Abstract: Drug transporters and metabolic enzymes are the key proteins in the disposition of drugs in the body. In recent years it has been found that there is a cooperative relationship between drug transporters and metabolizing enzymes. Functional changes in drug transporters or metabolizing enzyme can affect the ability to eliminate drugs. Therefore, it is important to clarify this cooperative relationship, which is directly related to the pharmacokinetics, pharmacodynamics and adverse effects of drugs. Intestine and liver are the main organs of drug metabolism. There are abundant drug transporters and metabolizing enzymes in the tissues. This paper reviews the influence of the cooperative relationship between drug transporters and metabolizing enzymes on drug disposition by intestine and liver.