Diabetes Mellitus (T2DM) is characterized by chronic hyperglycemia with disturbance in carbohydrate, lipid, and protein metabolism due to insulin resistance and beta cell dysfunction. Epidemiological studies have confirmed a global pandemic of T2DM, which has created an enormous burden on society, with regard to morbidity, mortality, and health care expenditures. Life style modifications are fundamental not only in early stages of disease management but need to be intensified as disease progresses. United Kingdom Prospective Diabetes Study (UKPDS) has demonstrated the progressive nature of T2DM, and as disease progresses, a combination agents-oral antidiabetic drugs (OAD) and insulin-are needed in order to maintain good sugar control. The general consensus of HbA1c target for most patients is less than 7%, and various guidelines and algorithms have provided guidance in patient management to keep patient at goal. As our understanding of pathophysiological defects advances, targeting treatment at underlying defects not only enables us to achieve HbA1c goal but also reduces morbidities, mortalities, and progression of the disease. Traditional oral agents like metformin and sulfonylureas have failed to arrest the progression of T2DM.