Abstract
AbstractRetrometabolic approaches represent systematic drug design methodologies that thoroughly integrate structure—activity and structure—metabolism relationships and are aimed to design safe compounds with an improved therapeutic index. They incorporate two major concepts aimed to design soft drugs and chemical delivery systems, respectively. Soft drugs are new, active therapeutic agents that undergo predictable metabolism to inactive metabolites after exerting their desired therapeutic effect. Chemical delivery systems are biologically inert molecules that provide enhanced and targeted delivery of an active drug to a particular organ or site through a designed sequential metabolism that involves several steps. The present comprehensive review includes an overview of the general retrometabolic drug design principles and provides a variety of specific examples to illustrate the concepts. If possible, the rationale for the design as well as the pharmacokinetic and pharmacodynamic properties of the new therapeutic agents are briefly summarized and compared to those of the other compounds used in the same field.
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