A comprehensive consensus has been reached that vascular endothelial growth factor (VEGF) plays an important role in the pathogenesis of diabetic retinopathy (DR). Theoretically, a block to any step of the VEGF signal pathway may interrupt the biological function of VEGF, so that the therapeutic effect can be achieved. This paper reviews the mechanisms and efficacies of different anti-VEGF drugs, either in clinical trial or laboratory research phase, that have been used in the treatment of DR.