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Review
. 2025 Jan-Feb;21(2):105-113.
doi: 10.1080/17425255.2024.2416046. Epub 2024 Oct 16.

Pharmacokinetic evaluation of fezolinetant for the treatment of vasomotor symptoms caused by menopause

Laura Cucinella  1   2 , Sara Tedeschi  1 , Stefano Memoli  1 , Chiara Cassani  1   3 , Ellis Martini  2 , Rossella E Nappi  1   2
Affiliations
Review

Pharmacokinetic evaluation of fezolinetant for the treatment of vasomotor symptoms caused by menopause

Laura Cucinella et al. Expert Opin Drug Metab Toxicol. 2025 Jan-Feb.

Abstract

Introduction: Vasomotor symptoms (VMS) affect the majority of menopausal women, with possible negative impact on several domains of quality of life (QoL). Although menopausal hormone therapy (MHT) represents an effective treatment, the risk-benefit profile is not favorable for every woman. Non-hormonal options are limited in number and efficacy.

Areas covered: Fezolinetant is a novel oral non-hormonal drug recently approved for the treatment of moderate-severe VMS. It acts as an antagonist of neurokinin 3 receptor (NK3R), the main target of neurokinin B (a tachykinin over-expressed by kisspeptin/neurokinin B/dynorphin [KNDy] neurons after menopausal hypoestrogenism), involved in the modulation of the thermoregulatory hypothalamic center. Here, we report pharmacodynamics and pharmacokinetic properties of fezolinetant as well as its efficacy and safety data from available clinical trials.

Expert opinion: Fezolinetant has shown efficacy in reducing the frequency and severity of VMS with a positive impact on sleep- and health-related QoL and acceptable safety and tolerability profile. Given the limited availability of effective non-hormonal options for VMS, fezolinetant could potentially represent a game-changer for care of menopausal women, especially when relative or absolute contraindications to MHT use are present. Further studies to gain more information about the safety profile and potential extra-VMS benefits or disadvantages are warranted in real-life clinical practice.

Keywords: Climacteric syndrome; NK3R antagonists; fezolinetant; hot flashes; menopause; vasomotor symptoms.

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