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McGraw-Hill / Lange rxlist.com (Glyset ®) Keywords DPP-4 Inhibitors Sitagliptin Trade Name: Januvia ® Drug Class: oral hypoglycemics Mechanism of Action: An inhibitor of dipeptidyl peptidase-4 (DPP-4), a protease that degrades the incretin GLP-1 Incretins are hormones released from the GI tract in response to nutrient ingestion Incretins potentiate glucose-stimulated insulin secretion from beta cells in the pancreas As a result of inhibiting DPP-4, increased or prolonged GLP-1 levels are able to potentiate the secretion of insulin by the pancreas The effect produced by DPP-4 inhibitors is dependent on endogenous GLP-1 levels, and produce a modest effect on GLP-1 activity compared to giving GLP-1 receptor agonists (hence DPP-4 inhibitors do not have the same impact to produce weight loss as GLP-1 agonists)