Gynecological uses of GnRH antagonists: review article

Daniel Ernesto Carvallo Ruiz, Elizabeth Natalia Martínez Núñez, José Núñez-Troconis
In: Obstetrics & Gynecology International Journal · 2022 · vol. 13(4) , pp. 226–238 · doi:10.15406/ogij.2022.13.00654 · W4312477283
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⚙ AI-generated summary by claude@2026-06, 2026-06-06 ⓘ

GnRH antagonists rapidly suppress hormones without a flare-up, proving effective for endometriosis, uterine fibroids, and other gynecological conditions, with quick recovery of gonadal function.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-06 ⓘ

This 2022 narrative review examines the pharmacology and gynecologic uses of gonadotropin-releasing hormone (GnRH) antagonists, including agents such as elagolix, relugolix, cetrorelix, and linzagolix, focusing on how rapid, dose-dependent suppression of the hypothalamic-pituitary-gonadal (HPG) axis occurs without the flare effect seen with GnRH agonists. The authors synthesize evidence from English and Spanish literature published mainly from 2015–2022 to summarize reported effects on conditions including endometriosis, adenomyosis, non-menstrual pelvic pain, uterine fibroids, female infertility, and precocious puberty, emphasizing immediate therapeutic effects and rapid cessation of hormonal suppression after treatment ends. A key limitation explicitly noted is the nature of the work as a review: it depends on literature selection criteria and does not present new experimental results, including reliance on recently published and “reliable” sources. Relevance to endometriosis: the review explicitly lists endometriosis among gynecologic pathologies treated with GnRH antagonists and states that these drugs can control non-menstrual pelvic pain.

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Abstract

Aim: to review and analyze the use of gonadotropin-releasing hormone (GnRH) antagonists in endometriosis, adenomyosis, non-menstrual pelvic pain, uterine fibroids, prostate cancer, female infertility, and precocious puberty. Methods: the information used to write this manuscript was obtained during a three-month period, between October and May 2022, from specialized literature, written in English and Spanish, related to the use and potential applications of GnRH antagonists in medicine, mainly published during the last five years, using journals found in the most relevant medical digital archives, including PubMed, SciELO, Google Scholar, Cochrane, and Elsevier. Among the keywords used for obtaining this updated information were gonadotropin-releasing hormone (GnRH) antagonists; GnRH receptors (GnRHR); elagolix; relugolix; cetrorelix; linzagolix; hypothalamic-pituitary-gonadal (HPG) axis; endometriosis; adenomyosis; pelvic pain; uterine fibroids; leiomyomas; infertility; precocious puberty; PP; and central PP. Results: GnRH antagonists induce a rapid onset of clinical effects, without the flare-up effect that is seen with agonists, and have immediate therapeutic effects; once treatment concludes, hormonal suppression rapidly ceases, with normalization of gonadal function within a few days, guaranteeing an increase of GnRH concentration, controlling non-menstrual pelvic pain and heavy menstrual bleeding, and serving as part of the treatment of infertility and precocious puberty. Conclusion: even though the aforementioned gynecological pathologies can be treated with the use of multiple drugs, GnRH antagonists have shown to be potential first lines of treatment, as long as their administration protocols are followed correctly.

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Condition tags

endometriosisadenomyosisinfertility

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