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.

Additional Metadata
Keywords chronic myelogenous leukemia, imatinib mesylate
Promotor J. Verweij (Jaap)
Publisher Erasmus University Rotterdam
Sponsor Verweij, Prof. Dr. J. (promotor)
ISBN 978-90-8559-367-6
Persistent URL
Gardner, E.R. (2008, April 18). Factors Affecting Pharmacokinetic Variability of Imatinib Mesylate (Gleevec, STI-571). Erasmus University Rotterdam. Retrieved from