Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Maximum Tolerated Dose
Drug exposure (area under the concentration-time curve) is dose proportional for the dose range of 25 to 1,000 mg, and there is a 1.5- to three-fold drug accumulation at steady-state after once-daily dosing. Analysis of the relationship between PD (WBC reduction) and PK parameters at steady-state indicates that a dose of 400 mg or greater is required for maximal PD effect.