<p>Sugarcane (<i>Saccharum officinarum L.</i>), a significant perennial grass of the Poaceae family, thrives in warm climates globally. It is processed to produce not only sucrose but also valuable by-products like molasses and bagasse. Rich in diverse components such as fatty acids, alcohols, phytosterols, higher terpenoids, flavonoids, O- and C- glycosides, and phenolic acids, sugarcane possesses multiple pharmacological activities, including antioxidant, antibacterial, anticancer, and antidiabetic properties. However, research on sugarcane phytochemicals remains limited, and as their bioactive potential has not been fully exploited, many of these compounds are simply discarded in molasses, filter cake, or bagasse leachate. Furthermore, the pharmacological mechanisms of these bioactives remain largely uncharted. Consequently, the very occurrence of these uncharacterized metabolites in industrial by-products positions sugarcane as an underexploited reservoir of bioactives whose systematic profiling and mechanism-based validation should be prioritized in future phytochemical and pharmacological research.</p>