: In recent decades, enzymes have been the target of considerable research, development, and innovation. This paper presents an up-to-date overview of the technological application of lipases in the pharmaceutical industry. Lipases have been used in a variety of ways in the pharmaceutical industry, both in the obtainment of bioactive molecules to overcome limitations in the formulation of medicines and in drug design. This is possible from alternative technologies, such as immobilization and the use of non-aqueous solvents, which allows the use of lipases in commercial scale processes. In addition, other technologies have provided the emergence of differentiated and more specific lipases in order to meet the perspectives of industrial processes. The research indicates that the next years should be promising for the application of lipase in the industrial biocatalysis and in drug design.