Cetrorelix Acetate (SB-075 acetate)

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-Trp⁶]GnRH (IC₅₀ = 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 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.

1.Beckers, T., Reil?nder, H., and Hilgard, P.Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assayAnal. Biochem.251(1)17-23(1997) 2.Yano, T., Pinski, J., Halmos, G., et al.Inhibition of growth of OV-1063 human epithelial ovarian cancer xenografts in nude mice by treatment with luteinizing hormone-releasing hormone antagonist SB-75Proc. Natl. Acad. Sci. USA91(15)7090-7094(1994) 3.Meirow, D., Assad, G., Dor, J., et al.The GnRH antagonist cetrorelix reduces cyclophosphamide-induced ovarian follicular destruction in miceHum. Reprod.19(6)1294-1299(2004)