binimetinib: clinical use

Prescribing considerations

• Confirm an appropriate tumour BRAF mutation using a suitable validated test before treatment.
• Initiate and supervise treatment through a clinician experienced in anticancer therapy.
• Review cardiac, ocular, thromboembolic, bleeding, pulmonary, hepatic and neuromuscular risks.
• The binimetinib–encorafenib combination is not recommended in moderate or severe hepatic impairment.
• Evidence is limited in brain metastases and after progression on a previous BRAF inhibitor.

Contraindications and cautions

• Hypersensitivity to binimetinib or any excipient.
• The formulation contains lactose and should not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.

Monitoring

• Confirm BRAF mutation status.
• Assess left ventricular ejection fraction before and during treatment.
• Ask about visual symptoms at each review and arrange prompt ophthalmological assessment when indicated.
• Monitor blood pressure, liver tests, creatine kinase and creatinine.
• Perform regular skin assessments and investigate new or changing lesions.
• Monitor clinically for bleeding, venous thromboembolism, pneumonitis and tumour lysis syndrome.

Clinical pharmacology

Binimetinib is an ATP-uncompetitive, reversible MEK1/MEK2 inhibitor. It suppresses MAPK-pathway signalling and is primarily cleared through UGT1A1-mediated glucuronidation.

Formulation and product differences

• The selected product is an unscored film-coated tablet containing lactose.
• The selected tablets can be dispersed in water, orange juice or apple juice when swallowing whole tablets is not possible.

Tablet

Route: Oral

Strengths: 15 mg, 45 mg