MedPath

Fezolinetant

Generic Name
Fezolinetant
Brand Names
Veozah, Veoza
Drug Type
Small Molecule
Chemical Formula
C16H15FN6OS
CAS Number
1629229-37-3
Unique Ingredient Identifier
83VNE45KXX

Overview

Vasomotor symptoms (VMS), more colloquially known as hot flashes or night sweats, are the most common symptoms, if not the cardinal symptoms, in women. With a median duration of 7.4 years, vasomotor symptoms are also the most common reasons why women seek treatments for menopausal issues. Although mostly considered a nuisance, vasomotor symptoms could potentially affect the quality of life, as women with 7 or more daily moderate to severe VMS reported a decline in sleep quality, concentration, sexual activity, energy, and concentration. Although the pathophysiology of VMS is not fully understood, unpredictable fluctuation of estrogen level is thought to be the main cause of VMS, as estrogen therapy has been one of the most effective treatments for VMS by relieving symptoms in as many as 95% of menopausal women. Women undergoing abrupt menopause due to oophorectomy also experienced more severe symptoms than those going through a gradual transition. Additionally, thermoregulatory dysfunction has been proposed as one of the three possible mechanisms for VMS in menopause. Estrogen is a potent neuromodulator, particularly in the hypothalamus, and has been shown to be involved as a negative regulator in generating Gonadotropin-releasing hormone (GnRH) pulse through the kisspeptin, neurokinin B, and dynorphin (KNDy) neurons. NK3, one of the receptors expressed in KNDy neurons, is activated by neurokinin B and can thus induce the release of GnRH. Lower estrogen levels during menopause will decrease the estrogen-mediated feedback loop and increase neurokinin B signalling, increasing the activity of KNDy neurons and therefore the activity of the temperature control center. By antagonizing NK3 receptors, neuronal signalling can be dampened to reduce VMS. Although hormone therapy is available for menopausal women, safety and tolerability concerns, such as an increased risk of stroke and venous thromboembolism or hormone-dependent cancer like breast cancer, can prevent some women from receiving this treatment. Fezolinetant, an NK3 receptor antagonist, was developed in response to this issue as well as more understanding of the role of NK3R in the hypothalamic-pituitary-gonadal (HPG) axis. Although previous NK3 receptor antagonists exist, such as osanetant and talnetant, only fezolinetant showed tangible effects on the HPC axis, potentially due to its favorable pharmacokinetics profile to cross the blood-brain barrier. Fezolinetant is approved by the FDA in May 2023 under the brand name VEOZAH.

Indication

Fezolinetant is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.

Associated Conditions

  • Moderate to Severe Vasomotor Symptoms

Research Report

Published: Aug 21, 2025

Fezolinetant (Veozah®): A Comprehensive Pharmacological and Clinical Monograph on the First-in-Class NK3 Receptor Antagonist for Vasomotor Symptoms

Introduction and Drug Profile

Overview of Fezolinetant as a First-in-Class Neurokinin-3 (NK3) Receptor Antagonist

Fezolinetant, marketed under the brand names Veozah and Veoza, represents a significant therapeutic innovation in the management of menopausal symptoms.[1] It is a first-in-class, orally administered, small-molecule, selective neurokinin-3 (NK3) receptor antagonist.[1] Its development and approval mark a paradigm shift away from traditional hormonal approaches, offering a novel, non-hormonal mechanism of action that directly targets the neurobiological underpinnings of vasomotor symptoms (VMS).[4]

The pathophysiology of VMS, colloquially known as hot flashes and night sweats, involves a complex interplay of neuroendocrine signals within the hypothalamus. Fezolinetant's mechanism is precisely targeted to this central pathway, offering a new therapeutic strategy for a condition that can persist for a median duration of 7.4 years and is the most common reason women seek medical treatment for menopausal issues.[5] Developed by Astellas Pharma following its acquisition from Ogeda, fezolinetant addresses a substantial unmet medical need for the large population of women who either have contraindications to hormone therapy (HT) or choose to avoid it due to safety and tolerability concerns, such as an increased risk of stroke, venous thromboembolism, or hormone-dependent cancers like breast cancer.[1] The U.S. Food and Drug Administration (FDA) has recognized its novelty by designating it a first-in-class medication.[1]

Approved Indication

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/07/22
Not Applicable
Not yet recruiting
2025/05/16
Phase 2
Not yet recruiting
2025/05/15
Phase 2
Not yet recruiting
2025/05/04
Phase 2
Not yet recruiting
Shehzad Basaria, M.D.
2025/04/08
Phase 2
Not yet recruiting
2025/02/06
Phase 2
Recruiting
2024/09/27
Phase 2
Recruiting
2024/06/04
Phase 3
Recruiting
2024/01/16
Phase 3
Recruiting
2024/01/16
Phase 3
Active, not recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Astellas Pharma US, Inc.
0469-2760
ORAL
45 mg in 1 1
5/19/2023
Astellas Pharma US, Inc.
0469-2460
ORAL
45 mg in 1 1
5/19/2023
Astellas Pharma US, Inc.
0469-2660
ORAL
45 mg in 1 1
5/19/2023

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
Authorised
12/7/2023

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
VEOZA™ FILM-COATED TABLETS 45 MG
SIN17196P
TABLET, FILM COATED
45.0mg
3/5/2025

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
VEOZA TABLETS 45MG
N/A
N/A
N/A
4/24/2025

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
VEOZA fezolinetant 45 mg film coated tablet blister pack
401401
Medicine
A
2/26/2024

Health Canada Drug Approvals

Approved Product
Company
DIN
Dosage Form
Strength
Market Date
VEOZAH
astellas pharma canada inc
02553600
Tablet - Oral
45 MG
3/11/2025

CIMA AEMPS Drug Approvals

Approved Product
Company
Registration Number
Pharmaceutical Form
Prescription Type
Status
VEOZA 45 MG COMPRIMIDOS RECUBIERTOS CON PELICULA
1231771001
COMPRIMIDO RECUBIERTO CON PELÍCULA
Medicamento Sujeto A Prescripción Médica
Commercialized

Philippines FDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product
Company
Registration Number
Dosage Form
Strength
Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name
MA Holder
MA Number
Pharmaceutical Form
Active Ingredient
Authorization Date
No UK EMC drug information found for this drug.

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