As a chronic disease encompassing a wide spectrum of liver-related histologic damage, nonalcoholic fatty liver disease (NAFLD) is becoming a global epidemic with significant impacts on all-cause morbidity and mortality. Insulin resistance and type 2 diabetes mellitus predispose individuals to NAFLD and related complications. Therefore, timely intervention with anti-diabetic medications may prevent and delay the development of NAFLD or have a therapeutic implication. The focus of this review is to evaluate the evidence supporting the efficacy of anti-diabetic medications in the treatment of NAFLD. While many of these anti-diabetic agents have shown to improve biochemical parameters, their effect on hepatic histology is limited. Among anti-diabetic medications, only thiazolidinediones and glucagon-like peptide-1 receptor agonists demonstrate significant improvement in hepatic histology.