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Published in: Drugs 12/2023

18-07-2023 | AdisInsight Report

Fezolinetant: First Approval

Author: Arnold Lee

Published in: Drugs | Issue 12/2023

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Abstract

Fezolinetant (VEOZAH™) is an oral, small molecule, neurokinin 3 receptor (NK3R) antagonist, which is being developed by Astellas Pharma Inc. for the treatment of moderate to severe vasomotor symptoms (VMS) or hot flashes due to menopause. Inhibiting NK3R-mediated signalling in the central nervous system is a non-hormonal strategy to modulate the activity of neurones that are associated with thermoregulation, thereby reducing the frequency and severity of VMS. Fezolinetant received its first approval in the USA in May 2023 for the treatment of moderate to severe VMS due to menopause. This article summarizes the milestones in the development of fezolinetant leading to this first approval in this indication.
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Literature
1.
2.
go back to reference Depypere H, Lademacher C, Siddiqui E, et al. Fezolinetant in the treatment of vasomotor symptoms associated with menopause. Expert Opin Investig Drugs. 2021;30(7):681–94.CrossRefPubMed Depypere H, Lademacher C, Siddiqui E, et al. Fezolinetant in the treatment of vasomotor symptoms associated with menopause. Expert Opin Investig Drugs. 2021;30(7):681–94.CrossRefPubMed
3.
go back to reference Skorupskaite K, Anderson RA. Hypothalamic neurokinin signalling and its application in reproductive medicine. Pharmacol Ther. 2022;230(107960):1–11. Skorupskaite K, Anderson RA. Hypothalamic neurokinin signalling and its application in reproductive medicine. Pharmacol Ther. 2022;230(107960):1–11.
8.
go back to reference Tahara A, Takamatsu H, Ohtake A, et al. Effects of neurokinin 3 receptor antagonist fezolinetant on hot flash-like symptoms in ovariectomized rats. Eur J Pharmacol. 2021;905(174207):1–9. Tahara A, Takamatsu H, Ohtake A, et al. Effects of neurokinin 3 receptor antagonist fezolinetant on hot flash-like symptoms in ovariectomized rats. Eur J Pharmacol. 2021;905(174207):1–9.
9.
go back to reference Lederman S, Ottery FD, Cano A, et al. Fezolinetant for treatment of moderate-to-severe vasomotor symptoms associated with menopause (SKYLIGHT 1): a phase 3 randomised controlled study. Lancet. 2023;401(10382):1091–102.CrossRefPubMed Lederman S, Ottery FD, Cano A, et al. Fezolinetant for treatment of moderate-to-severe vasomotor symptoms associated with menopause (SKYLIGHT 1): a phase 3 randomised controlled study. Lancet. 2023;401(10382):1091–102.CrossRefPubMed
10.
go back to reference Johnson KA, Martin N, Nappi RE, et al. Efficacy and safety of fezolinetant in moderate-to-severe vasomotor symptoms associated with menopause: a phase 3 RCT. J Clin Endocrinol Metab. 2023;108(8):1981–97.CrossRefPubMedPubMedCentral Johnson KA, Martin N, Nappi RE, et al. Efficacy and safety of fezolinetant in moderate-to-severe vasomotor symptoms associated with menopause: a phase 3 RCT. J Clin Endocrinol Metab. 2023;108(8):1981–97.CrossRefPubMedPubMedCentral
11.
go back to reference Astellas Pharma Inc. Astellas announces topline 12-week results from phase 3 study of fezolinetant for the nonhormonal treatment of vasomotor symptoms in women in Asia [media release]. 14 Mar 2022. http://www.astellas.com. Astellas Pharma Inc. Astellas announces topline 12-week results from phase 3 study of fezolinetant for the nonhormonal treatment of vasomotor symptoms in women in Asia [media release]. 14 Mar 2022. http://​www.​astellas.​com.
13.
go back to reference Fraser GL, Lederman S, Waldbaum A, et al. A phase 2b, randomized, placebo-controlled, double-blind, dose-ranging study of the neurokinin 3 receptor antagonist fezolinetant for vasomotor symptoms associated with menopause. Menopause. 2020;27(4):382–92.CrossRefPubMedPubMedCentral Fraser GL, Lederman S, Waldbaum A, et al. A phase 2b, randomized, placebo-controlled, double-blind, dose-ranging study of the neurokinin 3 receptor antagonist fezolinetant for vasomotor symptoms associated with menopause. Menopause. 2020;27(4):382–92.CrossRefPubMedPubMedCentral
14.
go back to reference Depypere H, Timmerman D, Donders G, et al. Treatment of menopausal vasomotor symptoms with fezolinetant, a neurokinin 3 receptor antagonist: a phase 2a trial. J Clin Endocrinol Metab. 2019;104(12):5893–905.CrossRefPubMed Depypere H, Timmerman D, Donders G, et al. Treatment of menopausal vasomotor symptoms with fezolinetant, a neurokinin 3 receptor antagonist: a phase 2a trial. J Clin Endocrinol Metab. 2019;104(12):5893–905.CrossRefPubMed
15.
go back to reference Neal-Perry G, Cano A, Lederman S, et al. Safety of fezolinetant for vasomotor symptoms associated with menopause: a randomized controlled trial. Obstet Gynecol. 2023;141(4):737–47.CrossRefPubMedPubMedCentral Neal-Perry G, Cano A, Lederman S, et al. Safety of fezolinetant for vasomotor symptoms associated with menopause: a randomized controlled trial. Obstet Gynecol. 2023;141(4):737–47.CrossRefPubMedPubMedCentral
Metadata
Title
Fezolinetant: First Approval
Author
Arnold Lee
Publication date
18-07-2023
Publisher
Springer International Publishing
Published in
Drugs / Issue 12/2023
Print ISSN: 0012-6667
Electronic ISSN: 1179-1950
DOI
https://doi.org/10.1007/s40265-023-01917-1

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