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Considering Drug Metabolism and Molecular Complexity in Drug Design

Author

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  • Rüdiger Hardeland

    (Department of Zoology and Anthropology, University of Göttingen, Germany)

Abstract

Drugs design is usually focused on affinity to binding sites. However, such an approach, which is meaningful and promising, should not neglect the contribution of metabolism to the efficacy and tolerability of a drug. Metabolism is often primarily regarded as a source of drug elimination. On the other hand, metabolites can have their own pharmacological properties, which may be highly undesired, but, in other cases, can be favorable. In this short review, examples are given for oxidotoxicity of metabolites, including the possibility of organic redox cycling, for non-enzymatic formation of metabolites with undesired properties, for unexpected changes in lipophilicity, and for presumably favorable properties of certain metabolites. The relationship of molecular complexity of a drug to the number of metabolites is addressed. The necessity for not neglecting the possible toxicity of minor metabolites is emphasized. Drug metabolism should be more systematically included in drug design, exceed actions of cytochrome P450 isoforms and also focus on metabolite properties.

Suggested Citation

  • Rüdiger Hardeland, 2017. "Considering Drug Metabolism and Molecular Complexity in Drug Design," Novel Approaches in Drug Designing & Development, Juniper Publishers Inc., vol. 2(5), pages 86-90, October.
    • Handle: RePEc:adp:jnapdd:v:2:y:2017:i:5:p:86-90
    DOI: 10.19080/NAPDD.2017.02.555596
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