Irosustat (INN, USAN; developmental code names STX-64, 667-coumate, BN-83495; also known as oristusane) is an orally active, irreversible, nonsteroidal inhibitor of steroid sulfatase (STS) which was under development by Ipsen for the treatment of hormone-sensitive cancers such as breast cancer, prostate cancer, and endometrial cancer but was never marketed.[2][1] The drug reached phase II clinical trials prior to the discontinuation of its development.[2][3]
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| Other names | Oristusane; STX-64; 667-Coumate; BN-83495; STX-64PC |
| Routes of administration | By mouth[1] |
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| Elimination half-life | 24 hours[1] |
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| Formula | C14H15NO5S |
| Molar mass | 309.34 g·mol−1 |
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By inhibiting STS, irosustat prevents the conversion of hormonally inactive steroid sulfates such as DHEA sulfate (DHEA-S) and estrone sulfate (E1S) into their respective active forms, DHEA and estrone (which, in turn, can be transformed into more potent androgens and estrogens, respectively).[1] Administration of 5 mg/day irosustat to women with breast cancer for 5 days inhibited STS activity by 98 to 99% in breast tumor tissue and significantly decreased serum levels of estrone (by 76%), estradiol (by 39%), DHEA (by 41%), androstenediol (by 70%), androstenedione (by 62%), and testosterone (by 30%), whereas levels of DHEA-S and E1S increased slightly (by 1.1% and 7.4%, respectively).[1]
See also
References
- ^ a b c d e Palmieri C, Januszewski A, Stanway S, Coombes RC (2011). "Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer". Expert Rev Anticancer Ther. 11 (2): 179–83. doi:10.1586/era.10.201. PMID 21342037.
- ^ a b http://adisinsight.springer.com/drugs/800020388
- ^ Carmen Avendano; J. Carlos Menendez (11 June 2015). Medicinal Chemistry of Anticancer Drugs. Elsevier Science. pp. 105–. ISBN 978-0-444-62667-7.
External links
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