Type 2 diabetes mellitus has reached epidemic proportions in the United States. Cardiovascular morbidity and mortality are particularly high in this patient population. Improved glucose control, especially early in the course of diabetes, can slow or prevent complications, preserve β-cell function, and improve long-term outcomes. Within the last decade, new treatments and glycemic goals have created an opportunity to better manage this prevalent, chronic disease. Defects of insulin resistance and deficiency leading to type 2 diabetes can now be directly targeted with available therapies. In addition to diet and exercise, oral treatment options have been broadened, with both insulin secretagogues and insulin sensitizers. These advances in treatment options make glycemic control an obtainable target, and therefore should improve overall morbidity and mortality for patients. This paper will review currently available oral therapies, with a focus on the unique attributes of the insulin sensitizers for patients with type 2 diabetes.