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In the era of advancement of biotechnology and molecular biology, the structure, catalytic site specification, role in biochemical processes, and many diseases of an enzyme have been discovered. Enzymes are protein in nature and are formulated in the human body from amino acids. Each enzyme carries its specific functions in the body and has particular substrates to work with. The enzymes are present in the optimal amount in the body to carry out essential functions for life and health. Proteases or proteinases or peptidases are the largest family of proteolytic enzymes whose primary function is cleaving proteins into smaller fragments. Due to their structural and functional diversity, these enzymes carry out many functions, including intracellular protein formation or recycling, nutrient digestion, and immune system cascade formation. Proteases have been used for years commercially in leather industries, in beer industries to prevent agglomeration of proteins, and detergent formulations. Still, in recent years their therapeutic functions have been discovered and utilized in the pharmaceutical industry. They have been used in the curing, diagnosis, and replacement therapies, etc. Proteases with the development of microbiology and protein engineering have been hitting the market now quite frequently as drugs/therapeutic agents. The U.S. FDA (Food and Drug Administration) now has approved various therapies utilizing protease enzymes as a therapeutic entities, and many next-generation or completely new proteases are in clinical development. There are multiple proteases in the development stage of clinical and preclinical trials. The utilization of enzymes has not achieved 100 percent of its potential mainly due to two reasons: the first reason is the economical difficulties in obtaining pure and homogeneous enzymes leading to higher cost issues, and second the immunogenicity, fast degradation, and inactivation in the body by inhibitors and secretions and due to Physiological pH and temperature barriers. The present article attempts to introduce various therapeutic roles of these enzymes and methods to utilize them to the maximum of their potential in the medical/pharmaceutical field.