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Sitagliptin: A Review of Its Use in Patients with Type 2 Diabetes Mellitus

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Abstract

Sitagliptin (Januvia®, Xelevia™, Glactiv®, Tesavel®) 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 of sitagliptin/metformin), or add-on therapy to metformin or to other antihyperglycaemic drugs, with or without metformin. The primary endpoint of the clinical trials was the reduction from baseline in glycosylated haemoglobin (HbA1c), although sitagliptin also showed beneficial effects for other endpoints, such as the proportion of patients who achieved target HbA1c, and reductions from baseline in fasting plasma glucose (FPG) levels and 2-h postprandial glucose (PPG) levels. Sitagliptin was generally well tolerated in clinical trials, had a low risk of hypoglycaemia (although this depends on background therapy) and had a neutral effect on body weight. Despite concerns regarding a possible increased risk of rare pancreatic adverse events (e.g. pancreatitis) with glucagon-like peptide-1 (GLP-1)-based therapies, such as GLP-1 receptor agonists and DPP-4 inhibitors, no causal association has been found; regulators in Europe recently conducted a review of available data, concluding that there is little evidence that these drugs could cause pancreatic inflammation or pancreatic cancer. A similar review is planned in the USA and postmarketing surveillance will continue. Thus, oral sitagliptin is an effective and generally well tolerated treatment option for the management of patients with type 2 diabetes.

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Disclosure

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes based on any comments received were made by the author on the basis of scientific and editorial merit.

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    Greg L. Plosker

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The manuscript was reviewed by: D.T. Eurich, Department of Public Health, School of Public Health, University of Alberta, Edmonton, AB, Canada; I. Raz, Diabetes Unit, Department of Internal Medicine, Hadassah University Hospital, Jerusalem, Israel; A.J. Scheen, Division of Diabetes, Nutrition and Metabolic Disorders and Clinical Pharmacology Unit, CHU Liège, University of Liège, Liège, Belgium.

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Plosker, G.L. Sitagliptin: A Review of Its Use in Patients with Type 2 Diabetes Mellitus. Drugs 74, 223–242 (2014). https://doi.org/10.1007/s40265-013-0169-1

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