Fezolinetant: A Non-hormonal NK3R Antagonist for the Treatment of Hot Flushes and Vasomotor Symptoms

Abstract

Background

Menopausal vasomotor symptoms (VMS), such as hot flashes (also known as night sweats), are experienced by 70% of women. These symptoms may be debilitating and last for many years. For 10%–20% of women, these symptoms are almost unbearable. Several pharmacotherapeutic approaches have been evaluated, and more are continually being developed. Although hormone therapy (HT) is often considered the most effective treatment, it is frequently accompanied by significant adverse effects. Consequently, there is a concerted effort to explore non-hormonal alternatives.

Objectives

The present study aims to provide a comprehensive overview of the key milestones and development trajectory of Fezolinetant from the preclinical stages to its FDA approval for the treatment of VMS.

Method

Fezolinetant's development trajectory was undertaken, employing a multifaceted information retrieval strategy. This approach leveraged scientific databases like PubMed, Google Scholar, and ScienceDirect, alongside authoritative resources including DrugBank and clinicaltrials.gov. Additionally, peer-reviewed journals and the official website of Astellas Pharma were meticulously examined to find the relevant information. The present study delves into various stages of Fezolinetant's development, including its medicinal chemistry, synthesis, mechanism of action, and pharmacodynamic and pharmacokinetic studies, as well as clinical data, and safety profiles.

Result

On May 12, 2023, the FDA approved Fezolinetant, a non-hormonal, selective neurokinin 3 (NK3) receptor antagonist, for treating mild to severe VMS marked on by menopause. It has been developed by Astellas Pharma under the brand name Veozah and is taken orally once a day, with or without meals, at a dose of 45 mg.

Conclusion

Fezolinetant represents a promising non-hormonal treatment option for women experiencing VMS. The key findings from the studies include the effectiveness of Fezolinetant in alleviating VMS symptoms and its favorable safety profile compared to hormonal therapy.