SITAGLIPTIN- A COMPREHENSIVE REVIEW

Sitagliptin is an orally administered, potent, and highly selective inhibitor of dipeptidyl
peptidase-4 (DPP-4) and was the first agent of its class to be approved for use in the
management of adults with type 2 diabetes. Numerous randomized placebo- or active
comparator-controlled trials have demonstrated the efficacy of sitagliptin in terms of
improving glycaemic control in patients with type 2 diabetes, including its use as
monotherapy, initial combination therapy (usually with fixed-dose combinations
ofsitagliptin/metformin), or add-on therapy to metformin or other antihyperglycaemic drugs,
with or without metformin. Sitagliptin was generally well tolerated in clinical trials, had a low
risk of hypoglycemia (although this depends on background therapy), and had a neutral
effect on body weight.It stimulates insulin secretion when hyperglycemia is present and
inhibits glucagon secretion. In clinical studies, it is weight neutral. This article gives an
overview of the mechanism of action, the pharmacology, and the clinical efficacy and safety
of sitagliptin in type 2 diabetes therapy.