A Prodrug is a specialized substance designed to contain the parent drug while remaining either inactive or only partially active. These molecules are intentionally engineered to undergo biotransformation within the body, either through chemical or enzymatic cleavage, in order to release the active compound at levels suitable for therapeutic effects. The prodrug approach holds great promise as a strategic modification in drug development, capable of addressing various pharmaceutical, pharmacokinetic, and pharmacodynamic challenges. The primary goal of prodrug development is to overcome barriers such as inadequate chemical stability, poor solubility, undesirable taste or odor, irritation or discomfort, insufficient oral absorption, limited blood-brain barrier permeability, substantial pre-systemic metabolism, and toxicity issues. Furthermore, the addition of a pro-moiety to the active moiety offers an innovative solution for circumventing the obstacles that hinder the full utilization of the active compound's potential. This chapter seeks to offer a comprehensive exploration of prodrugs, including their historical context, objectives, associated benefits, and therapeutic applications. It also advocates for the integration of prodrug technology into modern healthcare systems to enhance the effectiveness and safety of pharmaceutical treatments. In summary, prodrugs are a valuable tool in the realm of pharmaceutical science, serving as a means to optimize drug performance and overcome various limitations. This chapter endeavors to shed light on their multifaceted role and promote their integration within contemporary healthcare practices.