Adult: In combination with rituximab, cyclophosphamide, doxorubicin, vincristine and prednisolone (R-CHOP) alternating with rituximab, dexamethasone, cytarabine and cisplatin (R-DHAP) without ibrutinib, followed by ibrutinib monotherapy: In patients with previously untreated cases who are eligible for autologous stem cell transplantation (ASCT): 560 mg once daily. As monotherapy in patients with relapsed or refractory cases: 560 mg once daily; continue until disease progression or unacceptable toxicity occurs. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guidelines).
Oral Chronic lymphocytic leukaemia, Small lymphocytic lymphoma
Adult: Including patients with 17p deletion: As monotherapy or in combination with rituximab or obinutuzumab, or in combination with bendamustine and rituximab: 420 mg once daily; continue until disease progression or unacceptable toxicity occurs. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guidelines).
Oral Chronic lymphocytic leukaemia
Adult: In patients with previously untreated cases: As monotherapy or in combination with anti-CD20 therapy (e.g. rituximab, obinutuzumab): 420 mg once daily; continue until disease progression or unacceptable toxicity occurs. In combination with venetoclax: 420 mg once daily on Days 1-28 every 28 days (as a single agent) for 3 cycles, followed by 420 mg once daily on Days 1-28 every 28 days (in combination with venetoclax) for an additional 12 cycles. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guidelines).
Oral Waldenstrom's macroglobulinaemia
Adult: As monotherapy in patients who have received at least one prior therapy or as 1st-line treatment in patients unsuitable for chemo-immunotherapy; in combination with rituximab: 420 mg once daily; continue until disease progression or unacceptable toxicity occurs. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guidelines).
Oral Chronic graft versus host disease
Adult: In patients after failure of 1 or more lines of systemic therapy: 420 mg once daily; continue until disease progression, recurrence of underlying malignancy or unacceptable toxicity occurs. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guidelines).
What are the brands available for Ibrutinib in Hong Kong?
Mantle cell lymphoma; Chronic lymphocytic leukaemia; Small lymphocytic lymphoma; Waldenstrom's macroglobulinaemia:
Patients taking moderate CYP3A4 inhibitors: 280 mg once daily. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Patients taking strong CYP3A4 inhibitors: 140 mg once daily or withhold treatment for up to 7 days. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Chronic graft versus host disease:
Patients taking posaconazole (at doses ≤200 mg bid suspension) or voriconazole: 280 mg once daily. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Patients taking posaconazole (at doses 200 mg tid suspension, 400 mg bid suspension, 300 mg once daily delayed-release tab or 300 mg once daily IV) or other strong CYP3A4 inhibitors: Avoid use, interrupt treatment or decrease to 140 mg once daily. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Hepatic Impairment
Mild (Child-Pugh class A): 140 mg or 280 mg daily. Moderate (Child-Pugh class B): 140 mg daily. Severe (Child-Pugh class C): Not recommended. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Administration
Ibrutinib May be taken with or without food. Swallow whole w/ water, do not open/break/chew. Do not take w/ grapefruit juice or bitter oranges.
Contraindications
Concurrent use with St. John's wort.
Special Precautions
Patient with acute infection, history of cardiac arrhythmia, risk factors for cardiac events (e.g. hypertension, diabetes mellitus, history of cardiac arrhythmia). Withhold treatment at least 3-7 days before and after surgery based on the type of procedure and risk of bleeding. Hepatic and severe renal impairment. Pregnancy. Discontinue breastfeeding during therapy and for 1 week after the last dose. Concomitant use with moderate or strong CYP3A4 inhibitors.
Adverse Reactions
Significant: Minor bleeding events (e.g. epistaxis, contusion, petechiae), neutropenia, thrombocytopenia, anaemia, leucostasis, lymphocytosis, hypertension, hepatotoxicity, hepatitis B reactivation, hepatitis E, splenic rupture, infections (e.g. sepsis, neutropenic sepsis, bacterial, fungal or viral), interstitial lung disease, tumour lysis syndrome, non-melanoma skin cancer. Blood and lymphatic system disorders: Leucocytosis. Eye disorders: Blurred vision. Gastrointestinal disorders: Nausea, vomiting, dyspepsia, constipation, diarrhoea, stomatitis. General disorders and administration site conditions: Fever, peripheral oedema. Investigations: Increased blood creatinine. Metabolism and nutrition disorders: Hyperuricaemia. Musculoskeletal and connective tissue disorders: Musculoskeletal pain, muscle spasms, arthralgia. Neoplasms benign, malignant and unspecified: Squamous cell carcinoma, basal cell carcinoma. Nervous system disorders: Headache, dizziness, peripheral neuropathy. Renal and urinary disorders: UTI, acute kidney injury. Respiratory, thoracic and mediastinal disorders: URTI, sinusitis, pneumonia. Skin and subcutaneous tissue disorders: Rash, erythema, urticaria, onychoclasis, skin infection. Potentially Fatal: Major bleeding events (e.g. gastrointestinal bleeding, intracranial haemorrhage, haematuria), transient ischaemic attack, ischaemic stroke; CVA, progressive multifocal leucoencephalopathy (PML), serious cardiac arrhythmias and cardiac failure (including atrial fibrillation, atrial flutter and ventricular tachyarrhythmias); hepatic failure, drug-induced liver injury, invasive fungal infections (e.g. Pneumocystis jirovecii infections, aspergillosis, cryptococcosis), haemophagocytic lymphohistiocytosis.
This drug may cause dizziness, fatigue or asthenia; if affected, do not drive or operate machinery. Women of childbearing potential and men must use effective birth control methods during treatment and for up to 3 months after stopping the treatment. Ensure to maintain adequate hydration during therapy.
Monitoring Parameters
Evaluate pregnancy status before initiating therapy. Perform hepatitis B virus screening prior to treatment initiation. Monitor blood counts, blood pressure; LFTs (before and during treatment); uric acid levels (as clinically necessary); renal function; cardiac history or function at baseline and as clinically necessary. Assess for signs or symptoms of cardiac arrhythmias and/or heart failure, bleeding, hepatotoxicity, infections, PML, tumour lysis syndrome, second primary malignancies and leucostasis.
Drug Interactions
Increased risk of bleeding with anticoagulants, antiplatelets, vitamin E and vitamin K antagonists. May increase serum concentration with moderate CYP3A4 inhibitors (e.g. fluconazole, erythromycin, amprenavir, ciprofloxacin, diltiazem, verapamil, amiodarone, dronedarone) or strong CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, ritonavir, voriconazole, posaconazole, itraconazole, nefazodone, cobicistat). May reduce serum concentration with moderate or strong CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenytoin).
Food Interaction
Decreased serum concentration with St. John's wort. May increase exposure with grapefruit juice and Seville oranges. Increased risk of bleeding with fish oil.
Action
Description: Overview: Ibrutinib is a potent and irreversible inhibitor of Bruton's tyrosine kinase (BTK), a vital signalling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. Mechanism of Action: Ibrutinib binds covalently to the cysteine residue (Cys-481) in the BTK active site and irreversibly blocks tyrosine kinase phosphorylation which results in the inhibition of BTK enzymatic activity. The inhibition of BTK results in decreased malignant B-cell proliferation and survival. Pharmacodynamics: In vitro studies have shown that ibrutinib demonstrated effects on cell migration and substrate adhesion; mobilisation of cells from tissues to the peripheral blood results in a transient increase in the absolute lymphocyte count (lymphocytosis). Additionally, in vitro studies have shown that ibrutinib inhibits collagen-induced platelet aggregation. However, ibrutinib did not show a significant inhibition of platelet aggregation for adenosine diphosphate, arachidonic acid, ristocetin and thrombin receptor agonist peptide-6. In cardiac electrophysiology, ibrutinib did not prolong the QT interval to any clinically relevant extent. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Absolute bioavailability: 2.9% (fasted condition). Time to peak plasma concentration: 1-2 hours. Distribution: Volume of distribution: 683 L. Plasma protein binding: Approx 97%. Metabolism: Metabolised in the liver mainly by CYP3A4 and to a lesser extent by CYP2D6 to form the active dihydrodiol metabolite, PCI-45227. Excretion: Via faeces (80%; 1% as unchanged drug); urine (<10% as metabolites). Elimination half-life: 4-13 hours.
Chemical Structure
Ibrutinib Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 24821094, Ibrutinib. https://pubchem.ncbi.nlm.nih.gov/compound/Ibrutinib. Accessed Feb. 24, 2026.
Storage
Tab/Cap: Store between 20-25°C. Oral susp: Store between 2-25°C. Do not freeze. May store for up to 60 days after first opening of bottle. Follow applicable procedures for receiving, handling, administration, and disposal.
L01EL01 - ibrutinib ; Belongs to the class of Bruton's tyrosine kinase (BTK) inhibitors. Used in the treatment of cancer.
References
Brayfield A, Cadart C (eds). Ibrutinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2025.Ibrutinib. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/12/2025.Ibrutinib. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/12/2025.Imbruvica 140 mg Capsules (Johnson & Johnson Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/12/2025.Imbruvica 140 mg Film-coated Tablets (Janssen-Cilag Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/12/2025.Imbruvica Capsule, Film Coated Tablet, Suspension (Pharmacyclics LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/12/2025.Janssen-Cilag (New Zealand) Ltd. Imbruvica 140 mg Capsules; Imbruvica 140 mg, 280 mg, 420 mg and 560 mg Film-coated Tablets data sheet 15 January 2025. Medsafe. http://www.medsafe.govt.nz. Accessed 02/12/2025.Joint Formulary Committee. Ibrutinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2025.
Sign Out
Continue with Google