Abstract
Transporters play an important role in the pharmacokinetics and disposition of pharmaceuticals, environmental contaminants, and endogenous compounds. In the liver, the main organ responsible for biotransformation and disposition, drug transporters are essential for the uptake and excretion of chemicals. Changes in the expression of hepatobiliary transporters are common in multiple forms of liver disease, including drug-induced liver injury, cholestatic liver disease, fatty liver disease, and hepatocellular carcinoma. This chapter provides an overview of the localization, function, and substrate specificity of the various classes of uptake and efflux transporters in the liver. The major findings from studies examining the expression and regulation of hepatobiliary transporters in different models of liver disease are also discussed, in addition to the importance and relevance of changes in transporter expression to liver pathology and the signaling pathways contributing to altered transporter expression during liver disease. The information presented in this chapter provides an essential background for understanding the pharmacological and toxicological consequences of changes in drug transporter expression and function.