Patient considerations and clinical utility of a fixed dose combination of saxagliptin/metformin in the treatment of type 2 diabetes

Derosa, Giuseppe; Maffioli, Pamela

doi:10.2147/dmso.s16361

Cited by 26 publications

(19 citation statements)

References 26 publications

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“…In this regard, the use of FDC may improve convenience of drug therapy, patient's adherence and possibly clinical endpoints [11,12,14]. No sources of funding were used to assist in the preparation of this manuscript.…”

Section: Saxagliptin Versus a Sulfonylureamentioning

confidence: 99%

“…FDC can offer convenience, reduce the pill burden and simplify administration regimens for the patient [11,14].…”

Section: Introductionmentioning

confidence: 99%

“…Fixed-dose combinations (FDC) combining metformin plus sitagliptin and metformin plus vildagliptin are already commercialized, and a metformin extended-release (XR) plus saxagliptin FDC is already on the market in the US (Kombiglyze®). [10][11][12]. A saxagliptin/metformin immediate release FDC will also be available in Europe very soon (Komboglyze®).…”

mentioning

confidence: 99%

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Metformin + saxagliptin for type 2 diabetes

Scheen

2011

Expert Opinion on Pharmacotherapy

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Metformin is considered as the first-line drug therapy for the management of type 2 diabetes.Dipeptidyl peptidase-4 inhibitors, by promoting insulin secretion and reducing glucagon secretion in a glucose-dependent manner, offer new opportunities for oral therapy after failure of metformin. Saxagliptin, a DPP-4 inhibitor, and metformin may be administered together, separately or in fixed-dose combination (FDC) [1,2]. Metformin is considered as the firstline or reference drug because of its favourable overall profile, including its glucose-lowering activity, no weight gain or even slight weight loss, low risk of hypoglycemia and reduction in cardiovascular events [3]. Once metformin fails to maintain glycemic control, there is, however, no consensus about the next pharmacological strategy [1,4] [7] guidelines. Indeed, the addition of a DPP-4 inhibitor to metformin may be a logical option because of the almost similar effect on glycated hemoglobin (HbA1c) compared to the addition of a sulfonylurea or TZD, and because this incretin-based intervention is associated with a excellent tolerance profile, neutral effects on body weight, an absence of hypoglycemic risk and possible positive effects on beta-cell function [3,8].Furthermore, preliminary data suggested that DPP-4 inhibitors may be associated with a reduced rate of cardiovascular events [9], an effect that is currently tested in several prospective clinical trials [6]. Fixed-dose combinations (FDC) combining metformin plus sitagliptin and metformin plus vildagliptin are already commercialized, and a metformin extended-release (XR) plus saxagliptin FDC is already on the market in the US (Kombiglyze®). [10][11][12]. A saxagliptin/metformin immediate release FDC will also be available in Europe very soon (Komboglyze®). Saxagliptin/metformin XR 5? mg/500? mg and saxagliptin/metformin XR 5? mg/1000? mg FDCs were shown to be bioequivalent to individual tablets of saxagliptin and metformin of the same strengths [13]. Of note, however,

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Section: Saxagliptin Versus a Sulfonylureamentioning

confidence: 99%

“…FDC can offer convenience, reduce the pill burden and simplify administration regimens for the patient [11,14].…”

Section: Introductionmentioning

confidence: 99%

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Metformin + saxagliptin for type 2 diabetes

Scheen

2011

Expert Opinion on Pharmacotherapy

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“…The potential for this class of compounds to interfere with immune function is of concern, as an increase in upper respiratory infections has been reported. 27,28 GLP-1 agonists such as exenatide (injected twice daily) and liraglutide (injected once daily) act as an incretin mimetic; they have the structural similarity of, and bind to, the receptor for GLP-1, and they display a broad range of activities relevant to improving glycemic control. They have a much longer half-life after injection than native GLP-1 due to the absence of alanine at position two, which is recognized by DPP-4; this characteristic makes them resistant to DPP-4 cleavage.…”

Section: Current Therapeutic Strategiesmentioning

confidence: 99%

Optimizing glycemic control: clinical utility of exenatide prolonged release injection

Derosa¹,

Maffioli²

2012

RRED

Self Cite

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Abstract:Despite the large variety of antidiabetic drugs currently available, reaching an adequate glycemic control is still difficult. Recently, a new exenatide long acting release (LAR) formulation, which can be administered once a week, has been released. We conducted a review analyzing the clinical utility of this new formulation and its place in antidiabetic therapy, and included the most important studies about exenatide LAR in the latest 10 years. A systematic search strategy was developed to identify randomized controlled trials in both MEDLINE and the Cochrane Register of Controlled Trials. The terms "exenatide," "exenatide long active release," "GLP-1 agonists," "incretins," and "glycemic control" were incorporated into an electronic search strategy that included the Dickersin filter for randomized controlled trials. We concluded that exenatide LAR can be a valid option for the treatment of type 2 diabetes mellitus because it showed to be effective in reducing HbA 1c , and because of its pleiotropic effects, such as the reduction of blood pressure, the improvement of the patient's lipid profile, and the positive effects on body weight and β-cell function. Moreover, exenatide LAR has demonstrated a favorable cost/effectiveness ratio, and its once weekly administration may help to increase patient compliance.

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“…Studies have been conducted regarding dipeptidyl peptidase-4 (DPP-4) inhibitors, which is the newest diabetes drug. [11] It works by reducing the glucagon and blood glucose levels, and it acts at the molecular level, competitively inhibiting the enzyme DPP-4. In addition, it also prolongs and enhances the activity of incretins.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Evaluation of Nanoparticles Prepared by Nano Spray Drying for Stomach Mucoadhesive Drug Delivery

Harsha

2014

Drying Technology

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According to a World Health Organization report published in 2010, 346 million people worldwide have diabetes; in Saudi Arabia, 16.8% of the population has been diagnosed with type 2 disease. Many patients with type 2 diabetes are unable to maintain adequate glycemic control even after receiving recent anti-diabetic drugs. Combination vildagliptin and metformin hydrochloride tablets are available; however, both conventional drugs have a short half-life. The formulation of mucoadhesive nanoparticles for these classes of drugs can be most beneficial, as they release the drug slowly into the gastrointestinal tract and maintain the therapeutic drug concentration. Vildagliptin and metformin hydrochloride were prepared with carbopol (VMCN) using a Buchi Nano Spray Drier B-90. The surface morphology was found to be shriveled (due to surface folding), and the average particle size was 437 nm. The percentage drug yield for vildagliptin and metformin hydrochloride in the nanoparticles was 71%±0.5% and 74%±0.3%, respectively, while the drug content was 84%±0.4% and 89%±0.4%, respectively. Ex vivo studies of mucoadhesion were 6.9±0.3 hours. The percentage of swelling was recorded as 162%±4%. In vivo studies of nanoparticles containing vildagliptin and Downloaded by [Selcuk Universitesi] at 08:11 27 December 2014 2 metformin hydrochloride showed that these values were 3.9% and 4.1% at 12 hours respectively.

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Patient considerations and clinical utility of a fixed dose combination of saxagliptin/metformin in the treatment of type 2 diabetes

Cited by 26 publications

References 26 publications

Metformin + saxagliptin for type 2 diabetes

Metformin + saxagliptin for type 2 diabetes

Optimizing glycemic control: clinical utility of exenatide prolonged release injection

In Vitro and In Vivo Evaluation of Nanoparticles Prepared by Nano Spray Drying for Stomach Mucoadhesive Drug Delivery

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