产品描述:
Linzagolix is a nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 36.7 nM for the human receptor).{65962} Unlike the peptide GnRH receptor antagonist cetrorelix (Item No. 23910), linzagolix (10 µM) does not induce histamine release in isolated rat peritoneal mast cells.{65963} Linzagolix (25 and 50 mg/kg) suppresses the menstrual cycle in normal cynomolgus monkeys.{65962} It decreases serum luteinizing hormone (LH) levels in ovariectomized cynomolgus monkeys when administered at doses ranging from 1 to 100 mg/kg. Linzagolix (50-200 mg/kg, p.o.) decreases cyst volume in a rat model of endometriosis induced by autotransplantation of endometrial tissue into the renal subcapsular space.{65963} Formulations containing linzagolix have been used in the treatment of uterine fibroids.