The pharmacogenetics of imatinib

Abstract

Imatinib mesylate (IM), a tyrosine kinase inhibitor, is one of the fi rst molecularly targeted therapies to have been used in the clinic. It has proven to be effi cient in the treatment of chronic myeloid leukemia and also in other malignancies that involve expression of a tyrosine kinase. However, some patients can develop resistance and others suff er from toxic side eff ects. The pharmacokinetics of IM depends on several enzymes and transporters, and several studies have attempted to identify genetic factors associated with variable drug levels and clinical responses using a candidate gene approach. Larger and more homogenous studies are still needed to replicate the fi ndings obtained so far, or to analyze other genetic variations to get clearer insights into how IM treatment can be tailored to each patient's genetics. Here we summarize pharmacogenetic studies of IM and highlight the genetic markers that could be used to improve the treatment and management of diseases for which IM is used.© 2010 BioMed Central Ltd.