Validation of in vitro cell models used in drug metabolism and transport studies

Esther Brandon, Tessa Bosch, Maarten J Deenen, Rianne Levink, Evertdina van der Wal, J Van Meerveld, Monique Bijl, Jos H Beijnen, Jan Schellens, Irma Meijerman

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Human cell lines are often used for in vitro biotransformation and transport studies of drugs. In vivo, genetic polymorphisms have been identified in drug-metabolizing enzymes and ABC-drug transporters leading to altered enzyme activity, or a change in the inducibility of these enzymes. These genetic polymorphisms could also influence the outcome of studies using human cell lines. Therefore, the aim of our study was to pharmacogenotype four cell lines frequently used in drug metabolism and transport studies, HepG2, IGROV-1, CaCo-2 and LS180, for genetic polymorphisms in biotransformation enzymes and drug transporters. The results indicate that, despite the presence of some genetic polymorphisms, no real effects influencing the activity of metabolizing enzymes or drug transporters in the investigated cell lines are expected. However, this characterization will be an aid in the interpretation of the results of biotransformation and transport studies using these in vitro cell models. ? 2005 Elsevier Inc. All rights reserved.
Original languageEnglish
Pages (from-to)1 - 10
Number of pages10
JournalToxicology and Applied Pharmacology
Issue number1
Publication statusPublished - 2006

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