Enhancing Drug Design Through Prodrugs

Review Article

Abstract

Prodrugs represent a class of drug molecules engineered to undergo reversible chemical or enzymatic transformations in vivo, releasing the active parent drug. This strategic modification facilitates enhanced pharmacological effects while mitigating drawbacks associated with conventional drug administration. Ideal prodrugs exhibit pharmacological inactivity prior to conversion, swift and specific conversion to the active drug compound, and incorporation of non-toxic moieties. Effective prodrug design addresses challenges such as stability, toxicity, solubility, permeability, and drug targeting, which significantly impact drug discovery and development. By altering physicochemical, biopharmaceutical, or pharmacokinetic properties, prodrug design achieves precise drug delivery. Approximately 10-14% of globally approved drugs fall under the prodrug classification. This article comprehensively explores objectives, classifications, activation mechanisms, conceptual frameworks, prerequisites for clinically viable prodrugs, as well as their diverse applications across drug discovery and development endeavors