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Pharmacological and adverse effects of drugs depend on the pharmacokinetic properties of drugs, which determine their exposure to the targets. Drug transporters, showing broad substrate specificity to accept a variety of structurally unrelated drugs, mediate the influx and efflux of drugs across plasma membranes. In the body, they play significant roles in the elimination of drugs from the blood in the liver and kidney, the distribution of drugs into their target organs e.g., the brain, and drug absorption in the small intestine. Animal and clinical studies have elucidated that OATPs, OCTs, OATs are particularly important transporter for tissue uptake process, and MATEs, P-glycoprotein, MRPs and BCRP for efflux process. Variation of drug-transporter activities, caused by drug–drug interactions or genetic polymorphisms, influences the disposition of the substrate drugs, and consequently modifies the response. In addition, drug transporters are also important in the disposition of endogenous and food-derived compounds. This chapter illustrates the impact of drug transporters in the disposition of drugs and such endogenous and food-derived compounds.

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