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Telapristone

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Chemical compound Pharmaceutical compound
Telapristone
Clinical data
Other namesCDB-4124; Proellex; Progenta; 17β-(Acetyloxy)-11β--17α-(2-methoxyacetyl)estra-4,9-dien-3-one
Drug classSelective progesterone receptor modulator
Legal status
Legal status
  • Investigational
Identifiers
IUPAC name
  • -17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopentaphenanthren-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
3D model (JSmol)
SMILES
  • O=C5\C=C3/C(=C2/(c1ccc(N(C)C)cc1)C4((OC(=O)C)(C(=O)COC)CC42CC3)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
  • Key:JVBGZFRPTRKSBB-MJBQOYBXSA-N
  (verify)

Telapristone (INNTooltip 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. 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. In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity.

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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Progestogens and antiprogestogens
Progestogens
(and progestins)
PRTooltip Progesterone receptor agonists
Antiprogestogens
SPRMsTooltip Selective progesterone receptor modulators
PRTooltip Progesterone receptor antagonists
See also
Progesterone receptor modulators
Androgens and antiandrogens
Estrogens and antiestrogens
List of progestogens
Progesterone receptor modulators
PRTooltip Progesterone receptor
Agonists
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(SPRMsTooltip Selective progesterone receptor modulators)
Antagonists
mPRTooltip Membrane progesterone receptor
(PAQRTooltip Progestin and adipoQ receptor)
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See also
Receptor/signaling modulators
Progestogens and antiprogestogens
Androgen receptor modulators
Estrogen receptor modulators
List of progestogens
Glucocorticoid receptor modulators
GRTooltip Glucocorticoid receptor
Agonists
Mixed
(SEGRMsTooltip Selective glucocorticoid receptor agonists)
Antagonists
Others
See also
Receptor/signaling modulators
Glucocorticoids and antiglucocorticoids
Mineralocorticoid receptor modulators
List of corticosteroids


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