Chemistry:Inocoterone acetate
 | |
| Clinical data | |
|---|---|
| Other names | RU-38882; RU-882; 2,5-Seco-A-dinorestr-9-en-17β-ol-5-one 17β-acetate |
| Drug class | Nonsteroidal antiandrogen |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C18H26O3 |
| Molar mass | 290.403 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Inocoterone acetate (USAN) (developmental code names RU-38882, RU-882) is a steroid-like nonsteroidal antiandrogen (NSAA) that was developed for topical administration to treat acne but was never marketed.[1][2] It is the acetate ester of inocoterone, which is less potent in comparison.[3] Inocoterone acetate is actually not a silent antagonist of the androgen receptor but rather a weak partial agonist, similarly to steroidal antiandrogens like cyproterone acetate.[4]
Inocoterone acetate was investigated for the treatment of acne but showed only modest (albeit statistically significant) efficacy in clinical trials.[2][5][6] A reduction of 26% of lesions was observed in males treated with the drug after 16 weeks (~3.7 months).[6][1] However, this is notably far less than that achieved with other agents such as benzoyl peroxide or antibiotics, which produce 50–75% reductions within 2 months.[1] Similar poor results with the topical route have disappointingly been found for other antiandrogens, such as cyproterone acetate and spironolactone.[1] Similarly to rosterolone, inocoterone acetate has no systemic antiandrogenic activity when applied systemically.[7]
See also
References
- ↑ 1.0 1.1 1.2 1.3 "Common skin disorders". Textbook of Therapeutics: Drug and Disease Management. Lippincott Williams & Wilkins. 2006. pp. 203–256 (211). ISBN 978-0-7817-5734-8. https://books.google.com/books?id=aVmRWrknaWgC&pg=PA211.
- ↑ 2.0 2.1 "Current aspects of antiandrogen therapy in women". Current Pharmaceutical Design 5 (9): 707–23. September 1999. doi:10.1002/chin.200002286. PMID 10495361. https://books.google.com/books?id=9rfNZL6oEO0C&pg=PA717.
- ↑ "Dermatological agents.". Annual Reports in Medicinal Chemistry (Academic Press) 22: 201-212 (203). January 1987. doi:10.1016/S0065-7743(08)61168-9. ISBN 978-0-08-058366-2. https://books.google.com/books?id=oJeTSJveeuAC&pg=PA203.
- ↑ "A stable prostatic bioluminescent cell line to investigate androgen and antiandrogen effects". Molecular and Cellular Endocrinology 160 (1–2): 39–49. February 2000. doi:10.1016/s0303-7207(99)00251-8. PMID 10715537.
- ↑ "Androgen effects on the skin". Androgens in Gynecological Practice. Cambridge University Press. 25 June 2015. pp. 79–88 (84). doi:10.1017/CBO9781139649520.010. ISBN 978-1-316-29887-9. https://books.google.com/books?id=MMz2CQAAQBAJ&pg=PA84.
- ↑ 6.0 6.1 "Inocoterone and acne. The effect of a topical antiandrogen: results of a multicenter clinical trial". Archives of Dermatology 128 (9): 1197–1200. September 1992. doi:10.1001/archderm.128.9.1197. PMID 1387778.
- ↑ "Antiandrogens and Hair Growth: Basic Concepts and Experimental Research". Hair and Hair Diseases. 1990. pp. 791–826. doi:10.1007/978-3-642-74612-3_34. ISBN 978-3-642-74614-7.
 |  |
