Oral Moderate to severe vasomotor symptoms associated with menopause
Adult: 45 mg once daily. Periodically assess the benefit of long-term therapy. Do not initiate treatment if the patient's ALT, AST and/or total bilirubin are ≥2 times the ULN. Discontinue treatment if ALT/AST is >5 times the ULN, or if ALT/AST is >3 times the ULN and either the total bilirubin is >2 times the ULN or signs of liver injury occur. Missed dose: Take the missed dose as soon as possible. If there is <12 hours prior to the next scheduled dose, skip the missed dose and return to the usual dosing schedule.
Renal Impairment
ESRD: Contraindicated.
eGFR (mL/min/1.73 m2)
Dosage
<30
Contraindicated.
Administration
Fezolinetant May be taken with or without food. Swallow whole & do not cut/crush/chew.
Contraindications
Known cirrhosis. Severe renal (eGFR <30 mL/min/1.73 m2) impairment, including ESRD. Known or suspected pregnancy. Concomitant use with moderate to strong CYP1A2 inhibitors.
Special Precautions
Patient with previous breast cancer or other estrogen-dependent malignancies; seizures or other convulsive disorders. Patients undergoing oncologic treatment for breast cancer or other estrogen-dependent malignancies. Mild to moderate renal impairment. Not recommended in moderate to severe hepatic impairment. Lactation.
Adverse Reactions
Significant: Hepatotoxicity, particularly increased serum ALT and AST (>3 times the ULN), increased alkaline phosphatase and total bilirubin, and serious drug-induced liver injury. Gastrointestinal disorders: Diarrhoea, abdominal pain. Musculoskeletal and connective tissue disorders: Back pain. Psychiatric disorders: Insomnia. Vascular disorders: Hot flush.
PO: Z (Generally contraindicated during pregnancy.)
Patient Counseling Information
Perimenopausal women of childbearing potential must use an effective non-hormonal birth control method during therapy.
Monitoring Parameters
Perform a complete personal and family medical history prior to starting therapy. Obtain LFTs before treatment initiation, monthly for the 1st 3 months, then at the 6th and 9th months of therapy. Monitor for signs and symptoms suggestive of liver injury.
Overdosage
Symptoms: Headache, nausea, and paraesthesia.
Management: Symptomatic and supportive treatment.
Drug Interactions
Significantly increased plasma concentration and exposure with moderate and strong CYP1A2 inhibitors (e.g. ethinylestradiol-containing contraceptives, mexiletine, enoxacin, fluvoxamine).
Action
Description: Overview: Fezolinetant is a non-hormonal neurokinin 3 (NK3) receptor antagonist. Mechanism of Action: Fezolinetant inhibits the binding of neurokinin B (NKB) on the kisspeptin/neurokinin B/dynorphin (KNDy) neuron to modulate the neuronal activity in the thermoregulatory centre of the hypothalamus. Pharmacodynamics: In post-menopausal women, fezolinetant treatment transiently decreased the luteinising hormone (LH) levels at peak concentrations. Additionally, it did not show any clear trends or clinically relevant changes in the measured sex hormones (FSH, testosterone, estrogen, dehydroepiandrosterone sulfate).
Based on the conducted model-based approach to assess the risk of QT prolongation, fezolinetant does not prolong the QT interval to any clinically relevant extent at therapeutic or supratherapeutic doses. Pharmacokinetics: Absorption: Time to peak plasma concentration: 1.5 hours (range: 1-4 hours). Distribution: Volume of distribution: 189 L. Plasma protein binding: 51%. Metabolism: Metabolised mainly by CYP1A2 and to a lesser extent by CYP2C9 and CYP2C19 into ES259564 (less potent major metabolite). Excretion: Via urine (76.9%; 1.1% as unchanged drug); faeces (14.7%; 0.1% as unchanged drug). Elimination half-life: 9.6 hours.
Chemical Structure
Fezolinetant Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 117604931. https://pubchem.ncbi.nlm.nih.gov/compound/Fezolinetant. Accessed Nov. 25, 2025.
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