Luteinizing hormone-releasing hormone antagonists

Background: Luteinizing hormone-releasing hormone (LH-RH) plays a central role in the vertebrate reproduction by regulating gonadal activity. Based on its binding to pituitary LH-RH receptors, as well as to LH-RH receptors expressed on cancer cells, LH-RH agonists and antagonists have been developed for different therapeutic applications. Objective/method: Here we give an overview of the most relevant LH-RH antagonists and their therapeutic applications. Recently patented compounds as well as drug formulations and dosage are presented. Conclusion: LH-RH antagonists have found clinical applications in in vitro fertilization, benign prostatic hyperplasia, endometriosis and in the treatment of hormone-dependent tumors. Work in progress is focused on further development of both peptidic and orally active non-peptidic LH-RH antagonists.