Utility of Genetically Modified Animal Models for Drug Metabolism and Drug Transporters

Abstract

Genetically modified animals (GEMA) provide in vivo tools to understand the role of enzymes, transcriptional factors, and transporters in drug disposition and drug toxicities. Several phase I and II enzymes, transcriptional factors, and the clinically relevant drug transporters have been reviewed in this chapter by highlighting how the animal models have elucidated or validated their role in drug disposition, endogenous substrate regulation, or drug toxicities. The utility of animal models in research and drug development provides in vivo tools to gain a better understanding of the role of drug‐metabolizing enzymes, transcriptional factors, and transporters in the absorption, disposition, metabolism, and drug‐related toxicities.