Nateglinide: a new rapid-acting insulinotropic agent.

The United Kingdom Prospective Diabetes Study has shown that tight glycaemic control significantly reduces microvascular complications in Type 2 diabetes, but the effects on macrovascular complications were less impressive and did not reach statistical significance. Epidemiological studies have shown that post-prandial hyperglycaemia, rather than fasting hyperglycaemia, is more closely related to cardiovascular complications. It is, therefore, possible that previous studies may have overlooked the possible benefits of tight control of post-prandial hyperglycaemia as an important factor in reducing the cardiovascular mortality. Nateglinide is a novel D-phenylalanine derivative that inhibits ATP-sensitive K+ channels in pancreatic beta-cells in the presence of glucose and thereby restores first phase insulin response in patients with Type 2 diabetes. This helps in reducing post-prandial glucose excursion. Combination studies with metformin have shown it to be effective in controlling hyperglycaemia. While metformin reduces the basal plasma glucose, nateglinide helps in controlling post-prandial peaks. Nateglinide provides a new therapeutic option for treating Type 2 diabetes by specifically targeting post-prandial hyperglycaemia.