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In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development
Author(s) -
Brouwer K L R,
Keppler D,
Hoffmaster K A,
Bow D A J,
Cheng Y,
Lai Y,
Palm J E,
Stieger B,
Evers R
Publication year - 2013
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.2013.81
Subject(s) - drug discovery , drug development , computational biology , transporter , pharmacology , in vitro , drug , computer science , chemistry , medicine , biology , bioinformatics , biochemistry , gene
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. Clinical Pharmacology & Therapeutics (2013); 94 1, 95–112. doi: 10.1038/clpt.2013.81