Many clinical studies have implicated the importance of vascular endothelial growth factor (VEGF) in the pathogenesis of diabetic retinopathy(DR). VEGF inhibitors were combined with VEGF molecules to counteract its function. There are achievements in the therapy for treating neovascularization and vascular leak-age of DR. This article makes a review in the classification,mechanism of function,safety as well as applied development of VEGF inhibitors for DR.