In vitro characterization and in vitro to in vivo predictions of drug-drug interactions

Abstract The aim of this chapter is to illustrate the theory, concepts, and practices surrounding the in vitro characterization of drug-drug interactions and the subsequent prediction of in vivo drug interactions. More specific information can be found in the numerous manuscripts, reviews, and regulatory guidance referenced within this chapter. Though many of the basic ideas have been well established and studied for years, the field continues to evolve toward more mechanistic and accurate approaches to predict and understand the potential for clinical drug interactions before they occur. A number of the advanced mathematical models and complex modeling approaches such as physiologically based pharmacokinetic modeling coupled with our constantly expanding knowledge base around in vitro CYP enzymology will only serve to further underwrite our ability to identify safe and efficacious therapeutics in years to come.