Sufugolix

  • Chemical Properties
CAS No. 308831-61-0 Cat. No. BCP35686
Name Sufugolix
Synonyms TAK-013; TAK013; TAK 013;
Formula C36H31F2N5O4S M. Wt 667.73
  • Biological Activity
Description Sufugolix is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively). It was under development for the treatment of endometriosis and uterine leiomyoma and reached phase II clinical trials for both of these indications, but was subsequently discontinued. It seems to have been supplanted by relugolix (TAK-385), which is also under development by Takeda for the treatment of these conditions and has a more favorable drug profile (including reduced cytochrome P450 inhibition and improved in vivo GnRHR antagonistic activity) in comparison.
Pathways GPCR/G Protein 
Targets Glucagon Receptor 

Structure

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