High-throughput screening in drug metabolism and pharmacokinetic support of drug discovery

The application of rapid methods currently used for screening discovery drug candidates for metabolism and pharmacokinetic characteristics is discussed. General considerations are given for screening in this context, including the criteria for good screens, the use of counterscreens, the proper sequ...

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Published in:Annual review of pharmacology and toxicology 2000-01, Vol.40 (1), p.133-157
Main Author: White, R E
Format: Article
Language:English
Subjects:
Absorption
Animals
Biotransformation
Blood-Brain Barrier
Enzyme Induction
Humans
Pharmaceutical Preparations - metabolism
Pharmacokinetics
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description The application of rapid methods currently used for screening discovery drug candidates for metabolism and pharmacokinetic characteristics is discussed. General considerations are given for screening in this context, including the criteria for good screens, the use of counterscreens, the proper sequencing of screens, ambiguity in the interpretation of results, strategies for false positives and negatives, and the special difficulties encountered in drug metabolism and pharmacokinetic screening. Detailed descriptions of the present status of screening are provided for absorption potential, blood-brain barrier penetration, inhibition and induction of cytochrome P450, pharmacokinetics, biotransformation, and computer modeling. Although none of the systems currently employed for drug metabolism and pharmacokinetic screening can be considered truly high-throughput, several of them are rapid enough to be a practical part of the screening paradigm for modern, fast-moving discovery programs.
doi_str_mv 10.1146/annurev.pharmtox.40.1.133
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subjects Absorption
Animals
Biotransformation
Blood-Brain Barrier
Enzyme Induction
Humans
Pharmaceutical Preparations - metabolism
Pharmacokinetics
title High-throughput screening in drug metabolism and pharmacokinetic support of drug discovery
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