Prodrugs: design and clinical applications

J Rautio, H Kumpulainen, T Heimbach… - Nature reviews Drug …, 2008 - nature.com
J Rautio, H Kumpulainen, T Heimbach, R Oliyai, D Oh, T Järvinen, J Savolainen
Nature reviews Drug discovery, 2008nature.com
Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic and/or
chemical transformation in vivo to release the active parent drug, which can then exert the
desired pharmacological effect. In both drug discovery and development, prodrugs have
become an established tool for improving physicochemical, biopharmaceutical or
pharmacokinetic properties of pharmacologically active agents. About 5–7% of drugs
approved worldwide can be classified as prodrugs, and the implementation of a prodrug …
Abstract
Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic and/or chemical transformation in vivo to release the active parent drug, which can then exert the desired pharmacological effect. In both drug discovery and development, prodrugs have become an established tool for improving physicochemical, biopharmaceutical or pharmacokinetic properties of pharmacologically active agents. About 5–7% of drugs approved worldwide can be classified as prodrugs, and the implementation of a prodrug approach in the early stages of drug discovery is a growing trend. To illustrate the applicability of the prodrug strategy, this article describes the most common functional groups that are amenable to prodrug design, and highlights examples of prodrugs that are either launched or are undergoing human trials.
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