Grapefruit processing generates tons of peel waste. Valorization of grapefruit peel waste represents an archetype to extract valuable components viz., dietary fiber, pectin, flavonoids, phenolic acids, and essential oil that can be utilized in food, health, and cosmeceutical industries, materializing the circular economy concept, aligning with sustainable development goals (SDGs). This article chronicles updated information about the potential of bioactive components, methods for extraction, and their application in the food industry as natural additives, to develop functional foods and packaging. Furthermore, it elucidates the mechanism behind grapefruit peels' antioxidant, antimicrobial, anticancer, anti-diabetic, and anti-inflammatory activities. The suitability of thermochemical and biochemical technologies has been discussed for peel waste conversion into value-added products like adsorbents, biochar, and biofuel. Conclusively, this review provides valuable information to capitalize on the utilization of grapefruit peel waste for commercial aims to effectuate a "waste-to-worth" regime and serve the purpose well of SDGs.