Transporter- and enzyme-targeted prodrugs for improved oral drug delivery

Prodrugs are bioreversible derivatives of drug molecules designed to overcome pharmaceutical, pharmacokinetic, or pharmacodynamic barriers such as low oral absorption, lack of site-specificity, insufficient chemical stability, poor solubility, toxicity, unacceptable taste/odor, etc. The prodrug approach becomes more and more popular and successful; to date, around 10% of all the world’s marketed medications are prodrugs, 20% of all small molecular medicines approved between 2000 and 2008 were prodrugs, and when focusing on 2008 approved drugs, it emerges that over 30% of them were prodrugs (Huttunen et al., 2011; Stella, 2010).