Neue Behandlungsoptionen mit GnRH-Antagonisten bei Endometriose und Uterus myomatosus

In: Gynäkologische Endokrinologie · 2020 · vol. 18(3) , pp. 169–174 · doi:10.1007/s10304-020-00329-8 · W3048094355
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GnRH antagonists are presented as new treatment options for endometriosis and uterine myomas.

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Küpker and colleagues review new treatment options using GnRH antagonists for endometriosis and uterine myomatosis, drawing on prior developments in GnRH antagonist pharmacology and clinical experience with agents such as cetrorelix, as well as orally available antagonists like elagolix and relugolix. Across the cited literature, the article reports preserved or targeted pituitary suppression/ovarian effects in assisted reproduction settings and summarizes evidence for endometriosis-associated pain outcomes with elagolix, while also covering randomized trial data for relugolix and comparisons to leuprorelin in uterine fibroids. The main limitation is that it is not an original clinical trial but a narrative overview, with conclusions dependent on heterogeneity and scope of the included studies. This paper is centrally about endometriosis — it focuses on GnRH antagonists as emerging treatments for endometriosis and related gynecologic conditions.

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Bioorg Med Chem Lett 12(16):2179–2183 Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS (2008) Discovery of sodium R‑(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluortrifluoromethyl]benzyl)-4-methyl‑2,6‑dioxo‑3,6‑dihydro-2H-pyrimidin-1-yl]-1phenylethylamino}butyrate(elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem 51(23):7478–7485 Taylor HS, Giudice LC, Lessey BA, Abrao MS, Kotarski J, Archer DF, Diamond MP, Surrey E, Johnson NP, Watts NB, Gallagher JC, Simon JA, Carr BR, Dmowski WP, Leyland N, Rowan JP, Duan WR, Ng J, Schwefel B, Thomas JW, Jain RI, Chwalisz K (2017) Treatment of endometriosis-associated pain with Elagolix, an oral GnRH antagonist. N Engl J Med 377(1):28–40 Taylor HS (2018) Use of Elagolix in Gynaecology. J Obstet Gynaecol Can 40(7):931–934 Shebley M, Polepally A, Nader A, Ng JW, Winzenborg I, Klein CE, Noerteraheuser P, Gibbs MA, Mostafa NM (2020) Clinical pharmacology of elagolix: an oral gonadotropin-releasing hormone receptor antagonist for endometriosis. Clin Pharmakinetics 59:297–309 Lamb YN (2018) Elagolix: first global approval. Drugs 78(14):1501–1508 Osuga Y, Enya K, Kudou K, Tanimoto M, Hoshiai H (2019) Oral gonadotropin-releasinghormone antagonist relugolix compared with Leuprorelin injections for uterine leiomyomas: a randomized controlled trial. Obstet Gynecol 133(3):423–433 Osuga Y, Enya K, Kudou K, Hoshiai H (2019) Relugolix, a novel oral gonadotropin-releasing hormone antagonist, in the treatment of pain symptoms associated with uterine fibroids: a randomized, placebo-controlled, phase 3 study in Japanese women. Fertil Steril 112(5):922–929.e2 Pohl O, Marchand L, Bell D, Gotteland JP (2020) Effects of combined GnRH receptor antagonist Lingagolix and hormonal add-back therapy on vaginal bleeding-delayed add-back onset does not improve bleeding pattern. Reprod Sci 27(4):988–995 Shore ND, Saad F, Cookson MS et al (2020) Oral Relugolix for androgen-deprivation therapy in advanced prostate cancer. N Engl J Med 382(23):2187–2196 Author information Authors and Affiliations Corresponding author Ethics declarations Interessenkonflikt W. Küpker, D. Plathow, J. Bullerdiek und R. Felberbaum geben an, dass kein Interessenkonflikt besteht. Für diesen Beitrag wurden von den Autoren keine Studien an Menschen oder Tieren durchgeführt. Für die aufgeführten Studien gelten die jeweils dort angegebenen ethischen Richtlinien. Additional information Redaktion B. Imthurn, Zürich O. Ortmann, Regensburg C. Tempfer, Herne Teile dieses Beitrags wurden bereits publiziert in Küpker, W., Felberbaum, R. Neue Behandlungsmöglichkeiten der Endometriose mit GnRH-Antagonisten. Gynäkologe (2020). https://doi.org/10.1007/s00129-020-04633-z Rights and permissions About this article Cite this article Küpker, W., Plathow, D., Bullerdiek, J. et al. Neue Behandlungsoptionen mit GnRH-Antagonisten bei Endometriose und Uterus myomatosus. Gynäkologische Endokrinologie 18, 169–174 (2020). https://doi.org/10.1007/s10304-020-00329-8 Published: Version of record: Issue date: DOI: https://doi.org/10.1007/s10304-020-00329-8

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