Terpenoids are the most diverse and largest class of chemicals of the innumerable plant-based compounds. Plants carry out a number of essential growth and production functions using terpenoid metabolites. In contrast, most terpenoids are used in the abiotic and biotic systems for complex chemical interactions and defense. Terpenoids derived from plants mostly used humans for pharmaceutical, food, and chemical industries in the past. However, recently biofuel products have been developed by terpenoids. The metabolism of high-quality terpenoids in plants and microbes is facilitated in synthetic biology by genomic resources and emerging tools. Further focus has been given to the ecological value of terpenoids for establishing effective pesticide control approaches and abiotic stress protection. The awareness of the diverse metabolic and molecular regulatory networks for terpenoid biosynthesis needs to be increased continuously in all these efforts. This review gives an overview and highlights current improvements in our understanding of the organization, regulation, and diversification of core and specialized terpenoid metabolic pathways and discusses the prominent therapeutic roles of terpenoids. This review provides an overview and highlights recent literature in our understanding about the biomedical and therapeutic importance of terpenoids, regulation as well as the diversion of core and specialized metabolized terpenoid pathways.