New oral combined antagonist of the gonadotrope-releasing hormone in mixed gynecological pathology treatment: priority cohorts of patients. A review

А. Л. Тихомиров, В. В. Казенашев, M. V. Maminova
In: Gynecology · 2026 · vol. 28(3) , pp. 199–207 · doi:10.26442/20795696.2026.3.203820 · W7214401179
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Abstract

The presented article describes the key aspects of uterine fibroids (UF) and endometriosis, the most common benign hyperplastic processes in the female reproductive system, pathogenesis from the perspective of current research trends in this medical theme. The review of literature published over the past 10 years aims to update and systematize information on risk factors and molecular mechanisms of these diseases. The article covers the influence of genetics, epigenetics, hormonal stimulation, lifestyle, parity, microbiome, immune system, and ferroptosis on their development. Hormonal stimulation is one of the key links in the pathogenesis of UF and endometriosis. This is why the ability to medically suppress hormonal effects on tissues has long been the main conservative treatment for these benign gynecological hyperplasias worldwide. Hormonal modulation is the mechanism of action of a new combination drug containing the gonadotrope-releasing hormone (GnRH) antagonist relugolix 40 mg, as well as estradiol 1 mg and norethisterone acetate 0.5 mg. Long-term and high-quality suppression of sex steroid secretion due to the blocking of the hypothalamic-pituitary-ovarian axis without pronounced side effects caused by hypoestrogeniа allows us to consider it as a promising drug in the treatment of UF, endometriosis, as well as their combination. The new combined oral GnRH antagonist is capable of relieving two main symptoms that affect the life quality of patients suffering from these conditions: abnormal uterine bleeding associated with leiomyoma and chronic pelvic pain – a common companion of endometriosis. To date, published studies have demonstrated the high clinical efficacy and favorable safety profile of using a prolonged regimen of the drug for up to 104 weeks (2 years). The effects of the drug on the size of uterine fibroids and endometrioid heterotopias during long-term use are still under investigation. The practice-oriented part of the material describes the patient cohorts that are most promising in terms of the use of a new oral GnRH antagonist. This information may be useful to obstetricians and gynecologists when choosing the most optimal treatment strategy for each individual patient.

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