Abstract: Imatinib, the first line treatment of chronic myelocytic leukemia, is affected by various CYP450 metabolic enzymes and transporters in pharmacokinetic process. Many clinical combination drugs may change its process in vivo by different drug-drug interaction, and even cause significant clinical significance. This article reviews and discusses the effects of different kinds of drugs on the pharmacokinetics of imatinib, so as to ensure the clinical safety and effectiveness of imatinib.