Saccharum officinarum L., commonly known as sugarcane, is one of the most widely cultivated crops worldwide. In addition to its global value as the main source of sucrose, sugarcane possesses a variety of bioactivities owing to its myriad constituents. Despite the reported health benefits of sugarcane, phytochemical studies in sugarcane are scarce and its bioactive compounds have still not been adequately exploited. This review presents an updated knowledge of the potential bioactivities of sugarcane and its by-products in relation to its phytochemical profiles. We present a thorough understanding of the pharmacological activities of sugarcane and its by-products with a future prospective for maximizing their benefits as valuable medicinal products, in addition to opening new venues in the field of sugarcane industry. Various techniques used for sugarcane juice preservation as major product to maintain its bioactive compounds and stability are presented which in turn could enhance its introduction to a wider market.