Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain

Ezzati M, Mohammad Ezzati, Bruce R. Carr, Carr BR
Women's health (London, England) · 2015 · vol. 11(1) , pp. 19–28 · doi:10.2217/whe.14.68 · PMID:25581052 · W2029276653
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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

endometriosis

MeSH descriptors

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

Citation neighborhood (2-hop)

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. Outer rings show 2-hop neighbours — papers reached through the immediate citers/citees. [ collapse to 1-hop ]

References (76)

Cited by (27)

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