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
IUPAC name
  • [(8S,11R,13S,14S,17R)-11-[4-(Dimethylamino)phenyl]-17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate
CAS Number
PubChem CID
PubChem SID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC31H39NO5
Molar mass505.655 g·mol−1
3D model (JSmol)
SMILES
  • O=C5\C=C3/C(=C2/[C@@H](c1ccc(N(C)C)cc1)C[C@@]4([C@@](OC(=O)C)(C(=O)COC)CC[C@H]4[C@@H]2CC3)C)CC5
InChI
  • InChI=1S/C31H39NO5/c1-19(33)37-31(28(35)18-36-5)15-14-27-25-12-8-21-16-23(34)11-13-24(21)29(25)26(17-30(27,31)2)20-6-9-22(10-7-20)32(3)4/h6-7,9-10,16,25-27H,8,11-15,17-18H2,1-5H3/t25-,26+,27-,30-,31-/m0/s1 Y
  • Key:JVBGZFRPTRKSBB-MJBQOYBXSA-N Y
  (verify)

See also

References
  1. "Telapristone - Repros Therapeutics - AdisInsight".
  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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