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Sitagliptin

A Review of its Use in the Management of Type 2 Diabetes Mellitus

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Abstract

Sitagliptin (Januvia™, Glactiv®, Tesavel®) is a dipeptidyl peptidase-4 inhibitor indicated for the treatment of type 2 diabetes mellitus. Oral sitagliptin as mono-therapy or combination therapy was generally well tolerated and improved glycaemic control in well designed clinical trials in patients with type 2 diabetes. Glycosylated haemoglobin (HbA1c) levels were significantly reduced with sitagliptin monotherapy relative to voglibose monotherapy or placebo, and with sitagliptin as initial combination therapy with metformin or pioglitazone relative to monotherapy with these agents or placebo. Moreover, sitagliptin monotherapy was noninferior to metformin monotherapy in terms of the reduction in HbA1c levels. Significant reductions in HbA1c levels, relative to background therapy, were also observed with sitagliptin add-on therapy to ongoing treatment with thiazolidinediones, sulfonylureas or insulin with or without metformin, or metformin alone. In terms of the reduction in HbA1c levels as add-on treatment to metformin, sitagliptin was noninferior to glipizide and generally did not differ from rosiglitazone, and as add-on treatment to pioglitazone, it did not differ significantly from metformin. Sitagliptin had a low risk of hypoglycaemia (except when used in combination with agents that may be associated with hypoglycaemia, such as sulfonylureas or insulin) and was generally weight-neutral. Although additional comparative data and longer-term studies with glycaemic and clinical outcomes are required to definitively position sitagliptin relative to other antihyperglycaemic agents, current evidence suggests that it is a useful treatment option for patients with type 2 diabetes, with potential advantages including oral administration, a generally weight-neutral effect and a low risk of hypoglycaemia.

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Correspondence to Sohita Dhillon.

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Various sections of the manuscript reviewed by: B. Ahren, Department of Medicine, Lund University B11 Biomedical Centre, Lund University, Lund, Sweden; A. Barnett, Division of Clinical and Experimental Medicine, University of Birmingham and Heart of England National Health Service Foundation Trust, Birmingham, United Kingdom; J. Eriksson, Department of General Practice & Primary Health Care and Helsinki University Central Hospital Unit of General Practice Helsinki, University of Helsinki, Helsinki, Finland; V. Mohan, Diabetology, Dr. Mohan’s Diabetes Specialities Centre & Madras Diabetes Research Foundation, Gopalapuram, Tamil Nadu, India; P. Nilsson, Section of Medicine, Department of Clinical Sciences, University Hospital, Lund University, Malmo, Sweden; I. Raz, Diabetes Unit, Internal Medicine Department, Hadassah Hebrew University Hospital, Jerusalem, Israel; B. Yeap, School of Medicine and Pharmacology, Fremantle Hospital, University of Western Australia, Fremantle, Western Australia, Australia.

Data Selection

Sources: Medical literature published in any language since 1980 on ‘sitagliptin’, identified using MEDLINE and EMBASE, supplemented by AdisBase (a proprietary database). Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug.

Search strategy: MEDLINE, EMBASE and AdisBase search terms were ‘sitagliptin’ and (‘type-2 diabetes mellitus’ or ‘diabetes mellitus type 2’ or ‘non insulin dependent diabetes mellitus’). Searches were last updated 23 February 2010.

Selection: Studies in patients with type 2 diabetes mellitus who received sitagliptin. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.

Index terms: Sitagliptin, dipeptidylpeptidase-4 inhibitor, type 2 diabetes mellitus, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability.

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Dhillon, S. Sitagliptin. Drugs 70, 489–512 (2010). https://doi.org/10.2165/11203790-000000000-00000

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