ceritinib: clinical use

Prescribing considerations

• Confirm ALK-positive status using an accurate validated assay.
• Treatment should be initiated and supervised by a clinician experienced in anticancer therapy.
• Review hepatic impairment, diabetes or steroid use, cardiac disease, bradycardia, QT-risk factors, electrolyte disturbance and interacting medicines.
• Investigate new pulmonary symptoms promptly and exclude other causes of pneumonitis.
• Manage gastrointestinal toxicity and dehydration early with appropriate supportive care.

Contraindications and cautions

• Hypersensitivity to ceritinib or any formulation excipient.
• Avoid use in congenital long-QT syndrome; exercise particular caution with other QT-risk factors.

Monitoring

• Validated ALK testing before initiation.
• Liver enzymes and bilirubin before treatment and regularly.
• Fasting blood glucose before treatment and periodically, particularly with diabetes or concurrent corticosteroids.
• Lipase and amylase before treatment and periodically as clinically indicated.
• ECG and electrolytes in patients with cardiac disease, bradycardia, QT predisposition or interacting medicines.
• Heart rate and blood pressure; assess persistent gastrointestinal symptoms, hydration and pulmonary symptoms.

Clinical pharmacology

Ceritinib selectively inhibits ALK autophosphorylation and downstream signalling. CYP3A is the principal metabolic enzyme; ceritinib is also a strong CYP3A4 inhibitor and weak CYP2C9 inhibitor, with predominantly faecal elimination.

Formulation and product differences

• Film-coated tablets are the current listed UK formulation and should be swallowed whole with water.
• The selected hard-capsule product is discontinued in the UK; its product information remains relevant to remaining stock. Capsules should be swallowed whole and not chewed or crushed.
• Tablets and capsules contain different excipients, which should be checked where allergy or intolerance is relevant.

Tablet

Route: Oral

Strengths: 150 mg