Asoprisnil ecamate

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Asoprisnil ecamate
Asoprisnil ecamate.svg
Clinical data
Synonyms J-956; 11β-(4-((E)-(Ethylcarbamoyl-oxyimino)methyl)phenyl)-17β-methoxy-17α-(methoxymethyl)estra-4,9-dien-3-one
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C31H40N2O5
Molar mass 520.67 g·mol−1
3D model (JSmol)

Asoprisnil ecamate (INN) (developmental code name J-956) is a synthetic, steroidal selective progesterone receptor modulator (SPRM) which was under development for the treatment of endometriosis, uterine fibroids, and menopausal symptoms but was discontinued.[1][2][3] It is a potent and highly selective ligand of the progesterone receptor (PR) with mixed agonistic and antagonstic activity and much reduced antiglucocorticoid activity relative to mifepristone.[2][3][4] The drug reached phase III clinical trials for the aforementioned indications prior to its discontinuation.[1]

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References[edit]

  1. ^ a b http://adisinsight.springer.com/drugs/800015923
  2. ^ a b Schubert G, Elger W, Kaufmann G, Schneider B, Reddersen G, Chwalisz K (2005). "Discovery, chemistry, and reproductive pharmacology of asoprisnil and related 11beta-benzaldoxime substituted selective progesterone receptor modulators (SPRMs)". Semin. Reprod. Med. 23 (1): 58–73. doi:10.1055/s-2005-864034. PMID 15714390. 
  3. ^ a b Chwalisz K, Perez MC, Demanno D, Winkel C, Schubert G, Elger W (2005). "Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis". Endocr. Rev. 26 (3): 423–38. doi:10.1210/er.2005-0001. PMID 15857972. 
  4. ^ Chwalisz K, Garg R, Brenner R, Slayden O, Winkel C, Elger W (2006). "Role of nonhuman primate models in the discovery and clinical development of selective progesterone receptor modulators (SPRMs)". Reprod. Biol. Endocrinol. 4 Suppl 1: S8. doi:10.1186/1477-7827-4-S1-S8. PMC 1775068Freely accessible. PMID 17118172. 

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