Tachykinin NK3 receptor antagonist Treatment of menopausal-related vasomotor symptoms

G. D’Alessandro, F. Barra, G. Evangelisti, S. Ferrero

Research output: Contribution to journalArticlepeer-review

Abstract

Vasomotor symptoms (VMS) are common complaints in 80% of postmenopausal women, having a great impact on their global quality of life. Several therapeutic options are available for treating these patients. Hormonal replacement therapy is the current therapeutic standard for VMS, but it is associated with well-known potential risks. Fezolinetant (ESN-364) is an orally administered compound under development for use in the treatment of VMS associated with menopause. It selectively and reversibly blocks neurokinin B (NKB) signaling, leading to a relevant beneficial effect for the treatment of flushes. A phase II double-blind, placebo-controlled study showed that fezolinetant significantly decreases the severity of VMS, inducing a 93% reduction in their frequency from baseline to week 12 of treatment. Moreover, this drug is well tolerated and does not affect estradiol blood levels, supporting its potential use for patients with previous breast and endometrial cancers.

Original languageEnglish
Pages (from-to)537-546
Number of pages10
JournalDrugs of the Future
Volume45
Issue number8
DOIs
Publication statusPublished - Aug 2020

Keywords

  • ESN-364
  • Estradiol
  • Fezolinetant
  • Hot flushes
  • Neurokinin B
  • Vasomotor symptoms

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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