Taro corms contain valuable bioactive molecules effective against cancer and cancer-related risk factors, such as carcinogens and biological agents, several pathophysiological conditions, including oxidative stress and inflammation, while controlling metabolic dysfunctions and boosting the immunological response. Such broad effects are achieved by the taro health-influencing compounds displaying antitumoral, antimutagenic, immunomodulatory, anti-inflammatory, antioxidant, anti-hyperglycemic, and anti-hyperlipidemic activities. Taro bioactivities are attributed to the combination of tarin, taro-4-I polysaccharide, taro polysaccharides 1 and 2 (TPS-1 and TPS-2), A-1/B-2 α-amylase inhibitors, monogalactosyldiacylglycerols (MGDGs), digalactosyldiacylglycerols (DGDGs), polyphenols, and nonphenolic antioxidants. Most of these compounds have been purified and successfully challenged in vitro and in vivo, proving their involvement in the aforementioned activities. Although these health-promoting effects have been recognized since ancient times, as well as other valuable features of taro for food profit, such as hypo-allergenicity, gluten-free, and carbohydrates with medium-glycemic index, taro crop remains underexploited. The popularization of taro intake should be considered a dietary intervention strategy to be applied to improve the overall health status of the organism and as supportive therapy to manage tumorigenesis.