Abstract
It has been well recognized that transporters as well as metabolic enzymes are important as determinants of drug pharmacokinetics. One of the reasons is the accumulation of clinically-relevant transporter-mediated drug interaction cases. Since the substrate specificity of transporters is very broad as metabolic enzymes, substrate drugs are often recognized by multiple transporters and metabolic enzymes. Moreover, inhibitor drugs can sometimes simultaneously inhibit multiple molecules with different potencies. Under such situation, to understand the influence of altered functions of individual molecules on the efficiency of overall detoxification system of drugs, pharmacokinetic analysis using mathematical modeling is thought to be valuable. In this manuscript, the current status and challenges of the quantitative risk evaluation of drug interactions are briefly overviewed.
