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Cetrorelix


Mechanism of action:

Cetrorelix is a gonadotropin-releasing hormone (GnRH) antagonist. In the hypothalamic-pituitary-gonadal (HPG) axis, GnRH released from the hypothalamus binds to GnRH receptors in the anterior pituitary and stimulates the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These hormones in turn promote ovarian follicle maturation and ovulation. Cetrorelix competitively binds directly to pituitary GnRH receptors and immediately suppresses the secretion of LH and FSH.

Reference(s):

1. Volker P et al. (2002). Expression of receptors for luteinizing hormone-releasing hormone in human ovarian and endometrial cancers: frequency, autoregulation, and correlation with direct antiproliferative activity of luteinizing hormone-releasing hormone analogues. Am J Obstet Gynecol. 


2. Zapatero-Caballero H et al. (2003). Gonadotropin-releasing hormone receptor gene expression during pubertal development of male rats. Biol Reprod.

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