title: Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain.
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.
authors.affiliation: Division of Reproductive Endocrinology & Infertility, Department of Obstetrics & Gynecology, University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390, USA.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Ezzati
authors.forename: Bruce R
authors.initials: BR
authors.lastname: Carr
mesh_terms: D004341:Drug Evaluation; D004715:Endometriosis / Q000150:complications / Q000188:drug therapy*; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000627:therapeutic use*; D010146:Pain / Q000188:drug therapy* / Q000209:etiology; D011743:Pyrimidines / Q000627:therapeutic use*
chemical_list: D006845:Hydrocarbons, Fluorinated; D011743:Pyrimidines; D007987:Gonadotropin-Releasing Hormone; C539351:elagolix
keywords: GnRH antagonists; bone mineral density; elagolix; endometriosis; medical treatment