Transporters are membrane proteins that play a role in the movement of endogenous substances and xenobiotics across cellular membranes into and out of cells. Understanding the role of transporters in drug disposition is an evolving science and over the last 15-20 years there have been great advances. As such, the transporter area is considerably less developed than what is known about common enzymes influencing drug disposition such as cytochrome P450. This chapter provides basic information on transporter families, their localization, and known substrates and inhibitors.


4.1 List of Abbreviations 57

4.2 Basic Concepts 58

4.3 Methods for Studying Transporters 61

4.4 Transporter Localization 63

4.5 Substrates and Inhibitors 68

4.6 Transporter-Mediated Clinical Drug-Drug Interactions 70

References 72

Additional Reading 72

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