Considering the preference of platinum for S-donor ligands, it is not surprising that sulfur-containing compounds make up the majority of potential cytoprotective agents for platinum-based therapy explored for their applicability thus far. With respect to platinum-based anticancer chemotherapy, glutathione is known to act as a detoxifying agent. So far, amifostine is the only cytoprotective agent which has received approval for platinum cancer therapy. Intestinal-type alkaline phosphatase, a major isoenzyme involved in the conversion of amifostine, is present in high abundance in several normal tissues in contrast to malignant tissues of the same organs. The role of glutathione in protecting DNA by scavenging intracellular cisplatin has recently been re-evaluated and confirmed by cell culture experiments employing blocking agents which drastically reduce the number of thiol functions available for platinum binding. α-Lipoic acid is a physiological antioxidant capable of metal binding, oxygen radical scavenging and regenerating endogenous antioxidants such as vitamin E, vitamin C and glutathione.