Imatinib

Indications
 Oral
Chronic myeloid leukaemia
Adult: Chronic phase: 400 mg daily, increased to 600 mg daily or 400 mg bid. Blast crisis or accelerated phase: 600 mg daily, increased to 400 mg bid as required.
Child: Chronic or advanced phase: 340 mg/m2 daily. Max Dose: 600 mg. May be given once daily ordivided into morning and evening doses.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
Acute lymphoblastic leukaemia
Adult: 600 mg daily with induction, consolidation or maintenance chemotherapy.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
As monotherapy in relapsed or refractory acute lymphoblastic leukaemia
Adult: 600 mg daily with induction, consolidation or maintenance chemotherapy.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
Myelodysplastic disease
Adult: 400 mg daily. For eosinophilic syndrome: Start with 100 mg daily in patients with FIP1L1-platelet-derived growth factor receptor-a fusion kinase, may increase to 400 mg if response is insufficient.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
Hypereosinophilic syndrome
Adult: 400 mg daily. For eosinophilic syndrome: Start with 100 mg daily in patients with FIP1L1-platelet-derived growth factor receptor-a fusion kinase, may increase to 400 mg if response is insufficient.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
Unresectable, metastatic malignant gastrointestinal stromal tumours
Adult: 400 or 600 mg daily.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
Mastocytosis
Adult: 400 mg daily. Start with 100 mg daily if there is associated eosinophilia.
Hepatic impairment: Severe: Reduce dose by 25%.
Oral
Dermatofibrosarcoma protuberans
Adult: 400 mg bid.
Hepatic impairment: Severe: Reduce dose by 25%.

Special Populations: Recommended dose in patients on potent CYP3A4 inducers: Increase dose by 50%.
Contraindications
 Lactation.
Warnings / Precautions
 Cardiac disease or increased risk for CHF. Monitor for signs of severe fluid retention. Monitor CBC regularly. Renal and hepatic impairment. Monitor LFTs. Pregnancy.
Adverse Reactions
 Fluid retention/oedema, nausea and vomiting, muscle cramps, musculoskeletal pain, diarrhoea, rash. Fatigue, asthenia, headache, dizziness, insomnia, depression, anxiety, joint pain, arthralgia, myalgia, back pain, abdominal pain, flatulence, dyspepsia, loose stools, anorexia, constipation, taste disturbance, nasopharyngitis, cough, pharyngolaryngeal pain, pharyngitis, sinusitis, upper respiratory tract infection, pneumonia, influenza, dyspnoea, haemorrhage, pyrexia, increased wt, night sweats, rigors, hepatotoxicity, hypokalaemia, pruritus, chest pain, increased lacrimation.
Drug Interactions
 Increased blood levels with CYP3A4 inhibitors (azole antifungals, macrolide antibiotics). Reduced blood levels with CYP3A4 inducers (carbamazepine, dexamethasone, St John's wort, phenobarbital, phenytoin, rifampicin). May increase blood levels of substrates of CYP3A4 (ciclosporin, pimozide, triazolo-benzodiazepines, dihydropyridine calcium-channel blockers, certain statins), CYP2C9 (warfarin) and CYP2D6.
See Below for More imatinib Drug Interactions
Mechanism of Actions
 Imatinib, a tyrosine kinase inhibitor, inhibits the Bcr-Abl tyrosine kinase which is created by the Philadelphia chromosome abnormality in chronic myeloid leukaemia (CML). It blocks proliferation and induces apoptosis in BCR-ABL positive cell lines, as well as fresh leukaemic cells from Philadelphia chromosome positive CML.
Absorption: Mean bioavailability: approx 98%; peak blood concentrations reached after 2-4 hr.
Distribution: Protein-binding: Approx 95%.
Metabolism: Major isoenzyme responsible for metabolism is CYP3A4; isoenzymes CYP1A2, CYP2D6, CYP2C9 and CYP2C19 also play a minor role.
Excretion: Elimination half-life: 18 hr (imatinib), 40 hr (N-demethylated piperazine derivative). About 81% is eliminated within 7 days in the faeces (68%) and urine (13%). Excreted mostly as metabolites, with only 25% as unchanged drug.
Administration
 Should be taken with food.
ATC Classification
 L01XE01 - imatinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Available As
  • Imatinib 100 mg
  • Imatinib Mesylate 100 mg
  • Imatinib 400 mg
  • Imatinib Mesylate 400 mg

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