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Pharm Res. 1997 Nov;14(11):1504-10.

Preclinical drug metabolism in the age of high-throughput screening: an industrial perspective.

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Merck Research Laboratories, West Point, Pennsylvania 19486-0004, USA.


With the advent of genomics, combinatorial paradigms and high-throughput screen (HTS)-based pharmacological testing, the number of compounds flowing through the discovery pipeline is likely to escalate. At the same time, with increased knowledge of the human drug-metabolizing enzymes and the availability of in vitro absorption-metabolism (AM) models, Preclinical Drug Metabolism is poised to meet the challenges of HTS. In order to be successful, however, a rational HTS strategy (vs. serendipitous HTS) has to be employed. Such a strategy is based on automation, validation and integration of in vitro AM models and database management (AVID). A generalized strategy for rational (AVID-based) HTS in Preclinical Drug Metabolism is described briefly.

[Indexed for MEDLINE]

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