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In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development

Year: 2013
Type: review
Abstract: 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.
DOI: 10.1038/clpt.2013.81
Authors: K L R Brouwer, D Keppler, K A Hoffmaster, D A J Bow, Y Cheng, Y Lai, J E Palm, B Stieger, R Evers
Institutions: University of North Carolina at Chapel Hill, German Cancer Research Center, AbbVie (United States), Bristol-Myers Squibb (United States), AstraZeneca (Sweden), University Hospital Zurich, Merck & Co., Inc., Rahway, NJ, USA (United States)
Language: English
Subfield: Oncology
Field: Medicine
Open Access status: bronze
OpenAlex ID: W2010448327
FWCI: 3.331
Cites: 72
Cited by: 273
Related to: 10