Cardoon is a multi-purpose and versatile Mediterranean crop, adapted to climate change, with a wide spectrum of potential applications due its added value as a rich source of fibers, oils and bioactive compounds. The Cynara species are a component of the Mediterranean diet and have been used as food and medicine since ancient times. The important role of cardoon in human nutrition, as a functional food, is due to its high content of nutraceutical and bioactive compounds such as oligofructose inulin, caffeoylquinic acids, flavonoids, anthocyanins, sesquiterpenes lactones, triterpenes, fatty acids and aspartic proteases. The present review highlights the characteristics and functions of cardoon biomass which permits the development of innovative products in food and nutrition, pharmaceutics and cosmetics, plant protection and biocides, oils and energy, lignocellulose materials, and healthcare industries following the actual trends of a circular economy.