Abstract: Vitamin E group of vitamins consist of varying proportions of tocotrienols based upon the natural sources. The major health benefits are associated by the tocotrienols while their isomers, tocopherols, exert antioxidant properties. The two subgroups of vitamin E share many distinct biological activities. In vitro and in vivo mice studies suggested that tocotrienols are critical in mediating anticancer, anti-inflammatory, lipid lowering, radio protection and neuro protection functions. Numerous human studies showed the evidence that tocotrienols can be supplemented to reach high concentrations in whole blood but desired pharmacological activity is questionable. Bioavailability and further bio distribution depends upon the food in stomach, health condition of the patient and other metabolizing and excretion parameters. In this current review, we have a discussion about few human studies that were conducted to show the value of tocotrienol supplementation in cancer prevention and treatment.