Prodrugs: bridging pharmacodynamic/pharmacokinetic gaps.
In this mini review, prodrugs are discussed with a focus on their pharmaceutical, pharmacokinetic, and pharmacodynamic objectives, as well as on the resulting therapeutic benefits. Carrier-linked prodrugs remain the most extensively investigated and receive due attention here with recent successes highlighted. A clear trend is apparent in modern prodrug research, namely the increased attention given to the knowledge-based design of bioprecursors, namely prodrugs devoid of a detachable promoiety. In most cases, such prodrugs are activated by in situ reduction, hence their designation as bioreductive prodrugs. This is a particularly active field in the design of more selective, small-molecule antitumor agents. New antimicrobial agents are also in the pipeline. In addition, biooxidative bioprecursors offer a promising strategy in specific cases, as illustrated by the successful antiaggregating agent clopidogrel.
Testa
Bernard
B
Pharmacy Department, University Hospital Centre, CHUV/BH-04, 46 Rue du Bugnon, CH-1011 Lausanne, Switzerland. Bernard.Testa@chuv.ch
D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D006801:Humans; D011355:Prodrugs / Q000493:pharmacokinetics* / Q000494:pharmacology*
D011355:Prodrugs