Considering Drug Metabolism and Molecular Complexity in Drug Design

Rüdiger Hardeland
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Rüdiger Hardeland: Department of Zoology and Anthropology, University of Göttingen, Germany

Novel Approaches in Drug Designing & Development, 2017, vol. 2, issue 5, 86-90

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.

Keywords: juniper publishers; drug designing pdf; drug designing articles; drug designing abstract; drug designing journal; modern approaches in drug designing journal; drug designing & intellectual properties international journal; peer reviewed open access journals; high impact journals; juniper publishers review (search for similar items in EconPapers)
Date: 2017
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Persistent link: https://EconPapers.repec.org/RePEc:adp:jnapdd:v:2:y:2017:i:5:p:86-90

DOI: 10.19080/NAPDD.2017.02.555596

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