In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development.
Brouwer, K LR 1; Keppler, D 2; Hoffmaster, K A 3; Bow, D AJ 4; Cheng, Y 5; Lai, Y 5; Palm, J E 6; Stieger, B 7; Evers, R 8; on behalf of the International Transporter Consortium
[Review] Clinical Pharmacology & Therapeutics. 94(1):95-112, July 2013.

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: 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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