Diabetes mellitus (DM) is a disorder of abnormal glucose metabolism resulting primarily from insulin resistance and relative insulin deficiency and characterized by hyperglycemia causing significant short-and long-term complications. Type 2 diabetes mellitus (T2DM) contributes to more than 90% of cases of diabetes. Obesity, sedentary lifestyles, and consumption of very high-caloric meals are thought to be the primary triggering factors causing T2DM in genetically predisposed individuals. Although treatment of hyperglycemia plays a key role in the management, therapies directed at other comorbid conditions, such as dyslipidemia, hypertension, hypercoagulability, obesity, and insulin resistance, have also been a major focus of research and therapy. DM is rising to an epidemic proportion globally, and it is, indeed, one of the most challenging public health problems in the 21st century. According to 2011 statistics, there were approximately 366 million diabetes cases worldwide, and this figure would probably increase to 552 million by 2030. Long-term complications from high blood sugar include coronary artery disease, cerebrovascular events, peripheral arterial diseases leading to amputation, retinopathy, nephropathy leading to end-stage renal disease requiring hemodialysis and transplantation, and neuropathy. The acute complication of T2DM includes drug-induced hypoglycemia, hyperosmolar hyperglycemic state, and although uncommon, ketoacidosis. Diabetes care requires a comprehensive and multidisciplinary approach to delay the progression to acute as well as chronic and debilitating long-term complications. This approach requires the thorough understanding of the pathophysiology of hyperglycemia and impact of various risk factors and comorbidities, careful selection of antihyperglycemic agents, active and frequent participation of diabetes educator, and involvement of multidisciplinary team. The objective of this review is to highlight recent trends in hormonal treatment and to explore new and innovative therapeutic modalities in the management of T2DM.