Diabetes is an increasingly common metabolic disorder with high comorbidity and societal and personal costs. Insulin replacement therapy is limited by a lack of oral bioavailability. Recent studies suggest vanadium has therapeutic potential. A newly synthesized complex between oxidovanadium (IV) and orotic acid (OAH3), [(OAH1)(VO)(NH3)2].3H2O, was characterized using spectroscopic and thermogravimetric techniques. In vivo potential was assessed in a streptozocin-induced rat model of diabetes. OAH3 acts as a bidentate ligand in the formation of the dark green, crystalline oxidovanadium (IV) complex in a square pyramidal configuration. Treatment with oxidovanadium (IV)-orotate in vivo significantly improved many biochemical parameters with minimal toxicity and restored pancreatic and hepatic histology. The results of the present work describe a safe, new compound for the treatment of diabetes.