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Imatinib CANNOT be Co-Administered with the Following Agents1-3

  • Strong CYP3A4 inducers (e.g. rifampicin)
  • Warfarin

Additional Important Information when Prescribing Imatinib1,3

If co-administration of imatinib and a strong CYP3A4 inducer is needed, use with caution; the imatinib dose should also be increased.4

Co-administration of imatinib and strong CYP3A4 inhibitors should be feasible without dose adjustments. However, caution is needed, and regular monitoring for toxic effects is recommended.3 Alternative agents should be considered.4

Consider increasing the dose of imatinib to 600-700 mg/ 24 hours if co-administering with rifampicin.5

Consider decreasing the dose of imatinib to 300 mg/ 24 hours if co-administering with ketoconazole.5

If imatinib in combination with simvastatin is needed, simvastatin should be switched to another weakly CYP3A metabolised statin, such as rosuvastatin.3

Consider increasing the dose of imatinib to 600-700 mg/ 24 hours if co-administering with carbamazepine.5

Consider decreasing the dose of metroprolol.5


  1. European Medicines Agency. Imatinib (GLIVEC). Summary of Product Characteristics. 2015.
  2. Food and Drug Administration. Imatinib (GLEEVEC) Prescribing information. 2015.
  3. van Leeuwen RW, van Gelder T, Mathijssen RH, Jansman FG. Drug-drug interactions with tyrosine-kinase inhibitors: a clinical perspective. Lancet Oncol 2014; 15: e315-326.
  4. Teo YL, Ho HK, Chan A. Metabolism-related pharmacokinetic drug-drug interactions with tyrosine kinase inhibitors: current understanding, challenges and recommendations. Br J Clin Pharmacol 2015; 79: 241-253.
  5. Pajares B, Torres E, Trigo JM et al. Tyrosine kinase inhibitors and drug interactions: a review with practical recommendations. Clin Transl Oncol 2012; 14: 94-101.

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