PRECLINICAL DRUG-METABOLISM IN THE AGE OF HIGH-THROUGHPUT SCREENING -AN INDUSTRIAL PERSPECTIVE

With the advent of genomics, combinatorial paradigms and high-throughp ut 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 enz ymes and the availability of in vitro absorption-metabolism (AM) model s, Preclinical Drug Metabolism is poised to meet the challenges of HTS . In order to be successful, however, a rational HTS strategy (vs. ser endipitous HTS) has to be employed. Such a strategy is based on automa tion, validation and integration of in vitro AM models and database ma nagement (AVID). A generalized strategy for rational (AVID-based) HTS in Preclinical Drug Metabolism is described briefly.