ibrutinib: clinical use

Prescribing considerations

• Initiation and supervision should be by a clinician experienced in anticancer treatment.
• Assess bleeding risk, interacting medicines and planned invasive procedures.
• Review cardiac history and function, particularly with arrhythmia, heart failure, hypertension, diabetes or advanced age.
• Establish viral hepatitis status before treatment; seek liver-specialist input when hepatitis B serology is positive.
• Consider infection prophylaxis according to standard care for patients at increased risk of opportunistic infection.
• Hepatic impairment increases exposure; severe hepatic impairment is not recommended. Evidence in severe renal impairment or dialysis is limited.

Contraindications and cautions

• Hypersensitivity to ibrutinib or a formulation excipient
• Concurrent preparations containing St John’s wort

Monitoring

• Complete blood count before and during treatment; the SmPC specifies monthly monitoring.
• Blood pressure and signs of arrhythmia or heart failure.
• Liver function and viral hepatitis status before treatment, with periodic liver-function monitoring.
• Fever, neutropenia and bacterial, viral, fungal or opportunistic infection.
• Bleeding, particularly with anticoagulant or antiplatelet exposure.
• Renal function, hydration and tumour-lysis risk where clinically relevant.
• New pulmonary, neurological or cognitive symptoms.
• Skin examination for non-melanoma skin cancer.

Clinical pharmacology

Ibrutinib forms a covalent bond at the BTK active site, producing sustained inhibition of B-cell receptor and cytokine-receptor signalling. It is primarily metabolised by CYP3A4; its active dihydrodiol metabolite has substantially weaker BTK-inhibitory activity.

Formulation and product differences

• The selected Great Britain product is a film-coated tablet containing lactose monohydrate.
• The tablet must be swallowed whole and not broken or chewed.

Tablet

Route: Oral

Strengths: 140 mg, 280 mg, 420 mg, 560 mg