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Glutathione is quantitatively the most important antioxidant and scavenger. In addition it has a number of important functions in amino acid transport across membranes, in protein synthesis and degradation, in gene regulation and in cellular redox regulation. It becomes more and more evident that depletion of glutathione is associated with states of severe diseases. From this perspective, the possibility of manipulating the availability of glutathione becomes a very attractive form of treatment. In this review, new insights into pathophysiology and the regulation of glutathione metabolism, in addition to effects of precursors to and stimulants of glutathione synthesis, are covered. It is very likely that glutathione precursors will soon be an important pharmacological tool for treatment in a number of diseased states.