Fezolinetant

Other Therapeutics/Non-therapeutics · NK3 receptor antagonist

Indications

Treatment of moderate to severe vasomotor symptoms due to menopause.

Dosage

Adults: 45 mg once daily orally. Children: Not recommended.

Adverse Effects

Abdominal pain, diarrhoea, insomnia, back pain and hot flush.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: ALT or AST =2 x ULN or total bilirubin =2 x ULN. Known cirrhosis. Severe renal impairment or end-stage renal disease. Severe chronic hepatic impairment. Precautions: Perform baseline hepatic lab tests to evaluate for hepatic function and injury before starting treatment and follow-up tests monthly for the first 3 months, at 6 months, and 9 months after starting treatment. Mild or moderate hepatic impairment.

Interactions

Strong CYP1A2 inhibitors (e.g. Fluvoxamine). Moderate/weak CYP1A2 inhibitors (e.g. Mexiletine, Ciprofloxacin, Cimetidine).

Advice to Patient

Take with or without meals. Swallow whole tab with liquid. Do not cut, crush or chew tablet. Discontinue treatment and report urgently if you experience signs or symptoms of liver injury such as new onset fatigue, decreased appetite, nausea, vomiting, pruritus, jaundice, pale faeces, dark urine, or abdominal pain. Females of reproductive potential must use effective non-hormonal contraception during treatment. Avoid tobacco smoking.

Pharmacokinetics

Absorption: Rapid. Metabolism: Hepatic. Half-life elimination: 9.6 hrs. Time to peak, plasma: 1-4 hrs. Excretion: Urine (76.9%). Faeces (14.7%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.