Ibrutinib

Pronunciation: eye-BROO-ti-nib.

Generic name
ibrutinib
Drug class
Bruton's tyrosine kinase (BTK) inhibitor; antineoplastic agent
Form
Capsule, tablet, or oral suspension (140 mg, 280 mg, 420 mg, 560 mg strengths, depending on market and formulation)
Route
Oral
Legal status
Prescription-only; oncologist/haematologist-managed

Availability and supply rules vary by country

Trade names by country: United States · United Kingdom · Canada · Australia · New Zealand

Australia: Imbruvica (4) · Full directory

What ibrutinib is and how it works

Ibrutinib is a prescription-only oral cancer medicine (a Bruton's tyrosine kinase, or BTK, inhibitor) used to treat certain blood cancers, including chronic lymphocytic leukaemia/small lymphocytic lymphoma (CLL/SLL) and Waldenstrom's macroglobulinemia, and in some countries mantle cell lymphoma. (1)

You take ibrutinib once a day, usually as a capsule or tablet, exactly as your oncology or haematology team directs. It should only be prescribed and managed by a specialist experienced in treating blood cancers, because it carries serious risks including bleeding, infections, heart rhythm problems, and effects on an unborn baby, and requires regular monitoring.

Mechanism of action: how ibrutinib works

Ibrutinib is a small-molecule inhibitor of Bruton's tyrosine kinase (BTK), an enzyme important for B-cell receptor signalling. By forming a covalent bond with a cysteine residue in the BTK active site, ibrutinib irreversibly inhibits BTK activity, reducing the survival and proliferation of malignant B cells in conditions such as CLL/SLL, Waldenstrom's macroglobulinemia, and mantle cell lymphoma. (1) (2)

What ibrutinib is used for

Chronic lymphocytic leukaemia/small lymphocytic lymphoma (CLL/SLL), including with 17p deletion

Used as a single agent, or in combination with other medicines such as rituximab, obinutuzumab, bendamustine, or venetoclax depending on the country and treatment line, for adults with previously untreated or previously treated CLL/SLL, including disease with a 17p chromosomal deletion. (1) (2) (3)

Waldenstrom's macroglobulinemia (WM)

Used as a single agent, or in combination with rituximab, for adults with WM who have received at least one prior therapy, or as first-line treatment for patients unsuitable for chemo-immunotherapy. (1) (2)

Chronic graft-versus-host disease (cGVHD) (United States)

Used for adult and paediatric patients (age 1 year and older) with chronic graft-versus-host disease after failure of one or more lines of systemic therapy. (1)

Mantle cell lymphoma (MCL) -- United Kingdom, European Union, Australia, and New Zealand only

Used as a single agent for relapsed/refractory MCL, or in combination with rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisolone followed by ibrutinib monotherapy for previously untreated, transplant-eligible MCL. IMPORTANT: this indication was voluntarily withdrawn in the United States (FDA withdrawal of approval effective 18 December 2023) because confirmatory phase 3 trial data did not support converting the original accelerated approval to full approval. MCL is not a current US indication for ibrutinib, but remains a current, authorised indication in the UK, EU, Australia, and New Zealand. (2) (4) (5) (6)

Before taking ibrutinib

Do not take / not appropriate for

  • Do not take ibrutinib if you have had an allergic reaction to it or any of its ingredients. (all confirmed markets) (1)

Tell your clinician about

  • Any history of bleeding problems, or if you take blood thinners (anticoagulants) or antiplatelet medicines.
  • Any history of heart rhythm problems (such as atrial fibrillation), heart failure, or high blood pressure.
  • Any history of infections, or a weakened immune system.
  • Any history of liver problems.
  • Any history of skin cancer or other cancers.
  • If you have a high tumour burden, since this affects tumour lysis syndrome risk.
  • All other medicines you take, especially those that affect CYP3A (certain antifungals, antibiotics, and other drugs), since these can raise or lower ibrutinib levels.
  • Pregnancy, plans for pregnancy, or breastfeeding -- and whether effective contraception is in place, since ibrutinib may cause fetal harm.
  • Any upcoming surgery or dental procedure, since ibrutinib may need to be temporarily stopped by your clinician because of bleeding risk.
(1) (2)

How to take ibrutinib

  • Take ibrutinib once daily, at approximately the same time each day, exactly as prescribed.
  • Swallow capsules/tablets whole with a glass of water -- do not open, break, or chew them.
  • Do not take ibrutinib with grapefruit or grapefruit juice, or with Seville oranges, as these can raise ibrutinib levels.
  • If you vomit after taking a dose, or miss a dose, do not take an extra dose -- take your next dose at the usual scheduled time the next day.
  • You will have regular blood tests and clinical checks to monitor for bleeding, infection, blood counts, heart rhythm, and blood pressure.
  • Do not change your dose or stop taking ibrutinib without talking to your oncology or haematology team first -- your clinician may need to temporarily interrupt treatment around surgery or procedures because of bleeding risk.
(1) (2)

Procedures and treatment changes

Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1) (2) (3) (4) (5) (6)

Missed dose

If you vomit after taking a dose, or miss a dose entirely, do not take an additional or replacement dose -- simply take your next dose at the regular scheduled time the following day.

Overdose

Seek urgent medical attention if too much ibrutinib may have been taken, or if you develop signs of severe bleeding, severe infection, or an irregular heartbeat. (1)

Side effects

Side effects and their urgency vary; report severe, persistent, or concerning symptoms.

Bleeding or bruising more easily than usual (including nosebleeds and bruising) -- common.

What to notice: Bleeding or bruising more easily than usual (including nosebleeds and bruising) -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)

Diarrhoea, nausea, fatigue, and musculoskeletal pain -- common.

What to notice: Diarrhoea, nausea, fatigue, and musculoskeletal pain -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)

Infections, including upper respiratory tract infections -- common.

What to notice: Infections, including upper respiratory tract infections -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)

Low blood counts (neutropenia, thrombocytopenia, anaemia) -- common.

What to notice: Low blood counts (neutropenia, thrombocytopenia, anaemia) -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)

Rash and bruising -- common.

What to notice: Rash and bruising -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2)

Serious warnings

Signs of serious bleeding (haemorrhage) — emergency

Symptoms: Unusual or severe bruising, blood in urine or stool, coughing or vomiting blood, severe headache, confusion, or other signs of bleeding inside the head.

Action: Seek urgent medical attention -- major bleeding events, including bleeding inside the head and the gut, have occurred in ibrutinib-treated patients, and fatal bleeding has been reported. Tell your clinician about any blood thinners or antiplatelet medicines you take, and about any planned surgery or procedure, since ibrutinib may need to be temporarily stopped beforehand. In Canada, this risk is presented as a formal 'Serious Warnings and Precautions' box, the most prominent safety designation Health Canada uses; the US and UK labels present the same substance as a detailed Warnings and Precautions section rather than a boxed warning. (1) (2) (3)

Signs of an irregular heartbeat (cardiac arrhythmia) — high caution

Symptoms: Palpitations, dizziness, fainting, chest discomfort, or shortness of breath.

Action: Contact your care team promptly -- ibrutinib has been associated with heart rhythm problems, including atrial fibrillation and atrial flutter, as well as cardiac failure and, rarely, sudden death. Your clinician may monitor your heart rhythm and manage any pre-existing heart or blood pressure conditions closely. (1) (2)

Signs of infection — high caution

Symptoms: Fever, chills, cough, or other new signs of infection.

Action: Contact your care team promptly -- serious infections, including fatal cases, have been reported in patients treated with ibrutinib, related to its effects on the immune system and blood counts. (1) (2)

New or worsening high blood pressure — moderate caution

Symptoms: Headache, dizziness, or a high blood pressure reading.

Action: Your blood pressure will be monitored during treatment -- new or worsening hypertension has been reported with ibrutinib and may need treatment with blood-pressure-lowering medicine. (1)

Signs of tumour lysis syndrome — emergency

Symptoms: Rapid onset of nausea, vomiting, diarrhoea, muscle cramps, seizures, irregular heartbeat, or reduced urination, usually early in treatment in patients with a high burden of disease.

Action: Seek urgent medical attention -- tumour lysis syndrome is a serious, potentially life-threatening complication that can occur, particularly in patients with a high tumour burden; your clinician will assess your risk and may recommend preventive measures. (1)

Risk to an unborn baby — high caution

Symptoms: Not applicable -- this is a treatment-related risk, not a symptom to watch for.

Action: Ibrutinib may cause fetal harm based on animal studies and is not recommended during pregnancy. Women who could become pregnant should use effective contraception during treatment, and per the New Zealand data sheet, for up to 3 months after finishing treatment; men are advised not to father a child or donate sperm during treatment and for 3 months afterward. (1) (5)

New skin lesions or unusual moles — moderate caution

Symptoms: New or changing skin lesions or moles.

Action: Tell your care team -- second primary malignancies, including skin cancers, have been reported in patients treated with ibrutinib; routine skin checks are recommended. (1) (2)

Interactions

  • Strong or moderate CYP3A inhibitors (such as certain antifungal or antibiotic medicines) may increase ibrutinib levels and the risk of side effects -- your clinician may adjust your dose or choose an alternative medicine. (1)
  • Strong CYP3A inducers may reduce how well ibrutinib works. (1)
  • Grapefruit, grapefruit juice, and Seville oranges should be avoided, as they can raise ibrutinib levels. (1)
  • Blood thinners (anticoagulants) and antiplatelet medicines (including some over-the-counter supplements like fish oil or vitamin E) may add to bleeding risk -- tell your clinician about all such medicines and supplements. (2)

Pregnancy, breastfeeding, kidney/liver function, age

Pregnancy

Ibrutinib may cause fetal harm based on animal data and is not recommended during pregnancy. Effective contraception is required during treatment and, per the New Zealand data sheet, for up to 3 months afterward for women. (1) (2) (3) (4) (5) (6)

Breastfeeding

Breastfeeding is not recommended during treatment because of the potential for serious adverse reactions in a nursing infant; discuss with your clinician. (1) (2) (3) (4) (5) (6)

Children

Approved for chronic graft-versus-host disease in paediatric patients aged 1 year and older in the United States; safety and efficacy for other indications in children have not been established. (1) (2) (3) (4) (5) (6)

Elderly

Ibrutinib is used in older adults; your clinician will weigh individual risks such as bleeding and infection, which may be more consequential in frail or elderly patients. (1) (2) (3) (4) (5) (6)

Hepatic_impairment

Dose reduction is required for hepatic impairment (for example, starting at 280 mg once daily for mild impairment and 140 mg once daily for moderate impairment, per the New Zealand data sheet) -- your clinician will determine the appropriate dose. (1) (2) (3) (4) (5) (6)

Renal_impairment

Discuss with your clinician; ibrutinib is primarily eliminated by the liver. (1) (2) (3) (4) (5) (6)

Fertility

Discuss fertility preservation options with your care team before starting treatment if relevant to you. (1) (2) (3) (4) (5) (6)

Monitoring

Before starting

  • Baseline complete blood count
  • Baseline liver function
  • Blood pressure check
  • Cardiac history review, including any prior arrhythmia
  • Pregnancy test and contraception plan where relevant
  • Review of all other medicines for CYP3A interactions and bleeding risk

During treatment

  • Regular complete blood counts to monitor for low blood cell counts.
  • Monitoring for signs of bleeding, infection, and heart rhythm changes.
  • Blood pressure checks.
  • Skin checks for new or changing lesions.
  • Temporary interruption of treatment may be needed around surgery or invasive procedures because of bleeding risk -- this is a clinician decision.
(1) (2)

Storage

Store at room temperature, away from moisture and light, out of reach of children.

Professional information

Clinician-facing context only, sourced from the current US, UK, Canadian, Australian, and New Zealand labels; verify against the current full label before prescribing. Should only be prescribed and managed by a clinician experienced in treating haematological malignancies.

United States

Indication: CLL/SLL (including 17p deletion), Waldenstrom's macroglobulinemia, chronic GVHD (age 1+); mantle cell lymphoma and marginal zone lymphoma indications voluntarily withdrawn, FDA withdrawal effective 18 December 2023

Dose summary: 420 mg once daily for CLL/SLL and WM; reduced doses for hepatic impairment or concurrent strong/moderate CYP3A inhibitors per current label dose-modification tables.

Renal context: The FDA prescribing information gives no renal dose-adjustment recommendation for ibrutinib. Patients with creatinine clearance at or below 30 mL/min were generally excluded from the clinical trials, so exposure and safety in severe renal impairment or on dialysis are not established. Renal status should be assessed by the prescriber rather than adjusted from a published table. (1)

United Kingdom / European Union / Australia / New Zealand

Indication: CLL/SLL, Waldenstrom's macroglobulinemia, and mantle cell lymphoma (previously untreated, ASCT-eligible, in combination with R-CHOP followed by monotherapy; or relapsed/refractory as a single agent) -- MCL indication current in these markets, unlike the US

Dose summary: 420 mg once daily for CLL/SLL and WM; 560 mg once daily for mantle cell lymphoma.

Renal context: The FDA prescribing information gives no renal dose-adjustment recommendation for ibrutinib. Patients with creatinine clearance at or below 30 mL/min were generally excluded from the clinical trials, so exposure and safety in severe renal impairment or on dialysis are not established. Renal status should be assessed by the prescriber rather than adjusted from a published table. (2)

Mechanism of action

Hepatic guidance

Hepatic impairment (Child-Pugh, B-cell malignancies): mild (A) 140 mg daily; moderate (B) 70 mg daily; severe (C) avoid use. For chronic graft-versus-host disease: bilirubin >1.5-3x ULN, 140 mg daily (age 12 and over) or 80 mg/m2 (age 1 to under 12); bilirubin >3x ULN, avoid use.

Overdose note

Manage supportively; monitor closely for bleeding, infection, and cardiac effects. (1) (2)

Frequently asked questions

Does ibrutinib carry a boxed warning?

It depends on the country. The current US label has no boxed warning -- hemorrhage, infections, cardiac arrhythmias, hypertension, cytopenias, second primary malignancies, hepatotoxicity, tumor lysis syndrome, and embryo-fetal toxicity are presented as detailed Warnings and Precautions instead. The UK label follows the same non-boxed approach. Health Canada's product monograph, however, carries a formal 'Serious Warnings and Precautions' box specifically for hemorrhage/major bleeding -- a real, Canada-specific difference in how the same underlying risk is regulatory-formatted. (1) (3)

Is ibrutinib approved for mantle cell lymphoma?

It depends on the country. In the United States, the mantle cell lymphoma (and marginal zone lymphoma) indications were voluntarily withdrawn, with FDA withdrawal of approval effective 18 December 2023, because confirmatory clinical trial data did not support converting the original accelerated approvals to full approval. This withdrawal did not affect ibrutinib's other US indications (CLL/SLL, Waldenstrom's macroglobulinemia, and chronic graft-versus-host disease). Mantle cell lymphoma remains a current, authorised indication in the United Kingdom, European Union, Australia, and New Zealand. (2) (4)

Why do I need to be careful about bleeding on ibrutinib?

Ibrutinib increases the risk of bleeding and bruising, and major bleeding events -- including inside the head and the gut -- have occurred, with rare fatalities reported. Tell your care team about any blood thinners, antiplatelet medicines, or bleeding-risk supplements you take, and about any planned surgery or procedure, since your clinician may need to pause treatment beforehand. (1) (2)

Can ibrutinib affect my heart?

Yes -- ibrutinib has been associated with heart rhythm problems, particularly atrial fibrillation and atrial flutter, as well as cardiac failure and, rarely, sudden death. Tell your clinician about any history of heart problems or high blood pressure, and seek prompt medical attention if you notice palpitations, dizziness, fainting, or chest discomfort. (1) (2)

What is the mechanism of action of ibrutinib?

Ibrutinib is a small-molecule inhibitor of Bruton's tyrosine kinase (BTK), an enzyme important for B-cell receptor signalling. By forming a covalent bond with a cysteine residue in the BTK active site, ibrutinib irreversibly inhibits BTK activity, reducing the survival and proliferation of malignant B cells in conditions such as CLL/SLL, Waldenstrom's macroglobulinemia, and mantle cell lymphoma. (1) (2)

What is the generic name of Ibrutinib?

The generic name is ibrutinib. (1) (2)

What class of drug is ibrutinib?

Ibrutinib is classed as: Bruton's tyrosine kinase (BTK) inhibitor; antineoplastic agent. (1) (2)

References

  1. IMBRUVICA (ibrutinib) capsule, tablet, and oral suspension -- full prescribing information, revised 10/2025U.S. Food and Drug Administration / National Library of Medicine DailyMed, full prescribing information · United States · accessed 2026-07-31 · source 1
  2. Imbruvica 420 mg Film-Coated Tablets -- Summary of Product Characteristics (emc product 10040)UK Medicines and Healthcare products Regulatory Agency / electronic medicines compendium (emc), Summary of Product Characteristics · United Kingdom · accessed 2026-07-31 · source 2
  3. IMBRUVICA (ibrutinib) capsules/tablets -- Product Monograph (health-products.canada.ca Drug Product Database record; monograph PDF last confirmed updated 29 June 2022)Health Canada -- Janssen Inc., product monograph · Canada · accessed 2026-07-31 · source 3
  4. IMBRUVICA (ibrutinib) 140 mg / 280 mg / 560 mg film-coated tablets and 140 mg capsule -- ARTG registrations and AusPARAustralian Therapeutic Goods Administration (TGA), Australian Register of Therapeutic Goods (ARTG) and AusPAR · Australia · accessed 2026-07-31 · source 4
  5. IMBRUVICA (ibrutinib) capsules and tablets -- New Zealand Data SheetNew Zealand Medicines and Medical Devices Safety Authority (Medsafe) · New Zealand · accessed 2026-07-31 · source 5
  6. Imbruvica (ibrutinib) -- European Public Assessment Report (EPAR), EU centralised marketing authorisationEuropean Medicines Agency (EMA) · European Union · accessed 2026-07-31 · source 6

Brand names by country

Single-ingredient ibrutinib names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.

Priority countries

United States

  • Imbruvica70 mg/mL, 140 mg, 280 mg, 70 mg, 420 mg · pharmacyclics llc

United Kingdom

  • Imbruvica (2)UK licensed MCL indication current · 140 mg, 280 mg, 420 mg, 560 mg · Janssen-Cilag Ltd

Canada

  • IMBRUVICA

Australia

  • Imbruvica (4)TGA ARTG registered MCL indication current PBS listed · 140 mg, 280 mg, 560 mg (tablet); 140 mg (capsule) · Janssen-Cilag Pty Ltd

New Zealand

  • Imbruvica (5)Medsafe authorised MCL indication current · 140 mg (capsule); 140/280/420/560 mg (tablet) · Johnson & Johnson (New Zealand) Ltd
View brands in additional countries.

European Union

Imbruvica (6)