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
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.


CONCLUSIONS
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.
Mezo
Gábor
G
Eötvös Loránd University, Hungarian Academy of Sciences, Research Group of Peptide Chemistry, Budapest, Pázmány P. stny. 1/A, Hungary. gmezo@elte.hu
Manea
Marilena
M
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D015195:Drug Design; D004715:Endometriosis / Q000188:drug therapy / Q000503:physiopathology; D005260:Female; D005307:Fertilization in Vitro / Q000379:methods*; D007987:Gonadotropin-Releasing Hormone / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008297:Male; D009369:Neoplasms / Q000188:drug therapy* / Q000503:physiopathology; D010330:Patents as Topic; D011470:Prostatic Hyperplasia / Q000188:drug therapy / Q000503:physiopathology
D000970:Antineoplastic Agents; D007987:Gonadotropin-Releasing Hormone