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**Piragliatin** is a small molecule glucokinase activator developed by Roche for the treatment of type 2 diabetes mellitus. It enhances glucokinase activity in pancreatic β-cells and hepatocytes, increasing glucose-stimulated insulin secretion, improving β-cell sensitivity to glucose, suppressing hepatic glucose output, and promoting glucose uptake, thereby lowering fasting and postprandial plasma glucose levels in patients with mild type 2 diabetes. Clinical studies, including phase Ib and II trials, demonstrated dose-dependent glucose-lowering effects with oral administration, though development appears to have been discontinued.
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