Chapter 56 - Membrane transporters and transporter substrates as biomarkers for drug pharmacokinetics, pharmacodynamics, and toxicity/adverse events

Abstract

Membrane transporters belong to two major super families, ATP binding cassette (ABC) transporters and solute carriers (SLC), and play a central role in body homeostasis regulation. Among these membrane proteins, the transporters carrying drugs are extensively studied and participate into the protection of the body against xenobiotics. Drug transporters are involved in all aspects of drugs absorption, disposition, and excretion. Several ABC transporters are highly overexpressed in various tumors and play an important role in the development of multidrug resistance phenotypes in cancers. Furthermore, several transporter polymorphisms have been shown to alter the pharmacokinetic profile of drugs in clinics. Drug transporters are, therefore, biomarkers of drug pharmacodynamics and pharmacokinetics. Finally, transporter substrates can also serve as biomarkers when transporter function is impaired. This chapter reviews the recent research progress in this field with an emphasis on the use of drug transporters as biomarkers in clinics.