Fezolinetant

VEOZAH is a neurokinin 3 (NK3) receptor antagonist that blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDy) neuron to modulate neuronal activity in the thermoregulatory center. Fezolinetant has high affinity for the NK3 receptor (Ki value of 19.9 to 22.1 nmol/L), which is more than 450-fold higher than binding affinity to NK1 or NK2 receptors.

• VEOZAH ® is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause. VEOZAH is a neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.ICD-10: N95.1

• VEOZAH is contraindicated in women with any of the following conditions: • Known cirrhosis [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.7 ), and Clinical Pharmacology ( 12.3 )] . • Severe renal impairment or end-stage renal disease [see Use in Specific Populations ( 8.6 ) and Clinical Pharmacology ( 12.3 )] .contraindicated

One 45 mg tablet orally once daily with or without food. Perform baseline hepatic laboratory tests to evaluate for hepatic function and injury before beginning VEOZAH. While using VEOZAH, perform follow-up hepatic laboratory tests monthly for the first 3 months, at 6 months, and 9 months after initiation of therapy or when signs or symptoms suggest liver injury. ( 2.1 ) 2.1 Recommended Dosage Take a single 45 mg VEOZAH tablet orally once daily with or without food. Take VEOZAH with liquids and swallow whole. Do not cut, crush, or chew tablets. Administer VEOZAH orally at about the same time each day. If a dose of VEOZAH is missed or not taken at the usual time, administer the missed dose as soon as possible, unless there is less than 12 hours before the next scheduled dose. Return to the regular schedule the following day. Perform baseline hepatic laboratory tests to evaluate for hepatic function and injury [including serum alanine aminotransferase (ALT), serum aspartate aminotransferase (AST), serum alkaline phosphatase (ALP), and serum bilirubin (total and direct)] before initiating treatment with VEOZAH. Do not start VEOZAH if ALT or AST is ≥ 2 x ULN or if the total bilirubin is ≥ 2 x ULN for the evaluating laboratory. While using VEOZAH, perform follow-up hepatic laboratory tests monthly for the first 3 months, at 6 months, and 9 months after initiation of therapy.

Hepatotoxicity: Cases of hepatotoxicity and jaundice have been reported in the postmarketing setting. Perform hepatic laboratory tests prior to initiation of VEOZAH to evaluate for hepatic function and injury. Perform follow-up hepatic laboratory tests monthly for the first 3 months, at 6 months, and 9 months after initiation of therapy. Advise patients to discontinue VEOZAH immediately and seek medical attention including hepatic laboratory tests if they experience signs or symptoms that may suggest liver injury (new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, or abdominal pain). ( 5.1 ) 5.1 Hepatotoxicity In three clinical trials, elevations in serum transaminase [alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST)] levels > 3 x the upper limit of normal (ULN) occurred in 2.3% [exposure adjusted incidence rate (EAIR) of 2.7 per 100 person-years] of women receiving VEOZAH and 0.9% (EAIR of 1.5 per 100 person-years) of women receiving placebo. No elevations in serum total bilirubin (> 2 x ULN) occurred. Women with ALT or AST elevations were generally asymptomatic. Transaminase levels returned to pretreatment levels (or close to these) without sequelae with dose continuation, and upon dose interruption, or discontinuation. Women with cirrhosis were not studied [see Adverse Reactions ( 6.1 )] . In the postmarketing setting, cases of drug-induced liver injury with elevations of ALT, AST, alkaline phosphatase (ALP), and total bilirubin occurred within 40 days of starting VEOZAH.

The following serious adverse reactions are discussed elsewhere in the labeling: • Hepatic Transaminase Elevation and Hepatotoxicity [see Warnings and Precautions ( 5.1 )] . The most common adverse reactions with VEOZAH [at least 2% in VEOZAH 45 mg and greater than placebo] are: abdominal pain, diarrhea, insomnia, back pain, hot flush, and hepatic transaminase elevation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Astellas Pharma US, Inc. at 1-800-727-7003 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The safety of VEOZAH was evaluated in three 52-week clinical trials [see Clinical Studies ( 14 )] . Across the three clinical trials, a total of 1100 women received VEOZAH. Trials 1 and 2 were placebo-controlled for the first 12 weeks, followed by re-randomization of women previously receiving placebo to VEOZAH (women on VEOZAH remained on VEOZAH) for an additional 40 weeks of uncontrolled treatment. Trial 3 was a randomized, placebo-controlled, double-blind safety study evaluating the safety of VEOZAH for 52 weeks. The adverse reactions reported in at least 2% in VEOZAH 45 mg and greater than placebo in Trial 3 are presented in Table 1 .

8.1 Pregnancy Risk Summary There are no data on VEOZAH use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In embryo-fetal toxicity animal studies with fezolinetant, embryo-lethality occurred at high doses above the human therapeutic dose in rats and rabbits, but no teratogenicity was observed. In the pre- and post-natal development animal study, delayed parturition and embryo-lethality occurred at high doses above the human therapeutic dose in rats. Additionally, in the male offspring delayed male reproductive maturation was observed, characterized by incomplete preputial separation, which affected male fertility at doses above the human therapeutic dose in rats [see Data ] . In the U.S. general population, the estimated background risk of major birth defects or miscarriage in clinically recognized pregnancies are 2-4% and 15-20%, respectively. Data Animal Data In embryo-fetal development toxicity studies in rats and rabbits, embryo-lethality was noted at the highest doses (128- and 174-fold the human AUC 24 at the human therapeutic dose for rats and rabbits, respectively).

Metabolism

In healthy women, fezolinetant C max and AUC increased proportionally over a dosage range from 20 to 60 mg once daily (0.44 to 1.33 times the approved recommended dosage). Steady-state plasma concentrations of fezolinetant were reached after two once daily doses, with minimal fezolinetant accumulation.

Treatment of overdose consists of discontinuation of VEOZAH therapy with institution of appropriate symptomatic care.

• May 12, 2023NDANDA216578Astellas

1. 1Drug Ineffective22912%
2. 2Alanine Aminotransferase Increased1839.4%
3. 3Hepatic Enzyme Increased1728.9%
4. 4Aspartate Aminotransferase Increased1407.2%
5. 5Off Label Use1125.8%
6. 6Headache1105.7%
7. 7Hot Flush965.0%
8. 8Nausea954.9%
9. 9Insomnia874.5%
10. 10Liver Function Test Increased844.3%
11. 11Diarrhoea763.9%
12. 12Fatigue683.5%
13. 13Abdominal Pain623.2%
14. 14Dizziness623.2%
15. 15Abdominal Pain Upper442.3%

The 10 most recently updated of 29 ClinicalTrials.gov registrations naming Fezolinetant as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study Following Women in Menopause Treated With a Non-hormonal Therapy for Hot Flashes and Night Sweats
  Completed · Observational · 999 enrolled · Astellas Pharma Global Development, Inc.
  NCT06049797updated 2026-06-05
• FLASH-Breast: Evaluating the Efficacy of Fezolinetant in Reducing Vasomotor Symptoms in Women With Breast Cancer on Endocrine Therapy
  Recruiting · Phase 2 · Interventional · 92 enrolled · Yale University
  NCT06917313updated 2026-06-02
• Fezolinetant and Vascular Health and Brain Health
  Not yet recruiting · Phase 3 · Interventional · 220 enrolled · Rebecca Thurston
  NCT07606664updated 2026-05-26
• A Study in Canada to Follow Outcomes of Women in Menopause Treated With Fezolinetant for Hot Flashes, When Given in Clinical Practice
  Recruiting · Observational · 238 enrolled · Astellas Pharma Europe Ltd.
  NCT07602530updated 2026-05-22
• Fezolinetant for the Improvement of Vasomotor Symptoms in Breast Cancer Patients Taking Endocrine Therapy, VENT Trial
  Terminated · Phase 2 · Interventional · 9 enrolled · University of Michigan Rogel Cancer Center
  NCT06617455updated 2026-05-06
• A Trial on Fezolinetant for Vasomotor Symptoms in Men Receiving Androgen Deprivation Therapy (ADT)
  Not yet recruiting · Phase 2 · Interventional · 54 enrolled · Chinese University of Hong Kong
  NCT07568236updated 2026-05-05
• Focusing on the Menopausal Transition to Improve Mid-Life Women's Health
  Recruiting · Phase 2 · Phase 3 · Interventional · 200 enrolled · University of Colorado, Denver
  NCT06975111updated 2026-04-30
• A Study to Assess Long-term Safety of Fezolinetant Given to Japanese Women Going Through Menopause
  Completed · Phase 3 · Interventional · 277 enrolled · Astellas Pharma Inc
  NCT06206421updated 2026-04-08
• A Study to Confirm if Fezolinetant Helps Reduce Hot Flashes in Women With Breast Cancer Who Are Having Hormone Therapy
  Active not recruiting · Phase 3 · Interventional · 984 enrolled · Astellas Pharma Global Development, Inc.
  NCT06440967updated 2026-04-06
• A Study to Confirm if Fezolinetant Helps Reduce Hot Flashes in Chinese Women Going Through Menopause
  Completed · Phase 2 · Interventional · 150 enrolled · Astellas Pharma Global Development, Inc.
  NCT06812754updated 2026-03-19

Frequently asked questions

How does Fezolinetant work?

VEOZAH is a neurokinin 3 (NK3) receptor antagonist that blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDy) neuron to modulate neuronal activity in the thermoregulatory center. Fezolinetant has high affinity for the NK3 receptor (Ki value of 19.9 to 22.1 nmol/L), which is more than 450-fold higher than binding affinity to NK1 or NK2 receptors.

What is Fezolinetant used for?

According to FDA labeling, Fezolinetant carries indications including: VEOZAH ® is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause. VEOZAH is a neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Fezolinetant?

Fezolinetant is classified as Other gynecologicals, Neurokinin 3 Receptor Antagonist, Cytochrome P450 1A2 Inhibitors, Neurokinin 3 Receptor Antagonists.

What are the brand names for Fezolinetant?

Fezolinetant is marketed under brand names including Veozah.

What are the contraindications for Fezolinetant?

Fezolinetant labeling lists contraindications including: VEOZAH is contraindicated in women with any of the following conditions: • Known cirrhosis [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.7 ), and Clinical Pharmacology ( 12.3 )] . • Severe renal impairment or end-stage renal disease [see Use in Specific Populations ( 8.6 ) and Clinical Pharmacology ( 12.3 )] .. Always consult the full prescribing information and a clinician.