Gonadotropin-releasing-hormone-receptor antagonists

Pulsatile gonadotropin-releasing hormone (GnRH) stimulates the pituitary se cretion of both luteinising hormone (LH) and follicle-stimulating hormone ( FSH) and thus controls the hormonal and reproductive function of the gonads . Blockade of GnRH effects may be wanted for a variety of reasons-eg, to pr event untimely luteinisation during assisted reproduction or in the treatme nt of sex-hormone-dependent disorders. Selective blockade of LH/FSH secreti on and subsequent chemical castration have previously been achieved by dese nsitising the pituitary to continuously administered GnRH or by giving long -acting GnRH agonists. Only recently have GnRH-receptor antagonists, that i mmediately block GnRH's effects, been developed for clinical use with accep table pharmacokinetic, safety, and commercial profiles. In assisted reprodu ction, these compounds seem to be as effective as established therapy but w ith shorter treatment times, less use of gonadotropic hormones, improved pa tient acceptance, and fewer follicles and oocytes. All current indications for GnRH-agonist desensitisation may prove to be indications for a GnRH ant agonist, including endometriosis, leiomyoma, and breast cancer in women, be nign prostatic hypertrophy and prostatic carcinoma in men, and central prec ocious puberty in children. However, the best clinical evidence so far has been in assisted reproduction and prostate cancer.