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Clinical evaluation of the oral gonadotropin-releasing hormone-antagonist elagolix for the management of endometriosis-associated pain

Pain Manag. 2019 Sep;9(5):497-515. doi: 10.2217/pmt-2019-0010. Epub 2019 Aug 22.

Abstract

Endometriosis is an estrogen-dependent chronic inflammatory disease associated with pelvic pain symptoms that are often severe, mainly dysmenorrhea, nonmenstrual pelvic pain and dyspareunia. This condition is also associated with peripheral and central sensitization. The current medical treatment options for endometriosis-associated pain are limited. Recently, the US FDA approved the novel, oral, nonpeptide gonadotropin-releasing hormone antagonist elagolix for the management of moderate to severe endometriosis-associated pain. Elagolix produces dose-dependent estrogen suppression, from partial suppression at lower doses to nearly full suppression at higher doses. This review article summarizes the current understanding of the pathophysiology of endometriosis, with a focus on the role of estrogen and the mechanisms of pain symptoms, and reviews the clinical development of elagolix in women with endometriosis-associated pain.

Keywords: GnRH antagonist; chronic pelvic pain; dysmenorrhea; dyspareunia; elagolix; endometriosis; endometriosis-associated chronic pain; estradiol; estrogen suppression; nonmenstrual pelvic pain.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Clinical Trials as Topic
  • Endometriosis / complications
  • Endometriosis / physiopathology*
  • Estrogen Antagonists / therapeutic use*
  • Female
  • Gonadotropin-Releasing Hormone / antagonists & inhibitors*
  • Humans
  • Hydrocarbons, Fluorinated / therapeutic use*
  • Pain / complications
  • Pain / drug therapy*
  • Pain / physiopathology*
  • Pain Management / methods*
  • Pyrimidines / therapeutic use*
  • Treatment Outcome

Substances

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