Cetrorelix is a synthetic peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with a K
d value of 0.2 nM for radioligand binding to murine LTK- cells expressing human GnRHR.
1 It inhibits the activation of hGnRHR and a downstream luciferase reporter gene in murine LTK- cells by the GnRHR agonist [D-Trp
6]GnRH (IC
50 = 1.2 nM).
In vivo, cetrorelix (60 μg per day) reduces tumor volume to 35% of control and decreases serum luteinizing hormone levels by 50% in a human epithelial ovarian cancer mouse xenograft model.
2 Centrorelix (0.5 mg/kg) protects the primordial follicles (PMF) in mouse ovaries from damage induced by cyclophosphamide (Item No.
13849) with 65% to 86% PMF survival compared to 46% PMF survival with a saline control.
3 Formulations containing cetrorelix have been used to prevent ovulation during
in vitro fertilization.
