Prodrugs and drug delivery

Published on September 23, 2013 Archived on July 31, 2022   38 min

A selection of talks on Pharmaceutical Sciences

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Hello, everyone, I'm Professor Jarrko Rautio from the School of Pharmacy University of Eastern Finland. The subject of my talk is prodrugs and their role in drug delivery. In general, prodrugs can provide a means of solving drug delivery challenges associated with many new chemical entities having larger and more complex molecular structures. In fact, prodrugs are becoming an integral part of the drug discovery paradigm in some large pharmaceutical companies. Also, a number of small biotech companies have built around to design an application of prodrugs to improve their drug candidates. I myself have a 15-year experience with prodrugs, and I have been working on several various product applications so far. For example, in the early stages of my research carrier, I studied dermal prodrugs. This was followed by research on water soluble prodrugs mostly on phosphates and then on cytochrome p450 activated prodrugs, which were targeted to the liver. My most recent studies have focused on sulphenamide prodrug approach to increase the lipophilicity of a very hydrophilic and basic quantity in drug. And we have also spent quite a lot of time with prodrugs which are designed to take advantage of amino acid transporters at the blood-brain barrier and to be taken up into the brain.
I have divided my presentation into four parts. First, I'm going to tell what prodrugs are. Then in the second part, I'll show in one slide the most common functional groups and drugs amenable to prodrug design as well as the most common prodrug structures for this functional groups. Then the main part of my presentation will be dedicated to prodrug examples that have been approved for marketing. These examples are roughly divided based on various problems or barriers which have been overcome in prodrug approaches. Finally, at the end of my talk, I'll show some prodrug statistics, and I'm sure that the numbers I'll show will surprise some.