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Clin Pharmacol Ther. 2013 Jul;94(1):95-112. doi: 10.1038/clpt.2013.81. Epub 2013 Apr 10.

In vitro methods to support transporter evaluation in drug discovery and development.

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Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.

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  • Clin Pharmacol Ther. 2013 Sep;94(3):412.


This white paper addresses current approaches and knowledge gaps concerning methods to assess the role of transport proteins in drug/metabolite disposition in humans. The discussion focuses on in vitro tools to address key questions in drug development, including vesicle- and cell-based systems. How these methods can be used to assess the liability of compounds for transporter-based drug-drug interactions (DDIs) in vivo is also explored. Existing challenges and approaches to examine the involvement of transporters in drug disposition are discussed.

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