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- 1From: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy. (Vol. 5) Peer-ReviewedBackground: Linagliptin is an oral antihyperglycemic agent that selectively inhibits the enzyme dipeptidyl peptidase-4 (DPP-4). Inhibition of DPP-4 increases the levels of the incretin hormones glucagon-hke peptide and...