Imatinib (Gleevec/Glivec)

Pronunciation: eye-MAT-in-ib.

Generic name
imatinib (as imatinib mesylate/mesilate)
Drug class
BCR-ABL/KIT/PDGFR tyrosine kinase inhibitor (protein-tyrosine kinase inhibitor)
Form
Film-coated tablets, 100 mg and 400 mg (also available as capsules in some markets); taken with a meal and a large glass of water
Route
Oral
Legal status
Prescription-only medicine in every market confirmed this session (United States, United Kingdom, European Union, Canada, Australia, New Zealand); always check your own country and product label.

Availability and supply rules vary by country

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

Australia: Glivec (5) · Full directory

What imatinib (as imatinib mesylate/mesilate) is and how it works

Imatinib is an oral cancer medicine known as a tyrosine kinase inhibitor. It works by blocking specific enzymes (including the abnormal BCR-ABL protein made by the Philadelphia chromosome, and the Kit and PDGFR receptors) that drive uncontrolled growth in certain blood cancers and tumours, helping to control or shrink the disease. (1) (4) (2)

Imatinib is used for a range of cancers, most commonly chronic myeloid leukaemia (CML) and gastrointestinal stromal tumours (GIST), and treatment is typically long-term and taken daily by mouth. There is no boxed warning on the current US label, but Health Canada's product monograph carries its own formal boxed safety warning covering severe heart failure and reduced heart pumping function, rare severe muscle breakdown (rhabdomyolysis), and severe bleeding -- real risks that apply wherever imatinib is prescribed, even where a market's own label does not format them as a boxed warning. Other important risks include fluid retention, liver problems, severe skin reactions, and (in patients who carry hepatitis B) reactivation of that infection, so regular monitoring and blood tests are an expected part of treatment.

Mechanism of action: how imatinib (as imatinib mesylate/mesilate) works

Imatinib is a small-molecule protein-tyrosine kinase inhibitor that potently inhibits BCR-ABL tyrosine kinase (the constitutive abnormal kinase created by the Philadelphia chromosome in CML), as well as the Kit receptor (stem cell factor receptor), PDGFR-alpha and -beta, discoidin domain receptors DDR1/DDR2, and CSF-1R, inducing apoptosis and inhibiting proliferation in cells driven by these dysregulated kinases. (5) (6)

What imatinib (as imatinib mesylate/mesilate) is used for

Chronic myeloid leukaemia (CML)

Used for newly diagnosed Philadelphia-chromosome-positive (Ph+) CML in chronic phase (adults and children), and for Ph+ CML in accelerated phase, blast crisis, or chronic phase after interferon-alpha treatment has failed. (1) (4) (2)

Philadelphia-chromosome-positive acute lymphoblastic leukaemia (Ph+ ALL)

Used together with chemotherapy for newly diagnosed Ph+ ALL, and alone for relapsed or refractory Ph+ ALL. (1) (4)

Myelodysplastic/myeloproliferative diseases (MDS/MPD)

Used for MDS/MPD associated with PDGFR gene rearrangements. (1) (2)

Aggressive systemic mastocytosis (ASM)

Used for aggressive systemic mastocytosis without the D816V c-Kit mutation, or where mutation status is unknown and other treatments have not worked. (1) (4)

Hypereosinophilic syndrome (HES) / chronic eosinophilic leukaemia (CEL)

Used for advanced HES and/or CEL, particularly where a FIP1L1-PDGFRa gene fusion is present. (1) (2)

Dermatofibrosarcoma protuberans (DFSP)

Used for unresectable, recurrent, or metastatic DFSP, a rare skin tumour. (1) (4)

Gastrointestinal stromal tumours (GIST)

Used for Kit-positive unresectable or metastatic GIST, and as adjuvant (after-surgery) treatment for patients at intermediate-to-high risk of the tumour returning following complete resection. (1) (4) (2)

Before taking imatinib (as imatinib mesylate/mesilate)

Do not take / not appropriate for

  • Do not take imatinib if you have a known hypersensitivity (allergy) to imatinib or any ingredient in the tablet or capsule. (all countries) (1) (4)

Tell your clinician about

  • If you have heart disease, risk factors for heart failure, or a history of reduced heart pumping function -- imatinib can cause or worsen congestive heart failure.
  • If you have liver problems, since imatinib can rarely cause severe or fatal liver injury and monthly liver-function monitoring is typically needed.
  • If you have hepatitis B or have ever had it, even in the past -- imatinib can cause hepatitis B to reactivate, sometimes seriously; you should be tested before starting treatment.
  • If you have a history of unusual bleeding, or are being treated for a gastrointestinal stromal tumour (GIST), since bleeding risk (including at tumour sites) is higher in GIST patients.
  • If you have hypereosinophilic syndrome with possible heart involvement, since starting imatinib can rarely trigger cardiogenic shock in this specific group.
  • If you have had your thyroid removed and take levothyroxine, since imatinib can affect thyroid hormone levels.
  • If you or your child are still growing, since growth retardation has been reported in children and pre-adolescents taking imatinib.
  • If you are pregnant, planning pregnancy, or breastfeeding.
  • Any other medicines you take, including rifampicin, ketoconazole, ciclosporin, pimozide, or warfarin, because of important drug interactions.
(1) (2) (4) (6)

How to take imatinib (as imatinib mesylate/mesilate)

  • Take imatinib by mouth with a meal and a large glass of water, to help reduce stomach and gut irritation.
  • Swallow tablets whole; if you cannot swallow a tablet, it can be dispersed in a glass of water or apple juice and taken immediately once fully disintegrated, per the New Zealand data sheet reviewed -- confirm this is acceptable for your specific product with your pharmacist.
  • Take imatinib at the same time each day, exactly as prescribed by your care team.
  • Do not stop taking imatinib or change your dose without talking to your prescriber first, even if you feel well.
  • Attend all scheduled blood tests -- these check your blood counts, liver function, and other safety measures throughout treatment.
(6)

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

This dossier's sources did not provide specific patient-facing missed-dose instructions for imatinib. If you miss a dose, contact your pharmacist or prescriber for advice rather than doubling your next dose, and try to take your dose at the same time each day to keep levels consistent.

Overdose

This dossier's sources focused on dosing and safety monitoring rather than detailed overdose management. If an overdose is suspected, seek urgent medical attention or contact your local poison control service immediately.

Side effects

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

Nausea, vomiting, diarrhoea, indigestion, abdominal pain.

What to notice: Nausea, vomiting, diarrhoea, indigestion, abdominal pain.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Swelling (edema), including around the eyes.

What to notice: Swelling (edema), including around the eyes.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Muscle cramps, musculoskeletal pain, joint pain, bone pain.

What to notice: Muscle cramps, musculoskeletal pain, joint pain, bone pain.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Rash, dermatitis, or eczema-like skin changes.

What to notice: Rash, dermatitis, or eczema-like skin changes.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Fatigue and headache.

What to notice: Fatigue and headache.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Low blood counts (anaemia, neutropenia, thrombocytopenia) found on routine blood tests.

What to notice: Low blood counts (anaemia, neutropenia, thrombocytopenia) found on routine blood tests.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Weight changes (commonly weight gain, sometimes weight loss).

What to notice: Weight changes (commonly weight gain, sometimes weight loss).

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

Serious warnings

Congestive heart failure and reduced heart pumping function (reduced left ventricular ejection fraction) — canada_serious_warnings_box; high caution elsewhere

Symptoms: Shortness of breath, swelling in the legs or abdomen, unusual tiredness, or a rapid or irregular heartbeat.

Action: Seek medical attention promptly for these symptoms. This is one of the risks named in Health Canada's own formal boxed safety warning for imatinib, and applies wherever imatinib is prescribed; your prescriber will monitor you more closely if you have existing heart disease or risk factors for heart failure. (1) (4)

Severe bleeding (hemorrhage) — canada_serious_warnings_box; high caution elsewhere

Symptoms: Unusual bruising, blood in stool or vomit, black/tarry stools, or severe abdominal pain, especially if you are being treated for a gastrointestinal stromal tumour (GIST).

Action: Seek urgent medical attention. Severe hemorrhage is named in Health Canada's boxed safety warning; GIST patients specifically have a higher reported rate of serious bleeding, sometimes from the tumour site itself. (1) (4) (6)

Rhabdomyolysis (rare severe muscle breakdown) — canada_serious_warnings_box

Symptoms: Severe muscle pain, weakness, or dark/tea-colored urine.

Action: Seek urgent medical attention -- this is a rare but serious risk named specifically in Health Canada's boxed safety warning for imatinib. (4)

Severe or fatal liver injury — high caution

Symptoms: Yellowing of the skin or eyes (jaundice), dark urine, severe fatigue, or right-sided abdominal pain.

Action: Seek prompt medical attention. Fatal liver failure and severe liver injury requiring transplantation have been reported; your prescriber will check your liver function regularly, typically monthly, especially early in treatment. (1) (2)

Severe skin reactions (bullous reactions, erythema multiforme, Stevens-Johnson syndrome) — high caution

Symptoms: Blistering or peeling skin, painful rash, or sores in the mouth, eyes, or genitals.

Action: Seek urgent medical attention immediately and tell them you are taking imatinib -- these are rare but potentially life-threatening skin reactions that need prompt clinical assessment. (1)

Fluid retention — moderate to high caution

Symptoms: Rapid or unexpected weight gain, swelling, shortness of breath, or abdominal bloating.

Action: Tell your prescriber promptly -- severe fluid retention (in the lungs, around the heart, or in the abdomen) has been reported in around 1-2.5% of newly diagnosed CML patients and can be serious; your prescriber may recommend weighing yourself regularly. (1) (2) (6)

Gastrointestinal perforation — moderate caution

Symptoms: Sudden, severe abdominal pain.

Action: Seek emergency medical attention immediately -- rare cases, including fatalities, of GI perforation have been reported. (1)

Hepatitis B reactivation — important safety information

Symptoms: Yellowing of the skin/eyes, dark urine, severe fatigue, or abdominal pain, particularly if you are a known or past hepatitis B carrier.

Action: Tell your prescriber if you have ever had hepatitis B -- you should be tested before starting imatinib, and closely monitored during and for several months after treatment if you are a carrier, since reactivation can lead to serious liver damage. (2) (6)

Tumour lysis syndrome — moderate caution

Symptoms: Nausea, reduced urination, muscle cramps, or irregular heartbeat, particularly at the start of treatment in patients with a high tumour burden.

Action: Your prescriber will typically check and correct hydration and uric acid levels before you start imatinib if you are at higher risk. (2) (6)

Cardiogenic shock (specific to hypereosinophilic syndrome patients) — moderate caution, population-specific

Symptoms: Sudden severe shortness of breath, chest pain, or fainting shortly after starting treatment.

Action: If you have hypereosinophilic syndrome with suspected heart involvement, your prescriber may check your heart with an echocardiogram and blood tests, and may give you a short course of steroids when you start imatinib to reduce this rare but serious risk. (1) (2)

Decline in kidney function — moderate caution

Symptoms: Usually no symptoms until picked up on a blood test.

Action: Your prescriber will check your kidney function before starting and periodically during long-term treatment, since gradual decline has been reported. (1)

Growth retardation (children) — important safety information, population-specific

Symptoms: Slower-than-expected growth in height.

Action: If your child is taking imatinib, their growth will be monitored regularly -- the long-term effects on growth are not fully known. (1) (6)

Interactions

  • Strong CYP3A4 inhibitors (e.g. ketoconazole): can increase imatinib levels and side effects; use with caution. (6)
  • Strong CYP3A4 inducers (e.g. rifampicin, St John's Wort): can reduce imatinib's effectiveness; avoid or use with caution. (6)
  • CYP3A4 substrates with a narrow therapeutic window (e.g. ciclosporin, pimozide): imatinib may raise their levels; use with caution and monitoring. (6)
  • CYP2C9 substrates with a narrow therapeutic window (e.g. warfarin and other coumarin anticoagulants): imatinib may raise their levels; use with caution and closer monitoring (an alternative anticoagulant such as a heparin may be preferred). (6)
  • Levothyroxine: thyroidectomy patients on levothyroxine replacement may need dose adjustment, since imatinib has been linked to hypothyroidism in this group. (2)

Pregnancy, breastfeeding, kidney/liver function, age

Pregnancy

Imatinib should not be used during pregnancy unless clearly necessary, since it can cause fetal harm and was teratogenic in animal studies. Women who could become pregnant should use effective contraception during treatment and for at least 14-15 days after stopping. (1) (2) (3) (4) (5) (6)

Breastfeeding

Breastfeeding is not recommended during treatment and for at least 15 days after stopping, since imatinib and its metabolite pass into human milk. (1) (2) (3) (4) (5) (6)

Children

Used in children for CML and, less commonly, other indications, with dosing based on body surface area; long-term growth should be monitored, and there is very limited experience in children under 2 years of age. (1) (2) (3) (4) (5) (6)

Elderly

No specific dose recommendation is needed based on age alone, though no significant age-related pharmacokinetic differences were observed in clinical trials that included patients 65 and older; some fluid-retention adverse events were more frequent in elderly patients. (1) (2) (3) (4) (5) (6)

Hepatic_impairment

Dose adjustment may be needed depending on the severity of liver impairment; the minimum recommended dose is generally used, with careful monitoring of liver enzymes and blood counts. (1) (2) (3) (4) (5) (6)

Renal_impairment

Imatinib and its metabolites are not significantly excreted by the kidneys; patients with renal impairment can generally start at the minimum recommended dose, with caution and dose adjustment based on tolerability. (1) (2) (3) (4) (5) (6)

Monitoring

Before starting

  • Hepatitis B testing (to identify chronic carriers at risk of reactivation).
  • Baseline liver function tests and complete blood count.
  • Baseline kidney function tests.
  • Echocardiogram and troponin assessment in patients with hypereosinophilic syndrome and suspected cardiac involvement.
  • Correction of dehydration and high uric acid levels in patients at risk of tumour lysis syndrome.
  • Pregnancy test where relevant, and contraception counselling.

During treatment

  • Complete blood counts: weekly for the first month, every two weeks for the second month, then periodically.
  • Liver function tests: monthly, or as clinically indicated.
  • Regular weight checks to catch fluid retention early.
  • Periodic kidney function monitoring, especially with long-term treatment.
  • Growth monitoring in children.
  • Ongoing monitoring for hepatitis B reactivation in known carriers, continuing for several months after stopping treatment.
(1) (2) (6)

Storage

Store at room temperature as directed on the packaging, protected from moisture, and keep out of the reach of children.

Professional information

Clinician-facing context only, sourced from the current US DailyMed prescribing information, UK EMC SmPC, EU EMA EPAR, Health Canada product monograph, Australia's TGA ARTG/AusPAR Product Information, and New Zealand's Medsafe data sheet reviewed for this dossier; verify against the current full label for the specific product before prescribing.

United States, Canada, European Union

Indication: Full multi-indication set: CML (all phases), Ph+ ALL, MDS/MPD with PDGFR rearrangements, aggressive systemic mastocytosis, HES/CEL, DFSP, GIST (including adjuvant)

Dose summary: 400 mg once daily (chronic phase CML, GIST), 600 mg once daily (accelerated/blast crisis CML, Ph+ ALL), up to 800 mg daily (DFSP, or dose-escalated GIST/CML) -- 100 mg and 400 mg tablets.

Renal context: Not significantly renally excreted; caution and dose reduction as needed in renal impairment. (1) (4)

United Kingdom, Australia, New Zealand

Indication: Same broad indication set as the US/Canada/EU, per the UK SmPC, Australian AusPAR Product Information, and New Zealand data sheet reviewed

Dose summary: Dosing matches the US/Canada/EU pattern (400-800 mg/day depending on indication and response); dose reduced for severe hepatic dysfunction or severe hematologic adverse reactions per published thresholds.

Renal context: Caution advised in renal impairment; minimum recommended dose used as a starting point, per the New Zealand data sheet reviewed. (2) (6)

Mechanism of action

Hepatic guidance

Dose adjustment recommended depending on severity of hepatic dysfunction (mild/moderate/severe classifications based on bilirubin and AST); the minimum recommended dose is typically used with careful monitoring.

Overdose note

This dossier's sources did not detail specific overdose management guidance for imatinib beyond general supportive care principles. (5) (6)

Frequently asked questions

Is imatinib (Gleevec/Glivec) available in the US, UK, EU, Canada, Australia, and New Zealand?

Yes, confirmed authorised via direct regulator sources in all six markets: the United States (DailyMed, brand Gleevec), United Kingdom (EMC SmPC, brand Glivec), the European Union (EMA EPAR, brand Glivec), Canada (Health Canada product monograph, brand Gleevec), Australia (TGA ARTG/AusPAR, brand Glivec), and New Zealand (Medsafe, e.g. IMATIS). (1) (2) (3) (4) (5) (6)

Does imatinib carry a boxed warning?

Not in the United States -- there is no boxed warning on the current US FDA label. Health Canada's product monograph, however, carries a formal 'Serious Warnings and Precautions' section covering severe congestive heart failure and reduced left ventricular ejection fraction, rare rhabdomyolysis, and severe hemorrhage, which is Canada's own equivalent of a boxed warning. (1) (4)

What cancers is imatinib used to treat?

Imatinib is used mainly for Philadelphia-chromosome-positive chronic myeloid leukaemia (CML) and gastrointestinal stromal tumours (GIST), and also for Ph+ acute lymphoblastic leukaemia, certain myelodysplastic/myeloproliferative diseases, aggressive systemic mastocytosis, hypereosinophilic syndrome/chronic eosinophilic leukaemia, and dermatofibrosarcoma protuberans, depending on the specific genetic markers involved. (1) (4) (2)

What are the most serious risks of taking imatinib?

The most serious, well-documented risks are congestive heart failure/reduced heart pumping function, severe bleeding, rare rhabdomyolysis (all three named in Health Canada's boxed warning), severe or fatal liver injury, severe skin reactions, hepatitis B reactivation in carriers, and gastrointestinal perforation. Regular blood tests and monitoring are used to catch problems early. (1) (4) (2)

What is the mechanism of action of imatinib (as imatinib mesylate/mesilate)?

Imatinib is a small-molecule protein-tyrosine kinase inhibitor that potently inhibits BCR-ABL tyrosine kinase (the constitutive abnormal kinase created by the Philadelphia chromosome in CML), as well as the Kit receptor (stem cell factor receptor), PDGFR-alpha and -beta, discoidin domain receptors DDR1/DDR2, and CSF-1R, inducing apoptosis and inhibiting proliferation in cells driven by these dysregulated kinases. (5) (6)

What is the generic name of Imatinib (Gleevec/Glivec)?

The generic name is imatinib (as imatinib mesylate/mesilate). (1) (5)

What class of drug is imatinib (as imatinib mesylate/mesilate)?

Imatinib (Gleevec/Glivec) is classed as: BCR-ABL/KIT/PDGFR tyrosine kinase inhibitor (protein-tyrosine kinase inhibitor). (1) (5)

References

  1. GLEEVEC (imatinib mesylate) tablets -- full prescribing informationDailyMed (U.S. National Library of Medicine) -- FDA-approved prescribing information · United States · dated 2012-01-01 · accessed 2026-07-31 · source 1
  2. Glivec 400 mg film-coated tablets -- SmPCelectronic medicines compendium (emc), United Kingdom -- Summary of Product Characteristics · United Kingdom · dated 2025-01-01 · accessed 2026-07-31 · source 2
  3. Glivec (imatinib) -- EPAR summary for the publicEuropean Medicines Agency (EMA) -- European Public Assessment Report (EPAR) · European Union · dated 2025-01-01 · accessed 2026-07-31 · source 3
  4. GLEEVEC (imatinib mesylate) tablets -- Product Monograph including Patient Medication InformationHealth Canada -- Product Monograph (Novartis Pharmaceuticals Canada Inc.) · Canada · dated 2019-10-08 · accessed 2026-07-31 · source 4
  5. GLIVEC (imatinib) 100mg and 400mg tablets -- ARTG registrations 94216/94217; AusPAR Product Information (PM-2011-02797-3-4, final 4 June 2013)Therapeutic Goods Administration (TGA), Australia -- ARTG entries and AusPAR-approved Product Information · Australia · dated 2013-06-04 · accessed 2026-07-31 · source 5
  6. IMATIS (imatinib, as mesilate) 100 mg & 400 mg Film Coated Tablets -- New Zealand Data Sheet, Version NZ-V04/September 2024Medsafe (New Zealand Medicines and Medical Devices Safety Authority) · New Zealand · dated 2024-09-01 · accessed 2026-07-31 · source 6

Brand names by country

Single-ingredient imatinib (as imatinib mesylate/mesilate) names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.

Priority countries

United States

  • Gleevec (1)FDA approved confirmed · 100 mg, 400 mg · Novartis Pharmaceuticals Corporation

United Kingdom

  • Glivec (2)MHRA licensed confirmed · 100 mg, 400 mg · Novartis Pharmaceuticals UK Ltd

Canada

  • Gleevec (4)Health Canada authorised confirmed · 100 mg, 400 mg · Novartis Pharmaceuticals Canada Inc.

Australia

  • Glivec (5)TGA ARTG registered confirmed 94216 94217 · 100 mg, 400 mg · Novartis Pharmaceuticals Australia Pty Ltd

New Zealand

  • IMATIS (6)Medsafe listed confirmed · 100 mg, 400 mg · Devatis Limited (EastPharma)
View brands in additional countries.

European Union

Glivec (3)

This page provides general reference information about imatinib (Gleevec/Glivec) and is not a substitute for advice from your oncologist, pharmacist, or clinician. Imatinib is a cancer medicine requiring specialist supervision and regular monitoring -- never start, stop, or change your dose without medical advice. Seek urgent medical attention for shortness of breath, unusual bleeding, severe muscle pain, yellowing of the skin or eyes, or blistering skin reactions.

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