Will GNRH antagonists be worth the wait?

Abstract

Gonadotropin-releasing hormone (GnRH) is also known as luteinizing hormone-releasing hormone (LHRH), formerly luteinizing hormone releasing factor (LRF). Since this hormone regulates the secretion of both FSH and LH, we prefer to call it GnRH. GnRH antagonists, as the name implies, are a class of compounds that actively compete with GnRH for the GnRH receptor, thereby neutralizing the effects of GnRH by competitive receptor occupancy. In order to fully appreciate their potential clinical utility, it is first important to comprehend the critical role of GnRH in the regulation of the pituitary-gonadal axis and secondly to familiarize ourselves with the mechanisms of action of GnRH, GnRH agonists and GnRH antagonists.