Gliptins: DPP‐4 inhibitors to treat type 2 diabetes

Gliptins represent an emerging new class of oral agents to treat type 2 diabetes. They act by inhibiting the enzyme dipeptidyl peptidase‐4 (DPP‐4). This enzyme inactivates the incretin hormones glucagon‐like peptide‐1 (GLP‐1) and glucose‐dependent insulinotropic polypeptide (GIP). These hormones are released from the intestine during a meal and act on the pancreas to increase nutrient‐stimulated insulin secretion. Thus DPP‐4 inhibitors serve as incretin enhancers; they delay inactivation of GLP‐1 and GIP, increasing the insulin response to a meal, which improves glycaemic control. This therapeutic approach carries a low risk of interprandial hypoglycaemia and does not cause weight gain. The first gliptin, sitagliptin (Januvia), was introduced in the UK in April 2007 as ‘add‐on’ therapy for patients with type 2 diabetes inadequately controlled with metformin or a thiazolidinedione. Other gliptins, notably vildagliptin (Galvus), saxagliptin and alogliptin are advanced in clinical development. Copyright © 2007 John Wiley & Sons, Ltd.