title: An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons.
abstract: The liver is the predominant organ in which biotransformation of foreign compounds takes place, although other organs may also be involved in drug biotransformation. Ideally, an in vitro model for drug biotransformation should accurately resemble biotransformation in vivo in the liver. Several in vitro human liver models have been developed in the past few decades, including supersomes, microsomes, cytosol, S9 fraction, cell lines, transgenic cell lines, primary hepatocytes, liver slices, and perfused liver. A general advantage of these models is a reduced complexity of the study system. On the other hand, there are several more or less serious specific drawbacks for each model, which prevents their widespread use and acceptance by the regulatory authorities as an alternative for in vivo screening. This review describes the practical aspects of selected in vitro human liver models with comparisons between the methods.
authors.affiliation: Division of Drug Toxicology, Department of Biomedical Analysis, Faculty of Pharmaceutical Sciences, Utrecht University, The Netherlands. e.f.a.brandon@pharm.uu.nl
authors.forename: Esther F A
authors.initials: EF
authors.lastname: Brandon
authors.forename: Christiaan D
authors.initials: CD
authors.lastname: Raap
authors.forename: Irma
authors.initials: I
authors.lastname: Meijerman
authors.forename: Jos H
authors.initials: JH
authors.lastname: Beijnen
authors.forename: Jan H M
authors.initials: JH
authors.lastname: Schellens
mesh_terms: D000818:Animals; D001711:Biotransformation; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D006801:Humans; D008099:Liver / Q000166:cytology / Q000378:metabolism*; D008862:Microsomes, Liver / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism*
chemical_list: D004364:Pharmaceutical Preparations