This chapter summarizes the entire literature available on the nutritional value and diverse therapeutic potentials Gamma-oryzanol, a nutraceutical obtained from rice brain oil, composed of a mixture of γ - oryzanol, a mixture of ferulic acid esters of phytosterols and triterpenoids, cycloartenyl ferulate, 24-methylenecycloartanyl ferulate, and campesteryl ferulate. In brief, the review covers the aspects such as the antioxidant mechanisms, effects on immune system, lipid disorders, diabetes, obesity and inflammation with the details of preclinical experiments, models and observations. Among the other highlights are the hepatoprotective, neuroprotective role in various neurological disorders such as Alzheimer’s, anxiety, Parkinson’s disease and wound healing effects. An overview of the sources, chemistry, physicochemical properties, pharmacokinetics and toxicity studies are also included.