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Lepidium meyenii is a medicinal edible plant that have nutritional and therapeutic benefits due to synthesis of bioactive compounds. The main phytochemicals found in Lepidium meyenii can be categorized into six classes: glucosinolates and isothiocyanates, thiohydantoins, macaene and macamides, alkaloids, polysaccharides, and fatty acids. These compounds show a wide range of biological activities, which include antioxidant, anti-inflammatory, antimicrobial, cytotoxic, and immunomodulatory activities. Hereby, the objective of this review is to provide a wide comprehension of the nutraceutical properties of Lepidium meyenii. For that, we review and critically discussed original manuscripts describing the chemical and nutritional composition, as well as biological activities of Lepidium meyenii extracts. We showed that the nutraceutical properties of the belowground part of Lepidium meyenii shows great variations that are dependent of differences of phenotype, place of cultivation, type of soil, environmental conditions, and time of harvest. Additionally, we have demonstrated that diet supplementation with Lepidium meyenii may exert several health prophylactics benefits.