MiniReview: Which in vitro Screens Guide the Prediction of Oral Absorption and Volume of Distribution?

The development of medium to high-throughput in vitro screening of ADME (Absorption, Distribution, Metabolism, Excretion) properties has been the reply to higher demands on drug metabolism scientists to cope with progress in chemistry and biology. Two areas will be discussed here, namely screens for...

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Veröffentlicht in:Basic & clinical pharmacology & toxicology 2005-03, Vol.96 (3), p.162-166
1. Verfasser: van de Waterbeemd, Han
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
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Zusammenfassung:The development of medium to high-throughput in vitro screening of ADME (Absorption, Distribution, Metabolism, Excretion) properties has been the reply to higher demands on drug metabolism scientists to cope with progress in chemistry and biology. Two areas will be discussed here, namely screens for oral absorption and for volume of distribution. The prediction of these human pharmacokinetic parameters can be based on proper combination of simple physicochemical measurements. In the future in vitro screens most likely will be combined with in silico assessments of various ADME properties leading to the concept of in combo screening in drug discovery.
ISSN:1742-7835
1742-7843
DOI:10.1111/j.1742-7843.2005.pto960304.x