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The field of drug transporters has exploded over the past 30 years. It is now known that transporters are located in virtually every organ and tissue in the body and are involved in every aspect of drug absorption, distribution, excretion, and even influence drug metabolism by regulating access to drug metabolizing enzymes. Because of their ubiquity and function, drug transporters profoundly influence drug pharmacokinetics and pharmacodynamics. Moreover, factors which influence drug transporter function, such as genetic polymorphisms or transporter based drug interactions, can have a major impact on drug efficacy and safety. This chapter summarizes the role of transporters in drug disposition, gives examples of their clinical relevance, and describes the emerging role of drug transporters in drug discovery and development. |
