Elagolix, a Novel, Orally Bioavailable GnRH Antagonist under Investigation for the Treatment of Endometriosis-Related Pain

Mohammad Ezzati, Bruce R Carr
Women's health (London, England) · 2015 · vol. 11(1) , pp. 19–28 · doi:10.2217/whe.14.68 · PMID:25581052 · W2029276653
review OA: gold CC0 ⤵ 28 in-corpus citations
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⚙ AI-generated summary by claude@2026-06, 2026-06-07 ⓘ

Elagolix, an orally bioavailable nonpeptide GnRH antagonist, has shown safety and efficacy in partially and reversibly suppressing estrogen production and improving endometriosis-related pain in early clinical trials.

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Abstract

Suppression of estrogen production and reduction of menstrual blood flow are the mainstays of medical treatment of endometriosis-related pain and have been traditionally achieved by methods such as combined hormonal contraception, progestins and GnRH analogs, all with comparable efficacies, though different side-effect profiles. Elagolix is the frontrunner among an emerging class of GnRH antagonists, which unlike their peptide predecessors has a nonpeptide structure resulting in its oral bioavailability. Phase I and II clinical trials have demonstrated safety of elagolix and its efficacy in partial and reversible suppression of ovarian estrogen production resulting in improvements in endometriosis-related pain. Phase III clinical trials are currently underway and elagolix may become a valuable addition to the armamentarium of pharmacological agents to treat endometriosis-related pain.

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Condition tags

mesh:D004715endometriosis

MeSH descriptors

Endometriosis Gonadotropin-Releasing Hormone Hydrocarbons, Fluorinated Pain Pyrimidines Drug Evaluation Endometriosis Endometriosis Female Gonadotropin-Releasing Hormone Humans Hydrocarbons, Fluorinated Pain Pain Pyrimidines

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

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Cited by (28)

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