Inocoterone acetate
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| Synonyms | RU-38882; RU-882; 2,5-Seco-A-dinorestr-9-en-17β-ol-5-one 17β-acetate |
| Drug class | Nonsteroidal antiandrogen |
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| Formula | C18H26O3 |
| Molar mass | 290.403 g/mol |
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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]
See also
References
- 1 2 3 4 Richard A. Helms; David J. Quan (2006). Textbook of Therapeutics: Drug and Disease Management. Lippincott Williams & Wilkins. pp. 211–. ISBN 978-0-7817-5734-8.
- 1 2 Bentham Science Publishers (September 1999). Current Pharmaceutical Design. Bentham Science Publishers. pp. 717–.
- ↑ Annual Reports in Medicinal Chemistry. Academic Press. 2 September 1987. pp. 203–. ISBN 978-0-08-058366-2.
- ↑ Térouanne B, Tahiri B, Georget V, Belon C, Poujol N, Avances C, Orio F, Balaguer P, Sultan C (2000). "A stable prostatic bioluminescent cell line to investigate androgen and antiandrogen effects". Mol. Cell. Endocrinol. 160 (1–2): 39–49. doi:10.1016/s0303-7207(99)00251-8. PMID 10715537.
- ↑ Leo Plouffe, Jr; Botros R. M. B. Rizk (25 June 2015). Androgens in Gynecological Practice. Cambridge University Press. pp. 84–. ISBN 978-1-316-29887-9.
- 1 2 Lookingbill, D. P. (1992). "Inocoterone and acne. The effect of a topical antiandrogen: results of a multicenter clinical trial". Archives of Dermatology. 128 (9): 1197–1200. doi:10.1001/archderm.128.9.1197. ISSN 0003-987X.