Drug transporters can be major determinants in the pharmacokinetic, safety and efficacy profiles of drugs. For example, transporters expressed on liver and kidney play an important role in directional transport of drugs across hepatocytes and renal proximal tubule, therefore, involve in active hepatic and renal elimination. In many cases, transporter-mediated uptake and efflux can be the rate-determining step for the clearance and the exposure of drugs in the liver and kidney. These transporters open the possibility to selectively deliver a drug to the liver or kidney and to control the elimination process.  However, genetic polymorphisms in transporters may cause inter-individual variability in drug exposure.  Also, inhibition of these transporters may result in clinically significant drug-drug interactions (DDIs). In this presentation, I will focus on recent progress on evaluating the involvement of transporters on hepatic and renal clearance of drugs and predicting transporter related-DDIs.

Roles of transporters in the hepatobiliary and renal elimination of drugs

243rd National Meeting (2012)

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