Biochem/physiol Actions

Degarelix acetate (FE200486) is a gonadotropin-/luteinizing hormone-/follicle-stimulating hormone-releasing hormone (GnRH, LHRH, FSH-RH) receptor antagonist that inhibits plasma testosterone for more than 40 days following a single s.c. dosage of 2 mg/kg in rats and monkeys, showing longer in vivo duration than abarelix, ganirelix, cetrorelix, azaline B or D-Trp6-LHRH, and exhibiting only weak histamine-releasing potency in isolated rat mast cells. Bi-weekly s.c. dosing (2 mg/kg) is efficacious in suppressing the growth of human prostate cancer PAC120 xenograft-derived tumors in mice in vivo.