The explosion of metabolic information since the 1990s has served to accentuate the importance of drug metabolism to clinical pharmacology and therapeutics. This new knowledge emphasizes the need for a common understanding among investigators of the different disciplines that impact drug development. To help meet that need, my goal in writing this chapter was to provide a comprehensive overview of the scope of the chemistry and major enzyme systems involved in drug metabolism. Many of the topics could not receive the detailed coverage they merit because of the constraints of space. However, it is hoped that nothing of importance has been missed, and that the references provided serve as a key to deeper exploration by the interested reader.

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