Great hope has been given to micronutrients as anticancer agents, since they present natural compounds with beneficial effects for normal cells and tissues. One of these is vitamin E (VE), an antioxidant and an essential component of biological membranes and circulating lipoproteins. In spite of a number of epidemiological and intervention studies, little or no correlation between VE intake and incidence of cancer has been found. Recent reports have identified a redox-silent analogue of VE, alpha-tocopheryl succinate (alpha-TOS), as a potent anticancer agent with a unique structure and pharmacokinetics in vivo. alpha-TOS is highly selective for malignant cells, inducing them into apoptotic death largely via the mitochondrial route. The molecule of alpha-TOS may be modified so that analogues with higher activity are generated. Finally, alpha-TOS and similar agents are metabolised to VE, thereby yielding a compound with a secondary beneficial activity. Thus, alpha-TOS epitomises a group of novel compounds that hold substantial promise as future anticancer drugs. The reasons for this optimistic notion are discussed in the following paragraphs.