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: Mohammad Ezzati, Bruce R Carr
• Journal: Women's health (London, England) (Womens Health (Lond)) Vol. 11 Issue 1 Pg. 19-28 (Jan 2015) ISSN: 1745-5065 [Electronic] United States
• PMID: 25581052 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Hydrocarbons, Fluorinated
• Pyrimidines
• Gonadotropin-Releasing Hormone
• elagolix

Topics

• Drug Evaluation
• Endometriosis (complications, drug therapy)
• Female
• Gonadotropin-Releasing Hormone (antagonists & inhibitors)
• Humans
• Hydrocarbons, Fluorinated (therapeutic use)
• Pain (drug therapy, etiology)
• Pyrimidines (therapeutic use)