Gonadotropin-releasing hormone antagonist (linzagolix): a new therapy for uterine adenomyosis

Fertil Steril. 2020 Sep;114(3):640-645. doi: 10.1016/j.fertnstert.2020.04.017. Epub 2020 Jun 2.

Abstract

Objective: To compare the efficacy of a selective progesterone receptor modulator, ulipristal acetate, and a gonadotropin-releasing hormone antagonist, linzagolix, in a case of severe uterine adenomyosis.

Design: Case report.

Setting: Private clinic and infertility research unit.

Patient: One patient born in 1981 who presented because of heavy menstrual bleeding, pelvic pain, and dysmenorrhea due to diffuse and disseminated uterine adenomyosis confirmed by magnetic resonance imaging (MRI).

Intervention: The patient received a first treatment of 5 mg UPA daily for one course of 3 months. This therapy was discontinued because MRI revealed a worsened aspect. One year later, a once-daily dose of 200 mg linzagolix administered orally was initiated for 3 months, followed by another 3-month course of 100 mg once daily.

Main outcome measures: Clinical symptoms and MRI aspect.

Results: During treatment with UPA, the symptoms (pelvic pain, dysmenorrhea, bulk symptoms) worsened and MRI revealed aggravation of the adenomyotic lesions. During the 12-week course of once-daily 200 mg linzagolix, the patient remained in amenorrhea and noted a very significant improvement in symptoms. On MRI, the uterine volume had fallen from 875 cm3 to 290 cm3, and the adenomyotic lesions had significantly regressed. During the 100-mg linzagolix course (weeks 13-24), the patient reported continued alleviation of her symptoms.

Conclusion: To our knowledge, this is the first reported use of linzagolix, a new oral gonadotropin-releasing hormone antagonist that significantly reduced lesion size and improved quality of life in a patient with severe adenomyosis, who was previously nonresponsive to treatment with a selective progesterone receptor modulator, ulipristal acetate.

Keywords: GnRH antagonist; linzagolix; selective progesterone receptor modulator; uterine adenomyosis.

Publication types

  • Case Reports

MeSH terms

  • Adenomyosis / diagnostic imaging
  • Adenomyosis / drug therapy*
  • Adenomyosis / metabolism
  • Adult
  • Disease Progression
  • Drug Substitution
  • Female
  • Gonadotropin-Releasing Hormone / antagonists & inhibitors*
  • Gonadotropin-Releasing Hormone / metabolism
  • Hormone Antagonists / therapeutic use*
  • Humans
  • Magnetic Resonance Imaging
  • Norpregnadienes / therapeutic use*
  • Remission Induction
  • Severity of Illness Index
  • Treatment Failure
  • Uterus / diagnostic imaging
  • Uterus / drug effects*
  • Uterus / metabolism

Substances

  • Hormone Antagonists
  • Norpregnadienes
  • Gonadotropin-Releasing Hormone
  • ulipristal acetate