Chemistry-enabled drug delivery (prodrugs): recent progress and challenges
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Updated: May 8, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
Published on: February 17, 2023
Sophie-Dorothee Clas1, Rosa I Sanchez2, Rebecca Nofsinger3
1Basic Pharmaceutical Sciences, Merck & Co., West Point, PA 19486, USA.
Abstract:
Prodrugs can be used to enhance the properties of an active pharmaceutical ingredient or drug, generally by improving solubility and/or permeability of the compound. However, discovery teams duly spend considerable time and resources on structure-activity optimization and formulation-enabled drug delivery technologies to achieve the target exposures and biopharmaceutical properties, when early implementation of prodrugs could lead to an improved drug molecule. The goal of this review is to provide an overview of the achievements during the past few years in developing prodrugs and highlighting the challenges of following this approach.
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