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.

Verweij, Prof. Dr. J. (promotor)
J. Verweij (Jaap)
Erasmus University Rotterdam
Erasmus MC: University Medical Center Rotterdam

Gardner, E. (2008, April 18). Factors Affecting Pharmacokinetic Variability of Imatinib Mesylate (Gleevec, STI-571). Retrieved from