Gonadotropin-releasing hormone antagonists in obstetriciangynecologist practice: mechanism of action, indications, efficacy, and safety

Abstract

Worldwide, increasing comorbidity among women has led to a rapid rise in the prevalence of hyperproliferative estrogendependent diseases of the reproductive system (endometriosis, adenomyosis, uterine fibroids, endometrial hyperplasia, and benign breast dysplasia). In addition, the detection of combined forms of hyperproliferative diseases is increasing, as systemic changes associated with comorbidity are not anatomically selective and require a scientifically grounded search for innovative therapeutic approaches. Until recently, therapeutic options for combined hyperproliferative diseases were limited primarily to gonadotropin-releasing hormone (GnRH) agonists, which have several specific nuances, individual pharmacokinetic properties, and certain limitations. Currently, the first mediation based on relugolix, an oral selective GnRH antagonist (40 mg), in combination with norethisterone acetate (0.5 mg) and estradiol hemihydrate (1 mg) has been registered in the Russian Federation. It demonstrates significant therapeutic potential for the treatment of combined hyperproliferative diseases. Key words: uterine fibroids, endometriosis, adenomyosis, gonadotropin-releasing hormone antagonists, relugolix, norethisterone acetate, estradiol hemihydrate