Toxicity Risks and Drug Design

Metabolic activation is one of the outcomes for drug metabolism.This process produces reactive metabolites,which usually possess electrophilic properties and form covalent bond with proteins of the body.The reactive metabolites induce idiosyncratic adverse drug reactions,leading to the discontinuation,withdrawal from the market or the strict limitation of their usage of drug candidates during the late clinical trials or after marketing.Drug safety constitutes a critical factor in druggability,thus avoiding alert structures from being transformed into reactive metabolites is one of the important aspects in drug design.The structural features which lead to the toxicity risks and the obviation of those risks in drug design were illustrated in this review.