Rice (Oryza sativa seeds – Poaceae) is considered one of the most important grains, as it is consumed by the half of the world population. Various by-products of the rice industry, such as rice bran and the rice bran oil (RBO), have recently attracted much attention from both academia and industry due to their high content of high added-value phytochemicals such as tocopherols/tocotrienols, carotenoids, and γ-oryzanol, of nutritional, pharmaceutical, and cosmetic interest. In particular, γ-oryzanol, a mixture of triterpene alcohol and phytosterol ferulates, is characterized by a wide spectrum of health-beneficial effects, including anticarginogenic, anti-inflammatory, antihyperlipidemic, and neuroprotective, which are mainly attributed to its significant antioxidant capacity. This chapter presents the chemical characteristics of γ-oryzanol components, their classification and biosynthesis, as well as an overview regarding the traditional and modern methods for γ-oryzanol extraction, isolation, analysis, and identification. A summary regarding its biological profile and applications is also provided.