Luliberyn plays a pivotal role in the reproductive system. Its analogs have wide therapeutic applications ranging form the treatment of some human cancers, gynecological and sexually transmitted diseases to animal breeding. In the article, the development of luliberin agonists and antagonists and the principles of their application were briefly reviewed. Sequences of some important natural and synthetic analogs were presented. Carcinogenic and biodegradation resistable derivatives of luliberin analogs were also described.