Abstract

This chapter describes how pharmacokinetic and metabolism studies are performed during discovery and preclinical development of novel compounds. The techniques used for pharmacokinetic and metabolism studies are briefly reviewed and the strategy for application in preclinical research is described. A number of examples illustrate how such methods are applied at different stages ranging from early discovery to just prior to clinical studies. The interpretation of such studies and their relevance for humans are also critically discussed in the context of species differences in pharmacokinetic and metabolic processes.

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