Gonadotropin-releasing hormone antagonists have been widely used to prevent premature luteinizing hormone rises and surges in patients undergoing ovarian stimulation for assisted reproduction. The development of effective and approved oral non-peptide gonadotropin-releasing hormone antagonists allows using them as a therapy for endometriosis-associated pain syndrome and uterine leiomyoma. Applying the depot forms of agonists gonadotropin-releasing hormone during the first 2—3 weeks is noted as «flare-up» phase, which has a negative stimulating effect in estrogen-dependent diseases. On the contrary, gonadotropin antagonists cause immediate inhibition of gonadotropins secretion by competitive blocking of pituitary receptors, in this connection they may constitute an alternative therapy for these conditions. This article presents a review of current literature confirming the efficacy, safety and administration of the new oral agents of gonadotropin-releasing hormone receptor antagonists.