Description
Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC
50 = 0.1 nM). Sufugolix inhibits GnRH-induced arachidonic acid (Item Nos.
90010 |
90010.1 |
10006607) release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC
50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor. It inhibits luteinizing hormone (LH) release stimulated by GnRH in monkey pituitary cells
ex vivo (IC
50 = 36 nM). Sufugolix (10 and 30 mg/kg) reduces increases in plasma LH following castration in male cynomolgus monkeys and lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys when administered at a dose of 90 mg/kg.
