The immense contributions of chemical science, technology and industry to mankind are acknowledged by one and all. However, along with the human benefits of these precious pharmaceuticals, agrochemicals and fine chemicals, the processes of producing these need to be analyzed critically to modify them for sustainability. It is the ethical responsibility of the chemists and production engineers to design routes which comply with ‘greenness’ keeping in mind their economic and environmental implications, energy and cost-effectiveness and most importantly, the safety aspects. The philosophies of ‘green chemistry’ are certainly the way forward, and greater use of biocatalytic (enzymatic) routes is expected to achieve such goals. This chapter describes the incredible performance of biocatalysts in delivering cost- and power-effective products and processes complying with all aspects of greenness—be it safety, environmental benignity or economic factors. The terminologies ‘biocatalysts/biocatalytic’ and ‘enzymes/enzymatic’ are used interchangeably throughout the chapter. Initially, an overview of the science behind biocatalysis, in terms of the unique enzyme structure, is rationalized, and the mechanisms behind the performance of enzymes as supercatalysts are provided. This is followed by a brief account on the numerous benefits associated with it as well as new paradigm (directed evolution and recombinant DNA technology) and special techniques (enzyme immobilization, solvent engineering) of using biocatalysts to highlight its contributions in ‘green process chemistry’. Finally, representative examples of biocatalytic syntheses of a few drugs/drug intermediates, a food additive and novel biocatalysis-based-technologies are mentioned to demonstrate how these supercatalysts have integrated the natural world with that of academia, research and industry.