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Preclinical Drug Metabolism in the Age of High-Throughput Screening: An Industrial Perspective

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Abstract

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 vitroAM models and database management (AVID). A generalized strategy for rational (AVID-based) HTS in Preclinical Drug Metabolism is described briefly.

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  1. Drug Metabolism (Preclinical), Merck Research Laboratories, Sumneytown Pike, P.O. Box 4, WP26A 2044, West Point, Pennsylvania, 19486-0004

    A. David Rodrigues

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Rodrigues, A.D. Preclinical Drug Metabolism in the Age of High-Throughput Screening: An Industrial Perspective. Pharm Res 14, 1504–1510 (1997). https://doi.org/10.1023/A:1012105713585

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