Abstract: As a first generation tyrosine kinase inhibitor, imatinib is the gold standard drug for the clinical treatment of chronic myelogenous leukemia. However, interindividual differences in resistance and response to imatinib have been widely observed. In vivo and invitro studies have confirmed that ATP-binding cassette transporters, organic cation transporters, and organic anion transporting polypeptides have a large effect on imatinib pharmacokinetics and pharmacodynamics. In addition, the gene polymorphisms of drug transporters can directly or indirectly influence the intracellular concentration of imatinib, resulting in differences in treatment efficacyamong chronic myelogenous leukemia patients. This review profiles the effect of drug transporter gene polymorphisms on susceptibility to imatinib in chronic myelogenous leukemia so as to provide reference to further clinical researches.