Imatinib
Brand names: Glivec
Imatinib is an oral tyrosine kinase inhibitor used in Philadelphia chromosome-positive chronic myeloid leukaemia and acute lymphoblastic leukaemia, and in gastrointestinal stromal tumours.
Adult dose
Dose adjustments
Metabolism is mainly hepatic; only 13% of excretion is through the kidneys. Patients with a history of renal failure should be monitored carefully. (eMC SPC §4.2 excerpt does not state a specific renal dose reduction; verify against full SPC.)
Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.
Contraindications
- Hypersensitivity to the active substance or to any of the excipients
Side effects
- Nausea, vomiting, diarrhoea, abdominal pain
- Fatigue, myalgia, muscle cramps
- Rash
- Superficial oedema (primarily periorbital or lower limb); fluid retention (pleural effusion, ascites, pulmonary oedema, rapid weight gain) which may be serious or life-threatening
- Myelosuppression (more common in CML than GIST); GI and tumoural bleeding, which may be serious and sometimes fatal
Interactions
- Strong CYP3A4 inducers (e.g. dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarbital, St John's Wort) — avoid; may significantly reduce imatinib exposure and increase risk of therapeutic failure
- Protease inhibitors, azole antifungals, certain macrolides (caution — may increase imatinib exposure)
- CYP3A4 substrates with a narrow therapeutic window (e.g. ciclosporin, pimozide, tacrolimus, sirolimus, ergotamine, dihydroergotamine, fentanyl, alfentanil, terfenadine, bortezomib, docetaxel, quinidine) — caution
- Warfarin and other coumarin derivatives — caution
- Levothyroxine (hypothyroidism reported in thyroidectomy patients on replacement; monitor TSH)
Clinical monograph
How it works
It inhibits the BCR-ABL tyrosine kinase produced by the Philadelphia chromosome, and also KIT and PDGFR kinases, blocking the signalling that drives malignant cell proliferation.
Prescribing in practice
- Fluid retention and oedema, including pleural or pericardial effusion, can occur and may be serious, so monitor weight and watch for unexpected fluid accumulation.
- It is a CYP3A4 substrate and inhibitor, so review concomitant medicines for clinically important interactions.
- Myelosuppression and hepatotoxicity occur, requiring dose modification for significant cytopenias or deranged liver function.
Monitoring
Monitor full blood count, liver function and weight regularly, and assess molecular or cytogenetic response according to disease.
Counselling the patient
- Take it with food and a large glass of water to reduce stomach upset.
- Report rapid weight gain, swelling, breathlessness, bleeding or signs of infection.
- Avoid grapefruit juice and tell your team about any other medicines you take.
Evidence & guidelines
Imatinib transformed the management of chronic myeloid leukaemia following the IRIS trial and is recommended by NICE as first-line therapy.
Reference: NICE TA70; ELN Recommendations 2020; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).
Related
Curated clinical cross-links plus same-class fallbacks.
- SMART Risk Score for Recurrent CVD · Cardiovascular Risk
- PCSK9 Inhibitor Eligibility Assessment · Lipid Management
- Immune-Related Adverse Events (irAE) -- GI Toxicity Colitis Grading · Oncology-Related GI
- irAE Hepatitis Grading (CTCAE) · Immunotherapy
- DIPSS — Dynamic International Prognostic Scoring System for Myelofibrosis · Cancer Prognosis
- Sokal Index for Chronic Myelogenous Leukaemia · Leukaemia
- Major Haemorrhage / Massive Transfusion · BCSH; RCOA; RCEM; RCS — BCSH Guidelines
- Anaemia Investigation · BSH / NICE
- Splenomegaly Workup · BSH; BMJ Best Practice
- Deep Vein Thrombosis Diagnosis and Treatment · NICE CG144 / NICE NG158
- Sickle Cell Crisis · BSH 2021 / BCSH
- Neutropenic Sepsis · NICE CG151 2012 / ESMO