Eliminating Hormones With Orally Active Gonadotropin-releasing Hormone Antagonists

Gonadotropin-releasing hormone (GnRH) analogues have been used in clinical practice for nearly 3 decades. Beginning with GnRH agonists, these agents have been used to treat hormone-dependent disease and to suppress gonadotropin production in assisted reproductive technologies. With the development of GnRH antagonists and especially small-molecule antagonists, our ability to achieve gonadotropin and sex steroid suppression has become increasingly effective and convenient. In this review, we will briefly describe the development of GnRH analogues, review the evolution of orally active small-molecule GnRH antagonists and provide an overview of the expanding role of small-molecule GnRH antagonists in clinical practice.