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
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
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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