Relugolix for the treatment of uterine fibroids

Expert Opin Pharmacother. 2020 Oct;21(14):1667-1674. doi: 10.1080/14656566.2020.1787988. Epub 2020 Jul 17.

Abstract

Introduction: Uterine fibroids (UF) are benign tumors common in premenopausal women, with strong impact on the health-care systems. For many years, surgery represented the only therapy for symptomatic fibroids. However, clinicians are observing a switch from surgery to noninvasive methods; in particular, medical treatment has been shown to be efficacious in obtaining a bleeding reduction and in ameliorating patient conditions.

Areas covered: The authors review the current options available for the treatment of women with UF, with a special focus on the newest one, relugolix. It is an orally active non-peptide Gonadotropin-releasing hormone (GnRH)-receptor antagonist recently licensed for women with symptomatic fibroids. Relugolix is a well-tolerated safe drug; it is effective in inducing a dose-dependent decrease in menstrual blood loss, with faster reduction of heavy menstrual bleeding (HMB) and a greater shrinkage in fibroid volume compared to the current standard of GnRH agonist treatment.

Expert opinion: Relugolix is a promising drug for the non-surgical treatment of women with UF. To date, the only published data come from a well-selected Japanese female population study while results from worldwide ongoing studies are ongoing in order to confirm the efficacy of this GnRH agonist receptor.

Keywords: Gonadotropin-release hormone receptor (GnRH) antagonist; medical therapy; relugolix; uterine fibroids.

Publication types

  • Review

MeSH terms

  • Female
  • Humans
  • Hysterectomy
  • Leiomyoma / drug therapy*
  • Leiomyoma / metabolism
  • Leiomyoma / surgery
  • Menstruation / drug effects
  • Phenylurea Compounds / administration & dosage
  • Phenylurea Compounds / adverse effects
  • Phenylurea Compounds / pharmacokinetics
  • Phenylurea Compounds / therapeutic use*
  • Premenopause / drug effects
  • Pyrimidinones / administration & dosage
  • Pyrimidinones / adverse effects
  • Pyrimidinones / pharmacokinetics
  • Pyrimidinones / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Receptors, LHRH / antagonists & inhibitors*
  • Treatment Outcome
  • Uterine Neoplasms / drug therapy*
  • Uterine Neoplasms / metabolism
  • Uterine Neoplasms / surgery

Substances

  • Phenylurea Compounds
  • Pyrimidinones
  • Receptors, LHRH
  • relugolix