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Prodrug strategies to overcome problems in drug therapy
Published on July 31, 2022 37 min
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Hi, my name is Jarkko Rautio. I'm a Professor in Pharmaceutical Chemistry and Vice Head at the School of Pharmacy, University of Eastern Finland. The focus of this lecture is on prodrug strategies to overcome problems in drug therapy.
This slide shows you an outline of the lecture. The first part will briefly cover the broad concept of what prodrugs are and what prodrugs there are. This will then lead to examples of prodrugs that have been able to overcome various ADMET issues. Most of the examples will be dealing with prodrugs that were made to improve either poor solubility or poor lipophilicity. But there'll also be examples designed to reduce toxicity issues mainly by controlling the release of the active parent drug. I will then discuss some prodrug numbers and recent prodrug approvals. The final part of the lecture will shortly cover preclinical issues regarding prodrugs, and things to consider when working on prodrugs with a take home message. Several examples given in this lecture are described in an extensive prodrug review that was published in 2018.
This is a simplified prodrug concept. A drug promoiety molecule is a prodrug. According to the definition, it is pharmacologically inactive or significantly less active than the parent drug. The barrier which a prodrug should overcome can be basically any biological barrier, such as an epithelial barrier, or it can be a physicochemical barrier, such as poor solubility or poor lipophilicity. Both can result in poor absorption and so on. Once the prodrug has overcome the barrier as an inactive compound, it must undergo conversion, which, in most cases, is an enzymatic conversion to release the active parent drug in the body.