Nonalcoholic fatty liver disease (NAFLD) is an emerging epidemic in Western societies, and therapeutic modalities to treat this condition are needed desperately. Most early treatment studies tended to focus on improvement in the serum aminotransferases. Presently, treatment of NAFLD is aimed at improving the underlying steatosis, necroinflammatory activity, and fibrosis because elevations of the aminotransferases may not accurately reflect these important histologic endpoints. Unfortunately, well-defined treatment options are few,which is largely due to limited experience reported in small, prospective pilot trials. This article focuses on the various therapeutic agents that have been evaluated in the treatment of NAFLD and their efficacy as well as their limitations.