Biology:CYP17A1 inhibitor
CYP17A1 inhibitor | |
---|---|
Drug class | |
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 |
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
- Steroidogenic enzyme
- Steroidogenesis inhibitor
- Nonsteroidal antiandrogen
- Gonadotropin-releasing hormone analogue
References
- ↑ 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.
- ↑ Küçükemre-Aydın, Banu; Öğrendil-Yanar, Özlem; Bilge, Ilmay; Baş, Firdevs; Poyrazoğlu, Şükran; Yılmaz, Alev; Emre, Sevinç; Bundak, Rüveyde et al. (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. https://pubmed.ncbi.nlm.nih.gov/26701948/.
- ↑ 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. https://pubmed.ncbi.nlm.nih.gov/5114062/.
- ↑ 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. PMID 25560485.
External links
{{Navbox
| name = Androgens and antiandrogens | title = Androgens and antiandrogens | state = collapsed | listclass = hlist | groupstyle = text-align:center;
| group1 = Androgens
(incl. AAS)
| list1 =
| group2 = Antiandrogens | list2 = {{Navbox|child | groupstyle = text-align:center; | groupwidth = 9em;
| group1 = AR antagonists | list1 =
- Steroidal: Abiraterone acetate
- Canrenone
- Chlormadinone acetate
- Cyproterone acetate
- Delmadinone acetate
- Dienogest
- Drospirenone
- Medrogestone
- Megestrol acetate
- Nomegestrol acetate
- Osaterone acetate
- Oxendolone
- Potassium canrenoate
- Spironolactone
- Nonsteroidal: Apalutamide
- Bicalutamide
- Cimetidine
- Darolutamide
- Enzalutamide
- Flutamide
- Ketoconazole
- Nilutamide
- Seviteronel†
- Topilutamide (fluridil)
| group2 = Steroidogenesis| list2 =
inhibitors
5α-Reductase | |
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Others |
| group3 = Antigonadotropins | list3 =
- D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride)
- Estrogens (e.g., bifluranol, [[diethylstilbestrol, estradiol, estradiol esters, ethinylestradiol, ethinylestradiol sulfonate, paroxypropione)
- GnRH agonists (e.g., leuprorelin)
- GnRH antagonists (e.g., cetrorelix)
- Progestogens (incl., chlormadinone acetate, [[cyproterone acetate, hydroxyprogesterone caproate, gestonorone caproate, [[Chemistry:Medroxyprogesterone medroxyprogesterone acetate, Chemistry:Megestrol acetate|megestrol acetate]])
| group4 = Others | list4 =
- Androstenedione immunogens: Androvax (androstenedione albumin)
- Ovandrotone albumin (Fecundin)
}}
| liststyle = background:#DDDDFF;| list3 =
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
- See also
- Androgen receptor modulators
- Estrogens and antiestrogens
- Progestogens and antiprogestogens
- List of androgens/anabolic steroids
}}
Original source: https://en.wikipedia.org/wiki/CYP17A1 inhibitor.
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