Citrus fruits such as oranges, grapefruits, lemons, limes, tangerines, and mandarins, whose production is increasing every year with the rise of consumer demand, are among the most popular fruits cultivated throughout the globe. Citrus genus belongs to the Rutaceae family and is known for its beneficial effects on health for centuries. These plant groups contain many beneficial nutrients and bioactive compounds. These compounds have antimicrobial, anticancer, antidiabetic, antiplatelet aggregation, and anti-inflammatory activities. Citrus waste, generated by citrus-processing industries in large amounts every year, has an important economic value due to richness of bioactive compounds. The present review paper has summarized the application and properties of Citrus and its waste in some fields such as food and drinks, traditional medicine practices, and recent advances in modern approaches towards pharmaceutical and nutraceutical formulations.