Telapristone
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| Other names | CDB-4124; Proellex; Progenta; 17β-(Acetyloxy)-11β-[4-(dimethylamino)phenyl]-17α-(2-methoxyacetyl)estra-4,9-dien-3-one |
| Drug class | Selective progesterone receptor modulator |
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| Formula | C31H39NO5 |
| Molar mass | 505.655 g·mol−1 |
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Telapristone (INN Tooltip International Nonproprietary Name), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids.[1] [2] It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications.[1] In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity.[3]
See also
[edit ]- List of investigational sex-hormonal agents § Progestogenics
- Aglepristone
- Lilopristone
- Onapristone
- Toripristone
References
[edit ]- ^ a b "Telapristone - Repros Therapeutics - AdisInsight".
- ^ Attardi BJ, Burgenson J, Hild SA, Reel JR (2004). "In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone". J. Steroid Biochem. Mol. Biol. 88 (3): 277–88. doi:10.1016/j.jsbmb.200312004. PMID 15120421. S2CID 23958876.
- ^ Whitaker LH, Williams AR, Critchley HO (2014). "Selective progesterone receptor modulators". Curr. Opin. Obstet. Gynecol. 26 (4): 237–42. doi:10.1097/GCO.0000000000000082. PMID 24950125. S2CID 37474964.
External links
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