Dose adjustments(view chart below)
Dose adjustments may be necessary due to hepatotoxicity, other nonhematologic adverse reactions, or hematologic adverse reactions:
- Hepatic impairment: Patients with mild and moderate hepatic impairment do not require a dose adjustment and should be treated per the recommended dose. A 25% decrease in the recommended dose should be used for patients with severe hepatic impairment
- Renal impairment: Patients with moderate renal impairment (CrCL= 20-39 mL/min) should receive a 50% decrease in the recommended starting dose, and future doses can be increased as tolerated. Doses >600 mg are not recommended in patients with mild renal impairment (CrCL=40-59 mL/min)
- For patients with moderate renal impairment, doses >400 mg are not recommended
- Imatinib should be used with caution in patients with severe renal impairment
- Hepatotoxicity and nonhematologic adverse reactions: If elevations in bilirubin >3 x institutional upper limit of normal (IULN) or in liver transaminases >5 x IULN occur, GLEEVEC should be withheld until bilirubin levels have returned to <1.5 x IULN and transaminase levels to <2.5 x IULN. In adults, treatment with GLEEVEC may then be continued at a reduced daily dose (ie, 400 mg to 300 mg, 600 mg to 400 mg or 800 mg to 600 mg)
- If a severe nonhematologic adverse reaction develops (such as severe hepatotoxicity or severe fluid retention), GLEEVEC should be withheld until the event has resolved. Thereafter, treatment can be resumed as appropriate depending on the initial severity of the event
- Concomitant strong CYP3A4 inducers: Dosage of GLEEVEC should increase by at least 50%, and clinical response should be carefully monitored in patients receiving GLEEVEC with a potent CYP3A4 inducer such as rifampin or phenytoin
- Examples of commonly used drugs that may significantly interact with GLEEVEC include ketoconazole, acetaminophen, warfarin, and erythromycin. (Click here for full Prescribing Information for other potential drug interactions)
- For daily dosing of 800 mg and above, dosing should be accomplished using the 400-mg tablets to reduce exposure to iron
- Instead of adjusting the dose of GLEEVEC, switching to another treatment option may work for your adult patients when GLEEVEC is no longer effective. Click here to learn more about another treatment option for your GLEEVEC-resistant or -intolerant adult patients
Some adverse reactions may require dosage adjustment, dose interruption, or discontinuation.1,2Back to top
1. GLEEVEC® (imatinib mesylate) tablets prescribing information. East Hanover, NJ: Novartis Pharmaceuticals Corporation; January 2012.
2. Deininger MW, O'Brien SG, Ford JM, Druker BJ. Practical management of patients with chronic myeloid leukemia receiving imatinib. J Clin Oncol. 2003;21(8):1637-1647.