Opigolix

Opigolix (INN, USAN; developmental code name ASP-1707) is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which was under development by Astellas Pharma for the treatment of endometriosis and rheumatoid arthritis.[1][2] It was also under investigation for the treatment of prostate cancer.[1] It reached phase II clinical trials for both endometriosis and rheumatoid arthritis prior to the discontinuation of its development in April 2018.[1]

Opigolix
Clinical data
Other namesASP-1707
Routes of
administration		By mouth
Drug classGnRH modulator; GnRH antagonist; Antigonadotropin
Identifiers
IUPAC name
  • (2R)-N'-[5-[3-(2,5-difluorophenyl)-2-(1,3-dihydrobenzimidazol-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl]sulfonyl-2-hydroxypropanimidamide
CAS Number
PubChem CID
UNII
KEGG
Chemical and physical data
FormulaC25H19F3N4O5S
Molar mass544.51 g·mol−1
3D model (JSmol)
SMILES
  • C[C@@H](O)/C(N)=N/S(=O)(=O)c1cc(C(=O)C(C(=O)c2cc(F)ccc2F)=C2Nc3ccccc3N2)ccc1F
InChI
  • InChI=1S/C25H19F3N4O5S/c1-12(33)24(29)32-38(36,37)20-10-13(6-8-17(20)28)22(34)21(23(35)15-11-14(26)7-9-16(15)27)25-30-18-4-2-3-5-19(18)31-25/h2-12,30-31,33H,1H3,(H2,29,32)/t12-/m1/s1
  • Key:CWNLBPBIFALUQD-GFCCVEGCSA-N

See also
  • Gonadotropin-releasing hormone receptor § Antagonists

References
  1. "Opigolix - Astellas Pharma - AdisInsight".
  2. Ezzati M, Carr BR (2015). "Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain". Women's Health. 11 (1): 19–28. doi:10.2217/whe.14.68. PMID 25581052.


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