Abstract: In clinic, it is very common that a variety of drugs are used in the treatment of diseases. However, the combination of drugs can easily lead to the occurrence of drug-drug interaction (DDI), which can lead to the reduction or loss of drug efficacy, the increase of adverse reactions, and even lead to serious adverse reactions. Drug transporters play an important role in the occurrence and development of DDI by influencing the disposal process of combined drugs in vivo. In this paper, the relationship between DDI and transporter was summarized. The effects of transporter-mediated DDI on the drug disposal process in vivo, and the relations of DDI and disease or multidrug resistance were reviewed. The current guiding principles of DDI research in China were briefly introduced. The purpose was to remind clinical medical workers to pay attention to transporter-mediated DDI and improve the safety of drug combination, further to provide a new vision and ideas for disease treatment and avoiding multidrug resistance.

Key words: transporter, drug-drug interaction, diseases, multidrug resistance