Sufugolix
Sufugolix (, ) (developmental code name TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) ( = 0.1 and 0.06 nM for affinity and ''in vitro'' inhibition, respectively). It was under development by Takeda 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. Oral administration of sufugolix at a dose of 30 mg/kg to castrated male cynomolgus monkey The crab-eating macaque (''Macaca fascicularis''), also known as the long-tailed macaque and referred to as the cynomolgus monkey in laboratories, is a cercopithecin ...
[...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]