Summary: Nonalcoholic fatty liver disease (NAFLD), being a component of metabolic syndrome, is emerging as the most prevalent chronic liver disorder. Nonalcoholic steatohepatitis (NASH) is the subtype of NAFLD having the potential to progress to advanced liver damage. The disease progression is a complex process implicating many parallel pathogenic factors. The current mainstay of treatment is dietary and lifestyle changes aimed at reducing body weight, and the optimization of the management of individual components of metabolic syndrome. Vitamin E and pioglitazone showed partial efficacy in the treatment of NASH, but their safety in chronic use has been questioned. This review discusses the therapeutic significance of antidiabetic drugs, hypolipidemic agents, ursodeoxycholic acid, anti-oxidative preparations and essential phospholipids for NAFLD. At present there are several emerging drugs being assessed in phase 3 trials. With respect to the pharmacological mechanism of action, they belong to four classes (FXR agonists, CCR2/CCR5 antagonists, ASK1 inhibitors, and PPAR a/d agonists). Along with growing knowledge on the pathogenesis of NASH, there is increasing awareness of the necessity to use combinational therapies engaging different molecular targets, with different choices according to disease stage.