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Vildagliptin

A Review of its Use in Type 2 Diabetes Mellitus

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Abstract

Vildagliptin (Galvus®, Jalra®, Xiliarx®) is an orally administered dipeptidyl peptidase-4 (DPP-4) inhibitor. In patients with type 2 diabetes mellitus, vildagliptin 50mg twice daily is indicated for use in combination with metformin or a thiazolidinedione, and vildagliptin 50mg once daily is indicated for use in combination with a sulfonylurea. A fixed-dose combination of vildagliptin/metformin (Eucreas®, Icandra®, Zomarist®) is also available. This article reviews the clinical efficacy and tolerability of vildagliptin in patients with type 2 diabetes, as well as summarizing its pharmacological properties.

The efficacy of monotherapy or combination therapy with oral vildagliptin in patients with type 2 diabetes has been examined in randomized, double-blind, multicentre trials.

Monotherapy with vildagliptin 50mg once or twice daily reduced glycosylated haemoglobin (HbA1c) from baseline to a significantly greater extent than placebo, according to the results of 12- to 52-week trials in patients with type 2 diabetes. In terms of the reduction from baseline in HbA1c seen in active comparator trials of 12–104 weeks' duration, the noninferiority of vildagliptin 50mg twice daily was established versus acarbose or rosiglitazone, the noninferiority of vildagliptin 100mg once daily (an off-label dosage) versus metformin was established in elderly patients and vildagliptin 50mg twice daily was more effective than voglibose; however, the noninferiority of vildagliptin 50mg twice daily versus metformin or gliclazide was not established in two other trials.

Combination therapy with vildagliptin 50mg twice daily plus metformin improved HbA1c to a significantly greater extent than monotherapy with metformin and/or vildagliptin alone in patients with type 2 diabetes whose disease was inadequately controlled by metformin monotherapy or who were treatment naive, according to the results of 12- or 24-week trials. In addition, vildagliptin 50mg twice daily plus metformin demonstrated noninferiority to pioglitazone plus metformin, glimepiride plus metformin or gliclazide plus metformin in terms of the change from baseline in HbA1c after 24 or 52 weeks' therapy in patients with inadequately controlled type 2 diabetes. The addition of vildagliptin 50mg twice daily to pioglitazone or vildagliptin 50mg once daily to glimepiride improved HbA1c to a significantly greater extent than a thiazolidinedione or glimepiride alone in patients with type 2 diabetes whose disease was inadequately controlled, according to the results of 24-week trials.

Oral vildagliptin 50 mg once or twice daily was generally well tolerated in patients with type 2 diabetes. In particular, vildagliptin was associated with a low risk of hypoglycaemia and was weight neutral. Increases in transaminase levels were sometimes observed with a vildagliptin dosage of 100mg once daily in clinical trials, and liver function should be monitored in patients receiving vildagliptin. However, meta-analyses of clinical trial data suggested that vildagliptin 50mg once or twice daily was not associated with an increased risk of hepatic adverse events, transaminase elevations ≥3 × the upper limit of normal, pancreatitis, cardiovascular or cerebrovascular events, infections or skin-related toxicity.

In conclusion, vildagliptin is an important option for use in combination with metformin, a sulfonylurea or a thiazolidinedione in patients with type 2 diabetes who require combination therapy.

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Authors and Affiliations

  1. Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, Auckland, 0754, New Zealand

    Gillian M. Keating

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Correspondence to Gillian M. Keating.

Additional information

Various sections of the manuscript reviewed by: D. Cucinotta, Azienda Ospedaliera Universitaria Policlinico, Dipartimento di Medicina Interna, Messina, Italy; D.A. D’Alessio, Division of Endocrinology, Diabetes and Metabolism, University of Cincinnati, Cincinnati VA Medical Center, Cincinnati, Ohio, USA; P.M. Nilsson, Department of Clinical Sciences, Lund University, University Hospital, Malmö, Sweden; A. Penfornis, Service d’Endocrinologie Metabolisme et Diabetologie Nutrition, Hôpital Jean Minjoz, Besancon, France; A.E. Pontiroli, Dipartimento di Medicina, Chirurgia e Odontoiatria, Università degli Studi di Milano, 2a Divisione di Medicina Interna, Ospedale San Paolo, Milan, Italy; H. Schatz, University Clinic Bergmannsheil, Ruhr-University Bochum, Bochum, Germany; A.J. Scheen, University of Liège, Department of Medicine, CHU Sart Tilman, Liège, Belgium.

Data Selection

Sources: Medical literature published in any language since 1980 on ‘vildagliptin’, 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 ‘vildagliptin’ and (‘type-2 diabetes mellitus’ or ‘diabetes mellitus type 2’ or ‘non insulin dependent diabetes mellitus’). Searches were last updated 11 October 2010.

Selection: Studies in patients with type 2 diabetes mellitus who received vildagliptin. 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: Vildagliptin, type 2 diabetes mellitus, pharmacodynamics, pharmacokinetics, therapeutic use.

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Keating, G.M. Vildagliptin. Drugs 70, 2089–2112 (2010). https://doi.org/10.2165/11206370-000000000-00000

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