The Medical Letter on Drugs and Therapeutics
Sitagliptin (Januvia) for Type 2 Diabetes
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Sitagliptin phosphate (Januvia – Merck) is the first dipeptidyl-peptidase-4 (DPP-4) inhibitor to be marketed for treatment of type 2 diabetes. It has been approved by the FDA for oral use as monotherapy or in combination with metformin (Glucophage, and others), pioglitazone (Actos) or rosiglitazone (Avandia).

MECHANISM OF ACTION — Sitagliptin inhibits DPP- 4, the enzyme responsible for inactivation and degradation of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulin-otropic polypeptide (GIP). These hormones are released by the intestine throughout the day, with an increase postprandially; they potentiate insulin synthesis and release by pancreatic beta cells and decrease glucagon production by pancreatic alpha cells in a glucose-dependent manner, lowering serum glucose concentrations. Exenatide (Byetta), an injectable incretin mimetic, was approved by ... more      

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Title: Sitagliptin (Januvia) for Type 2 Diabetes
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