Taspoglutide. GLP-1 analogue, Treatment of diabetes.

Incretin agonists and analogues are receiving increasing attention as potential antidiabetic agents due to their ability to stimulate insulin secretion only during hyperglycemic states. Exploitation of the incretin effect reduces the risk of rebound hypoglycemia that accompanies many antidiabetic treatments. Taspoglutide (R-1583, BIM-51077, ITM-077) is a long-acting glucagon-like peptide 1 (GLP-1) analogue that shows promise for the treatment of type 2 diabetes. In addition to having enhanced resistance to enzymatic degradation by the protease dipeptidyl peptidase 4 (DPP4), clinical studies have shown that taspoglutide increases insulin levels and lowers glycemia. Phase II trials have also demonstrated that weekly administration of a slow-release formulation was associated with enhanced glycemic control, reduced body weight and improved beta-cell function. Taspoglutide is generally well tolerated, with mild gastrointestinal symptoms being the most commonly reported adverse events. Several phase III clinical trials of this novel GLP-1 analogue are under way.