A prodrug is a medication or compound that metabolizes into a pharmacologically active drug after administration, offering opportunities to optimize the pharmaceutical property to improve bioavailability. Approximately 10% of all marketed drugs worldwide can be considered prodrugs. However, there are challenges for developing prodrugs.

The therapeutic rationale of a prodrug is to improve the physicochemical, biopharmaceutical, or pharmacokinetic properties of an active pharmaceutical ingredient (API). Key properties that prodrugs seek to modify generally fall within one or more of the ADME categories (Absorption, Distribution, Metabolism, and Excretion) with the end goal being the creation of a new chemical entity (NCE) that optimizes the performance, utility, and potential life-cycle management of the parent drug.

This week’s shared presentation is titled “A Prodrug Approach for Improving Bioavailability” from Dedong Wu at AstraZeneca. Dedong delivered this talk at our past Global Drug Bioavailability Summits earlier this year. This deck will give a brief introduction of the prodrug concept, intrinsic solubility improvement by prodrugs, as well as permeability enhancement by prodrugs. It additionally discusses in vivo molecule stability optimization by prodrugs and perspectives of prodrug design with examples. Scroll through the presentation below…