Enzyme inhibition is a crucial pharmacological approach for treating various diseases as it targets enzymes involved in disease pathogenesis. This review explores the fundamental concepts of enzyme inhibition, including reversible and irreversible mechanisms, and the various types of enzymes, such as proteases, kinases, and polymerases, and their contributions to different disease states. The review discusses the design and production of enzyme inhibitors using methods like structurebased drug design, high-throughput screening, and rational drug design. The review also discusses the challenges and successes encountered in discovering and optimizing potent and selective enzyme inhibitors. Examples of enzyme inhibition's therapeutic benefits include protease inhibitors in HIV/AIDS therapy, kinase inhibitors in cancer treatment, and acetylcholinesterase inhibitors in Alzheimer's disease management. The review also examines possible side effects and limits of enzyme inhibition, focusing on ways to reduce off-target effects and make drugs more specific. At the end of the review, new trends and future possibilities in enzyme inhibition for treating diseases are talked about. These include personalized medicine, combination therapies, and new ways to get drugs into the body. By shedding light on the latest developments, challenges, and future directions, the review aims to contribute to the advancement of this vital field and revolutionize disease treatment modalities.