Since its discovery in the 1900s, vitamin E remains an essential micronutrient, playing a pivotal role as an antioxidant and neuroprotection agent. It is a family of compounds categorized into two groups based on chemical structure, i.e. tocopherols and tocotrienols. Although tocopherols are widely recognized due to their abundance in vegetable oils, little was known about tocotrienols. In fact, tocotrienols were found in high amounts in vegetable oils commonly used in Asian countries, including palm oil and rice bran oil. A recent shift in research focus revealed novel nutritional benefits of tocotrienols, beyond tocopherols. These nutritional benefits were extensively studied on a laboratory scale using in vitro and in vivo models. Moving into human studies, numerous clinical trials were conducted using commercial products of tocotrienols, marketed as tocopherol/tocotrienol mixtures. In addition to nutritional benefits, interest in the areas of their bioavailability, safety profile, and analytical methods have attracted global attention. In this chapter, we aim to address the research findings of tocotrienols over the past two decades, as well as the way forward. This review serves as a time-travel capsule, taking us on the journey of tocotrienol development from the bench to the bedside.