化合物简介
Sufugolix (INN, BAN) (developmental code name TAK-013) 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 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.
基本信息
中文名称
舒夫戈利
英文名称
sufugolix
中文别名
英文别名
CAS号
308831-61-0
分子式
C36H31F2N5O4S
分子量
667.724
精确质量
667.206
PSA
125.84
LOGP
6.9862
物化性质
密度
1.383g/cm3
折射率
1.667
合成路线
上游原料
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