Elagolix, a Novel, Orally Bioavailable GnRH Antagonist under Investigation for the Treatment of Endometriosis-Related Pain
Open Access
- 1 January 2015
- journal article
- review article
- Published by SAGE Publications in Women's Health
- Vol. 11 (1), 19-28
- https://doi.org/10.2217/whe.14.68
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.Keywords
This publication has 64 references indexed in Scilit:
- Aromatase inhibitors for the treatment of endometriosisFertility and Sterility, 2012
- Endometriosis and infertility: a committee opinionFertility and Sterility, 2012
- Impact of endometriosis on quality of life and work productivity: a multicenter study across ten countriesFertility and Sterility, 2011
- EndometriosisThe New England Journal of Medicine, 2010
- Discovery of 6-({4-[2-(4-tert-Butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): An Orally Active Antagonist of the Gonadotropin Releasing Hormone Receptor (GnRH-R)Journal of Medicinal Chemistry, 2009
- Suppression of Gonadotropins and Estradiol in Premenopausal Women by Oral Administration of the Nonpeptide Gonadotropin-Releasing Hormone Antagonist ElagolixJournal of Clinical Endocrinology & Metabolism, 2009
- Return of Chronic Pelvic Pain From Endometriosis After Raloxifene TreatmentObstetrics & Gynecology, 2008
- Discovery of a Novel, Orally Active, Small Molecule Gonadotropin-Releasing Hormone (GnRH) Receptor AntagonistJournal of Medicinal Chemistry, 2006
- Nonpeptide Luteinizing Hormone-Releasing Hormone Antagonists Derived from Erythromycin A: Design, Synthesis, and Biological Activity of Cladinose Replacement AnaloguesJournal of Medicinal Chemistry, 2004
- Discovery of a Novel, Potent, and Orally Active Nonpeptide Antagonist of the Human Luteinizing Hormone-Releasing Hormone (LHRH) ReceptorJournal of Medicinal Chemistry, 1998