The aim of the course is to increase the participant’s understanding of the significance and impact of the metabolism of small molecules in the discovery and development process of drugs. A brief introduction to enzymology will continue into an overview of in silico, in vitro and in vivo approaches. The different in vitro test systems, their properties, best practice, use and relevance will be presented and discussed. The course will also describe how metabolism characteristics have to be further investigated to reveal potential safety issues and drug interactions as well as discuss the importance of understanding their impact. Studies performed to confirm that metabolites formed in humans are safe, will be particularly emphasized.
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