ABSTRACT
In 1971, Schally first achieved the isolation, elucidation of structure and synthesis of hypothalamic luteinizing hormone-releasing hormone (or gonadotropin-releasing hormone, GnRH)1-5. In the past 30 years, more than 3000 analogs of GnRH have been synthesized6-8. Agonistic analogs, such as triptorelin, leuprolide, goserelin and buserelin, which are superior to GnRH with respect to activity, are frequently used for the treatment of hormone-sensitive tumors as well as in reproductive medicine7-10. Potent peptidic antagonists of GnRH, such as cetrorelix, ganirelix and abarelix have become clinically available in recent years11,12. New peptidic and nonpeptidic antagonists such as teverelix, degarelix, D-63153, TAK-013 and NBI-42902 are currently being tested in various clinical studies.
