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  • Title: Imatinib disposition and ABCB1 (MDR1, P-glycoprotein) genotype.
    Author: Gurney H, Wong M, Balleine RL, Rivory LP, McLachlan AJ, Hoskins JM, Wilcken N, Clarke CL, Mann GJ, Collins M, Delforce SE, Lynch K, Schran H.
    Journal: Clin Pharmacol Ther; 2007 Jul; 82(1):33-40. PubMed ID: 17495881.
    Abstract:
    The aim of this study was to explore the impact of individual variation in drug elimination on imatinib disposition. Twenty-two patients with gastrointestinal stromal tumor or chronic myeloid leukemia initially received imatinib 600 mg daily with dosage subsequently toxicity adjusted. Pharmacokinetic parameters on day 1 and at steady-state were compared with elimination phenotype and single-nucleotide polymorphisms of CYP3A5 and ABCB1. A fivefold variation in estimated imatinib clearance (CL/F) was present on day 1 and mean CL/F had fallen by 26% at steady state. This reduction in imatinib CL/F was associated with ABCB1 genotype, being least apparent in thymidine homozygotes at the 1236T>C, 2677G>T/A and 3435C>T loci. Toxicity-related dose reduction also tended to be less common in these individuals. ABCB1 genotype was associated with steady-state CL/F due to an apparent genotype-specific influence of imatinib on elimination. Further evaluation of ABCB1 genotype and imatinib dosage is warranted.
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