Amaranthus spinosus has long been cultivated in tropical and subtropical areas of the world, especially in South Asia. It is well accepted by the people for its nutritional, pharmacological, phytochemical, and therapeutic functions in the human body. Tender stems, leaves, shoots, grains and sometimes the whole part of A. spinosus are eaten by humans or fed to farm animals, which contain carbohydrates, proteins, fats, fibers, vitamins, minerals and many other phytochemicals. This review aims to represent the nutritional and pharmacological activities of A. spinosus. To have a better understanding, we have discussed the nutritional status of A. spinosus, its available phytochemicals and their functional properties. Further, we demonstrated the potentiality of A. spinosus in various disease condition by discussing its functional activities, which includes antioxidant, antidiabetic, immuno-modulatory, hematological, gastrointestinal, anti-inflammatory, diuretic, antimicrobial, antimalarial, anti-ulcer, antipyretic, and antigenic activity. The availability of various important phytochemicals along with their functional properties make Amaranthus spinosus valuable for pharmaceuticals and nutraceuticals industry.