Drug transporters and metabolic enzymes are two major factors in the regulation of disposition of drug in the body. Interestingly, resveratrol, as a new star of anticancer drug, has a close relationship with transporters and metabolic enzymes. It is known that resveratrol can activate or inhibit the function of several transporters directly. Furthermore, the expression of several transporters was changed. Meanwhile, resveratrol is able to inhibit the function of metabolic enzymes (cytochrome P450, CYP450) and regulate the expression of metabolic enzymes. For this reason, when resveratrol is administrated in combination with other drugs, drug-drug interaction (DDI) should be considered. In this review, we summarize the distribution of transporters and metabolic enzymes in the body, the effect of resveratrol on transporters and metabolic enzymes as well as the drug-resveratrol interaction mediated by transporters and metabolic enzymes.