Prodrugs: My Initial Exploration and Where It Led

Abstract

This review presents my early exploration in the area of prodrugs and specifically prodrugs of the anticonvulsant, phenytoin, also called diphenylhydantoin. My journey started in graduate school with an introduction to the prodrug concept and continued for much of my career as I remain fascinated by the topic/technique. I have also included some backstories that the reader might find noteworthy. Prodrug intervention is now recognized as one of the better tools for taking a challenging small molecule drug from un-developable to developable.

Keywords: Formulation; Limitations; Prodrugs; Safety; Solubility; Stability; Synthesis.