Processing pineapple industry produces huge amounts of waste thus contributing to worsen the global environmental problem. Valorising pineapple waste through further processing until it is transformed into valuable products using environmentally friendly techniques is both, a challenge, and an opportunity. The aim of this review is to characterize and highlight the phytochemical constituents of pineapple peel, their biological activity, and to evaluate the current state-of-art for the utilization of pineapple waste from the processing industry for obtaining pharmaceuticals, food, and beverages, biocombustibles, biodegradable fibers, and other different usage. Pineapple residues are rich in many bioactive compounds such as ferulic acid, vitamin A and C as antioxidant, and containing alkaloids, flavonoids, saponins, tannins, cardiac glycoside, steroids, triterpenoids and phytosterols may provide a good source of several beneficial properties, as well as bromelain that showed significant anticancer activity. Also, pineapple processing residues contain important volatile compounds used as aroma enhancing products and have high potential to produce value-added natural essences.