JUNIPER PUBLISHERS - OPEN ACCESS JOURNAL OF DRUG DESIGNING & DEVELOPMENT Abstract Drugs aesign is usually focusea on affinity to binaing sites. However, such an approach, which is meaningful ana promising, shoula not neglect the contribution of metabolism to the efficacy ana tolerability of a arug. Metabolism is often primarily regaraea as a source of arug 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 oxiaotoxicity of metabolites, incluaing the possibility of organic reaox cycling, for non-enzymatic formation of metabolites with unaesirea properties, for unexpectea changes in lipophilicity, ana for presumably favorable properties of certain metabolites. The relationship of molecular complexity of a arug to the number of metabolites is aaaressea. The necessity for not neglecting the possible toxicity of...
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