Metabolism Studies In Vitro and In Vivo

  • Angela Dudda
  • Gert Ulrich Kuerzel
Reference work entry


In the era of combinatorial chemistry and high-throughput screening, a huge number of hits and structural analogs potentially interesting as new chemical entities (NCEs) can be produced in a short period of time. Drug metabolism is a decisive determinant of the pharmacokinetic behavior of these compounds. Approximately three quarters of the top 200 prescribed drugs in the United States in 2002 are cleared by metabolism, one-third are cleared via the kidney, while biliary clearance of unchanged drug plays only a minor role (Williams et al. 2004). Thus, understanding and description of the metabolism of a new chemical entity is an essential part of the submission dossier (Weaver and Jochemsen 2009) as well as an important optimization parameter in drug discovery programs to reduce attrition in drug development (Kola and Landis 2004)


Drug Metabolism Human Liver Microsome Accelerator Mass Spectrometry Liver Slice Metabolic Stability 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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© Springer-Verlag Berlin Heidelberg 2013

Authors and Affiliations

  1. 1.Sanofi Deutschland GmbHFrankfurt am MainGermany

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