YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Reviews
Pharmacologically Active Metabolites of Currently Marketed Drugs: Potential Resources for New Drug Discovery and Development
Myung Joo KANG, Woo Heon SONG, Byung Ho SHIM, Seung Youn OH, Hyun Young LEE, Eun Young CHUNG, Yesung SOHN, Jaehwi LEE
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Keywords: pharmacologically active metabolite, biotransformation, metabolism, drug discovery
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2010 Volume 130 Issue 10 Pages 1325-1337

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Abstract

  Biotransformation is the major clearance mechanism of therapeutic agents from the body. Biotransformation is known not only to facilitate the elimination of drugs by changing the molecular structure to more hydrophilic, but also lead to pharmacological inactivation of therapeutic compounds. However, in some cases, the biotransformation of drugs can lead to the generation of pharmacologically active metabolites, responsible for the pharmacological actions. This review provides an update of the kinds of pharmacologically active metabolites and some of their individual pharmacological and pharmacokinetic aspects, and describes their importance as resources for drug discovery and development.

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© 2010 by the PHARMACEUTICAL SOCIETY OF JAPAN
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