Linzagolix

Linzagolix (INN; developmental code names KLH-2109, OBE-2109; tentative brand name Yselty) is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by Kissei Pharmaceutical and ObsEva for the treatment of uterine fibroids, endometriosis, and adenomyosis.[1][3][2] As of December 2020, it is under review for approval for uterine fibroids, is in phase III clinical trials for endometriosis, and is in phase II clinical studies for adenomyosis.[1]

Linzagolix
Clinical data
Trade namesYselty
Other namesKLH-2109; OBE-2109
Routes of
administration		By mouth[1][2]
Drug classGnRH modulator; GnRH antagonist; Antigonadotropin
ATC code
  • None
Identifiers
  • 3-{5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl}-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid
CAS Number
  • 935283-04-8
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC22H15F3N2O7S
Molar mass508.42 g·mol−1
3D model (JSmol)
  • O=C(C1=C(C(N2C3=CC(OCC4=C(OC)C=CC(F)=C4F)=C(OC)C=C3F)=O)C(NC2=O)=CS1)O
  • InChI=1S/C22H15F3N2O7S/c1-32-14-4-3-10(23)18(25)9(14)7-34-16-6-13(11(24)5-15(16)33-2)27-20(28)17-12(26-22(27)31)8-35-19(17)21(29)30/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30)
  • Key:BMAAMIIYNNPHAB-UHFFFAOYSA-N

See also

References
  1. "Linzagolix - Kissei Pharmaceutical/ObsEva - AdisInsight".
  2. Ezzati M, Carr BR (2015). "Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain". Womens Health (Lond). 11 (1): 19–28. doi:10.2217/whe.14.68. PMID 25581052.
  3. Chodankar, Rohan; Allison, Jennifer (2018). "New Horizons in Fibroid Management". Current Obstetrics and Gynecology Reports. 7 (2): 106–115. doi:10.1007/s13669-018-0242-6. ISSN 2161-3303.



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