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Factors Affecting Pharmacokinetic Variability of Imatinib Mesylate (Gleevec, STI-571)
Imatinib mesylate, the first tyrosine kinase inhibitor to gain approval by the FDA,
remains as a pivotal example of rational drug design. Initially, imatinib was found to target
the bcr-abl fusion protein in CML and further targets have subsequently been identified,
including c-kit in GIST. Though a great number of studies have elucidated underlying
mechanisms to explain emerging resistance to this anti-cancer agent, many cases of
resistance remain unexplained. Furthermore, patients exhibit high interindividual
variability in imatinib pharmacokinetics, which may contribute to suboptimal drug
exposure and response