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Tyrosine kinase inhibitor (BCR-ABL) Pregnancy: Avoid — teratogenic in animal studies. Effective contraception mandatory.

Imatinib

Brand names: Glivec

Adult dose

Dose: CML chronic phase: 400 mg once daily; accelerated/blast phase: 600–800 mg/day
Route: Oral (with food to reduce GI irritation)
Frequency: Once daily (or 400 mg twice daily if tolerated poorly once)
Max: 800 mg/day
CML chronic phase: 400 mg daily. CML accelerated phase/blast crisis: 600 mg daily (may increase to 400 mg BD). Ph+ ALL: 600 mg/day. GIST: 400 mg/day. Take with a meal and glass of water.

Paediatric dose

Route: Oral
Frequency: Once or twice daily
Max: 600 mg/day
≥1 year: 340 mg/m²/day (max 600 mg). Can be dispersed in water or apple juice for children. Dose based on body surface area.

Dose adjustments

Renal

Reduce dose by 25% if eGFR 20–39; avoid if eGFR <20.

Hepatic

Severe hepatic impairment: reduce dose by 25%. Monitor LFTs.

Clinical pearls

  • First BCR-ABL TKI — revolutionised CML treatment (survival comparable to general population)
  • Major molecular response (MMR) target: BCR-ABL <0.1% at 12 months
  • Resistance may be overcome by dose escalation or switch to 2nd gen TKI (dasatinib, nilotinib)
  • T315I mutation: fully resistant — use ponatinib
  • Oedema managed with dose reduction and diuretics if needed

Contraindications

  • Hypersensitivity to imatinib

Side effects

  • Nausea and vomiting
  • Oedema (periorbital, peripheral)
  • Muscle cramps
  • Musculoskeletal pain
  • Myelosuppression (neutropenia, thrombocytopenia, anaemia)
  • Skin rash
  • Elevated liver enzymes
  • Fluid retention / pleural effusion

Interactions

  • CYP3A4 inhibitors (ketoconazole, clarithromycin) — increase imatinib levels
  • CYP3A4 inducers (rifampicin, phenytoin) — reduce imatinib levels significantly
  • Warfarin — avoid co-prescribing; use LMWH instead
  • Ciclosporin, pimozide — increased plasma levels

Monitoring

  • FBC weekly for 1 month, then monthly
  • LFTs monthly for 3 months
  • BCR-ABL transcript levels (PCR) every 3 months
  • Bone marrow cytogenetics

Reference: BNFc; BNF; NICE TA70; ELN Recommendations 2020. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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