Type 2 diabetes is a complex disease characterized by a dual defect of insulin secretion and insulin sensitivity, which may vary from patient to patient, but also along the natural history of the disease in a particular patient. Besides the lifestyle changes, the treatment strategy comprises the administration of agents that promote insulin secretion and/or that improve insulin sensitivity. Drugs facilitating weight loss also improve glucose control by reducing insulin resistance. A global approach should be recommended to reduce the high cardiovascular risk of diabetic patients. The present article aims at summarizing our contribution to the development of drugs designed for the treatment of type 2 diabetes.