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

Womens Health (Lond). 2015 Jan;11(1):19-28. doi: 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: GnRH antagonists; bone mineral density; elagolix; endometriosis; medical treatment.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

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

Substances

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