Telapristone

Telapristone (INN), 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]

Telapristone
Clinical data
Other namesCDB-4124; Proellex; Progenta; 17β-(Acetyloxy)-11β-[4-(dimethylamino)phenyl]-17α-(2-methoxyacetyl)estra-4,9-dien-3-one
Drug classSelective progesterone receptor modulator
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC31H39NO5
Molar mass505.655 g·mol−1
3D model (JSmol)
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See also

References

  1. http://adisinsight.springer.com/drugs/800014404
  2. 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.2003.12.004. PMID 15120421. S2CID 23958876.
  3. 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.



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