Prodrugs are bioreversible, cunning drug derivatives, which can be converted into a parent/active drugs in the organism. They must possess qualities like effective absorption, distribution, metabolism, and elimination (ADME), alongside stability and selectivity to be pharmacologically valuable. Traditional prodrug design is aimed to modify drug properties to mask undesirable features, but modern approaches aim to target physiological enzymes and transporters, enhancing both therapeutic efficacy and convenience. This review outlines modern prodrug synthesis techniques and their clinical benefits, exemplified with various prodrugs (ie: Valganciclovir, L-Val-Zanamivir) and their metabolic pathways, as well as specific targets such as PEPT1 carrier, or valaciclovirase enzyme (VACVase) are exposed.
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