Fruit and its extract consumption as part of a diet is a long-standing and well-established practice that aids in supplementing the body’s essential nourishment. The demand for healthy food habits is increasing day by day as the population increases and becoming health cognizant. Fruits and vegetables are exceptional sources of high nutrition. Among fruits, citrus fruits are the most consumed and globally grown in more than 140 countries throughout the world. Citrus fruits majorly belong to the Rutaceae family, are abundant in dietary fiber, and contain mainly sugars like sucrose, glucose, and fructose which help to prevent gastrointestinal disorders and increase the high circulation of cholesterol in the blood. Citrus fruits are one of the most widely processed fruits in the world, resulting in the production of enormous amounts of by-products that are high in cellulose, hemicellulose, soluble sugars, pectin, and essential oils. Citrus peel waste is rich in ascorbic acid, essential oils, pectin, flavonoids, polyphenols, sugars, dietary fibres, and biomass and contains some trace elements. Biomass of citrus waste is used as animal feed and is helpful in soil fertility by adding organic matter. Citrus residues are rich in diversified phytochemicals, which are antimicrobial, anti-inflammatory, antidiabetic, antidepressant, and anticarcinogenic in nature. Studies reported that citrus waste possesses promising nutraceutical candidates for controlling hypercholesterolemia and other health problems. Additionally, exhibits inhibitory activity against pathogenic bacteria and fungi due to the presence of alkaloids, flavonoids, terpenoids, and others. Flavonoids help in reducing the viral attacking risk. In addition, citrus waste is used in biogas production, production of biodegradable polymers in industries, production of cosmetics, and also used as nutraceuticals. Certain compounds from citrus waste are used as preservatives, flavoring agents, and food additives in food industries. Hence, taking into account the importance of citrus waste, this chapter gives an overview of the bioactive compounds found in citrus waste and their applications. Further, this chapter brings together new studies in the areas of nutrition, nutraceuticals, biological and industrial applications of citrus waste. Moreover, concise and in-depth knowledge of this multiformity is offered, which may aid in the optimization and long-term use of citrus waste for the extraction of novel bioactive compounds.