fezolinetant: clinical use

Prescribing considerations

• Confirm the diagnosis and review personal, family and complete medication histories.
• Avoid use in active or higher-risk liver disease and assess renal and hepatic function.
• Safety and efficacy are unknown during active treatment for breast or other oestrogen-dependent malignancy; previous malignancy requires individual benefit–risk assessment.
• Evidence is limited for patients starting treatment after age 65 and for those with a history of seizures.
• Periodically reassess whether continuing treatment remains beneficial.

Contraindications and cautions

• Hypersensitivity to fezolinetant or an excipient
• Concurrent moderate or strong CYP1A2 inhibitor use
• Known or suspected pregnancy

Monitoring

• Check ALT, AST, alkaline phosphatase and total and direct bilirubin before starting.
• Do not initiate when ALT or AST is at least twice the upper limit of normal, or total bilirubin is similarly elevated.
• Repeat liver-function tests monthly during the first three months and subsequently according to clinical judgement.
• Test promptly if symptoms suggest liver injury; stop according to product-defined biochemical or symptomatic thresholds and monitor until results normalise.

Clinical pharmacology

A selective, non-hormonal NK3-receptor antagonist. It is metabolised mainly through CYP1A2, with lesser CYP2C9 and CYP2C19 involvement; its principal oxidised metabolite is substantially less active. Elimination is predominantly urinary.

Formulation and product differences

• The selected product is a round, light-red film-coated tablet marked with the company logo and “645”.
• The tablet should be swallowed intact because administration after breaking, crushing or chewing has not been studied.
• Available pack sizes may vary, and not every authorised pack is necessarily marketed.

Tablet

Route: Oral

Strengths: 45 mg