Synthetic biology (SB) has emerged as a revolutionary tool to address pressing challenges in modern drug development, offering unparalleled efficiency and precision. This transformative scientific domain has overcome limitations of the traditional approaches by engineering custom-built biological systems seamlessly aiding the production of therapeutics that were otherwise limited in the past. SB has significantly accelerated various stages of drug discovery by facilitating high-throughput screening, de novo design of biosynthetic pathways, and development of predictive animal models. From the identification of Drug targetsdrug targets using Biosensorsbiosensors and synthetic circuits to the development of advanced cell-based therapies, monoclonal antibodies, and vaccines, SB has laid its hands on various aspects of drug discovery processes. One of the notable milestones brought by this innovative field of biotechnology is the industrial-scale production of artemisinin, which has greatly helped clinicians in meeting the demand of antimalarial drug at the reasonable cost. This chapter puts forth the chronicles of historical milestones of SB from serendipitous discoveries to dedicated intentional efforts addressing the medical needs of our time. It provides a thorough overview of the multifaceted applications of SB in the drug discovery, which include target identification, designing novel assays for screening of inhibitors, and efficient production of drugs utilizing live cells or cell components. Highlighting these breakthroughs, this chapter underscores the paramount role of SB in offering revolutionary solutions to global healthcare challenges and promising the pursuit of effective and accessible therapies.