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

Pharm Res. 1997 Nov;14(11):1504-10. doi: 10.1023/a:1012105713585.


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.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Delivery Systems / trends*
  • Drug Evaluation, Preclinical / trends*
  • Drug Industry / trends*
  • Humans
  • Pharmacokinetics*