An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons

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 vi...

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Bibliographic Details
Published in:Toxicology and applied pharmacology 2003-06, Vol.189 (3), p.233-246
Main Authors: Brandon, Esther F.A, Raap, Christiaan D, Meijerman, Irma, Beijnen, Jos H, Schellens, Jan H.M
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Biotransformation
Cell lines
Drug Evaluation, Preclinical - methods
General aspects. Methods
Human liver fractions
Humans
In vitro techniques
Liver - cytology
Liver - metabolism
Liver slices
Medical sciences
Microsomes
Microsomes, Liver - metabolism
Pharmaceutical Preparations - metabolism
Supersomes
Toxicology
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Summary: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.
ISSN:0041-008X
1096-0333
DOI:10.1016/S0041-008X(03)00128-5