.steroids.2014.12.021. ISSN 1878-5867. PMC 4323677. PMID 25560485.

External links


Androgens and antiandrogens
Categories