Elagolix in the treatment of heavy menstrual bleeding associated with uterine fibroids in premenopausal women

Expert Rev Clin Pharmacol. 2021 Apr;14(4):427-437. doi: 10.1080/17512433.2021.1900726. Epub 2021 Mar 15.

Abstract

Introduction: Uterine fibroids (UFs) are the most common benign tumor arising from myometrium of reproductive age women, with significant financial burden estimated in hundreds of billions of dollars. Unfortunately, there are limitations in available long-term treatment options. Thus, there is a large unmet need in the UF space for noninvasive therapeutics.

Areas covered: Authors reviewed the literature available for elagolix; an orally bioavailable, second-generation, non-peptide gonadotropin-releasing hormone (GnRH) antagonist recently approved by the US Food and Drug Administration (FDA) in combination with estradiol/norethindrone acetate for the management of heavy menstrual bleeding associated with UFs in premenopausal women.

Expert opinion: The utility of new-generation oral GnRH-antagonists, such as elagolix, relugolix and linzagolix, is offering a new potential opportunity for the future therapy of UFs: elagolix has been the most studied drug of this class for treating benign gynecological diseases, including endometriosis and UFs, for which it has been US FDA-approved in 2018 and 2020, respectively.

Keywords: Add-back Therapy; GnRH Antagonists; elagolix; heavy Menstrual Bleeding; leiomyoma; uterine Fibroids.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Combinations
  • Estradiol / administration & dosage
  • Female
  • Gonadotropin-Releasing Hormone / antagonists & inhibitors
  • Humans
  • Hydrocarbons, Fluorinated / administration & dosage*
  • Hydrocarbons, Fluorinated / pharmacology
  • Leiomyoma / complications
  • Leiomyoma / drug therapy
  • Menorrhagia / drug therapy*
  • Menorrhagia / etiology
  • Norethindrone / administration & dosage
  • Premenopause
  • Pyrimidines / administration & dosage*
  • Pyrimidines / pharmacology
  • Uterine Neoplasms / complications
  • Uterine Neoplasms / drug therapy

Substances

  • Drug Combinations
  • Hydrocarbons, Fluorinated
  • Pyrimidines
  • estradiol, norethindrone drug combination
  • Gonadotropin-Releasing Hormone
  • Estradiol
  • elagolix
  • Norethindrone