Lung cancer is the leading cancer killer in the United States today. The current methods of treatment, radiation and various chemotherapies, have been used with some success; however, early detection remains the key to successful therapy. Current clinical trials indicate that an improvement of available therapies is needed. Consequently, the development of new approaches to treatment is foremost in the minds of researchers. Advances in molecular medicine have produced new drugs that can protect normal cells from chemotherapy-induced toxicities, resulting in enhanced drug delivery with few dose reductions. This review will discuss some of the advances that have been made in understanding the molecular biology of lung cancer as well as the current and most promising methods of treatment used for various forms of lung cancer. The potential contribution of cytoprotectors to enhance the safety and effectiveness of these therapies will be examined.