Gonadotropin-releasing hormone antagonists
Abstract
Hypothalamic gonadotropin-releasing hormone (GnRH) is a decapeptide that
stimulates pituitary synthesis and secretion of gonadotropins and,
therefore, gonadal hormones. GnRH antagonists, of which thousands have
been formulated, inhibit the hormone from binding to its receptor,
inducing a pharmacological hypophysectomy. Peptide derivations of GnRH and
non-peptide compounds are both in clinical trials or approved for assisted
reproduction. As these compounds reach the market, the use of antagonists
might expand to treatment of other hormonally dependent diseases, hormonal
male contraception and growth inhibition of extra-pituitary cancer cells
expressing GnRH receptors.