Current treatments and treatment regimens include combinations of oral antidiabetic drugs (OADs), antihypertensive medications, and antidyslipidemic agents, but these have been less than successful in managing their respective disease targets with clinical goals. Measures such as screening and intensive life-style modification can help to delay the onset of diabetes in at-risk individuals, and stringent glycemic control with pharmacotherapy may improve outcomes. To manage the type 2 diabetes epidemic effectively, however, agents that can effectively and durably controls glycemia while providing pleiotropic benefits (e.g. blood pressure reduction) are required.