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Tyrosine kinase inhibitor (BCR-ABL) Pregnancy: Should not be used during pregnancy unless clearly necessary; if used, inform patient of potential risk to the foetus. Post-marketing reports of spontaneous abortions and infant congenital anomalies. Women of childbearing potential must use effective contraception during treatment and for at least 15 days after stopping. Breast-feeding: women should not breast-feed during treatment and for at least 15 days after stopping (imatinib and active metabolite distribute into human milk).

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.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 400 mg/day (chronic phase CML)
Route: Oral (with a meal and a large glass of water)
Frequency: Doses of 400 mg or 600 mg once daily; a daily dose of 800 mg given as 400 mg twice a day (morning and evening)
Max: 800 mg/day (given as 400 mg twice daily)
Therapy should be initiated by a physician experienced in the treatment of haematological malignancies and malignant sarcomas. Dose is indication-specific. Adult CML: 400 mg/day chronic phase; 600 mg/day accelerated phase; 600 mg/day blast crisis. Dose increases from 400 mg to 600 mg or 800 mg (chronic phase), or from 600 mg to a maximum of 800 mg (accelerated phase/blast crisis) may be considered in the absence of severe adverse drug reaction and severe non-leukaemia-related neutropenia or thrombocytopenia (e.g. disease progression, inadequate haematological response after >=3 months, no cytogenetic response after 12 months, or loss of previous response). Adult Ph+ ALL: 600 mg/day. Adult MDS/MPD: 400 mg/day. Adult HES/CEL: 100 mg/day (increase from 100 mg to 400 mg may be considered if insufficient response). Adult GIST (unresectable and/or metastatic): 400 mg/day (limited data on increases to 600 mg or 800 mg on progression). Treatment generally continued until disease progression. Paediatric (BSA-based, not per-kg): CML chronic and advanced phase 340 mg/m2 daily (not to exceed total dose 800 mg), as a once-daily dose or split morning/evening; may increase to 570 mg/m2 daily (not to exceed 800 mg) under the same circumstances as adults. Ph+ ALL children: 340 mg/m2 daily (not to exceed total dose 600 mg). No experience in children below 2 years of age. For patients unable to swallow tablets, tablets may be dispersed in still water or apple juice.

Dose adjustments

Renal

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.