Prodrugs: design and clinical applications.
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.
Rautio
Jarkko
J
Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FI-70211 Kuopio, Finland. jarkko.rautio@uku.fi
Kumpulainen
Hanna
H
Heimbach
Tycho
T
Oliyai
Reza
R
Oh
Dooman
D
Järvinen
Tomi
T
Savolainen
Jouko
J
D000042:Absorption; D000287:Administration, Topical; D000818:Animals; D001682:Biological Availability; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D010288:Parenteral Nutrition; D011355:Prodrugs / Q000008:administration & dosage / Q000737:chemistry
D011355:Prodrugs