Abstract
With the increase in the numbers of molecules synthesized in a typical drug discovery program, as well as the large amount of information utilized in the selection of a drug candidate, there is a need for a plethora of drug metabolism and pharmacokinetic (DMPK) information to be regularly generated in discovery. Over the past decade, many in vitro, and even in vivo, DMPK screens have been developed and routinely deployed to generate this information in support of drug discovery efforts. In the past few years, newer methods, or adaptations to methods, have been published, and this review attempts to summarize these advances. In particular, advances have been reported for experimental approaches to metabolic clearance, CYP inhibition, in vivo exposure, and distribution, as well as in silico determinations of absorption, distribution, metabolism, and excretion (ADME) properties. Bioanalytical approaches aimed at optimizing analyte method development, sample preparation, and analyte detection, have also been reported. Future advances will further improve the ability to make decisions on molecules earlier in drug discovery.
Combinatorial Chemistry & High Throughput Screening
Title: Recent Advances in High Throughput Screening for ADME Properties
Volume: 11 Issue: 3
Author(s): Timothy J. Carlson and Michael B. Fisher
Affiliation:
Abstract: With the increase in the numbers of molecules synthesized in a typical drug discovery program, as well as the large amount of information utilized in the selection of a drug candidate, there is a need for a plethora of drug metabolism and pharmacokinetic (DMPK) information to be regularly generated in discovery. Over the past decade, many in vitro, and even in vivo, DMPK screens have been developed and routinely deployed to generate this information in support of drug discovery efforts. In the past few years, newer methods, or adaptations to methods, have been published, and this review attempts to summarize these advances. In particular, advances have been reported for experimental approaches to metabolic clearance, CYP inhibition, in vivo exposure, and distribution, as well as in silico determinations of absorption, distribution, metabolism, and excretion (ADME) properties. Bioanalytical approaches aimed at optimizing analyte method development, sample preparation, and analyte detection, have also been reported. Future advances will further improve the ability to make decisions on molecules earlier in drug discovery.
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Cite this article as:
Carlson J. Timothy and Fisher B. Michael, Recent Advances in High Throughput Screening for ADME Properties, Combinatorial Chemistry & High Throughput Screening 2008; 11 (3) . https://dx.doi.org/10.2174/138620708783877717
DOI https://dx.doi.org/10.2174/138620708783877717 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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