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Vildagliptin

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https://www.readbyqxmd.com/read/28532406/the-addition-of-vildagliptin-to-metformin-prevents-the-elevation-of-interleukin-1%C3%A3-in-patients-with-type-2-diabetes-and-coronary-artery-disease-a-prospective-randomized-open-label-study
#1
Arwa Younis, Dana Eskenazi, Ronen Goldkorn, Jonathan Leor, Nili Naftali-Shani, Enrique Z Fisman, Alexander Tenenbaum, Ilan Goldenberg, Robert Klempfner
BACKGROUND: Patients with type 2 diabetes present with an accelerated atherosclerotic process. Animal evidence indicates that dipeptidyl peptidase-4 inhibitors (gliptins) have anti-inflammatory and anti-atherosclerotic effects, yet clinical data are scarcely available. DESIGN AND METHODS: A prospective, randomized, open-label study was performed in 60 patients with coronary artery disease (CAD) and type 2 diabetes, who participated in a cardiac rehabilitation program...
May 22, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28526921/glp-1-signalling-compensates-for-impaired-insulin-signalling-in-regulating-beta-cell-proliferation-in-%C3%AE-irko-mice
#2
Dan Kawamori, Jun Shirakawa, Chong Wee Liew, Jiang Hu, Tomoaki Morioka, Alokesh Duttaroy, Bryan Burkey, Rohit N Kulkarni
AIMS/HYPOTHESIS: We aimed to investigate potential interactions between insulin and glucagon-like peptide (GLP)-1 signalling pathways in the regulation of beta cell-cycle dynamics in vivo, in the context of the therapeutic potential of GLP-1 to modulate impaired beta cell function. METHODS: Beta cell-specific insulin receptor knockout (βIRKO) mice, which exhibit beta cell dysfunction and an age-dependent decrease in beta cell mass, were treated with the dipeptidyl peptidase-4 inhibitor vildagliptin...
May 20, 2017: Diabetologia
https://www.readbyqxmd.com/read/28515791/vildagliptin-has-the-same-safety-profile-as-a-sulfonylurea-on-bone-metabolism-and-bone-mineral-density-in-post-menopausal-women-with-type-2-diabetes-a-randomized-controlled-trial
#3
Andre Gustavo Daher Vianna, Claudio Silva de Lacerda, Luciana Muniz Pechmann, Michelle Garcia Polesel, Emerson Cestari Marino, Victoria Zeghbi Cochenski Borba, Fellype de Carvalho Barreto
BACKGROUND: Several antidiabetic therapies affect bone metabolism. Sulfonylureas have the lowest impact on bone among oral antidiabetics. The objective of this study is to compare the effects of vildagliptin and gliclazide modified release (MR) on bone turnover markers (BTMs) and bone mineral density (BMD) in postmenopausal women with uncontrolled type 2 diabetes (T2D). METHODS: Forty-two postmenopausal women with uncontrolled T2D were randomly allocated into vildagliptin or gliclazide MR (control) groups...
2017: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/28493402/development-and-validation-of-hplc-ms-ms-method-for-the-determination-of-lixivaptan-in-mouse-plasma-and-its-application-in-a-pharmacokinetic-study
#4
Adnan A Khady, Haithem Alrabiah, Mohamed W Attwa, Sabray Attia, Gamal A E Mostafa
The aim of the present study was to develop a simple, sensitive, and accurate liquid chromatography-electrospray ionization tandem mass spectrometry (ESI-MS/MS) method for the determination of lixivaptan (LIX) in mouse plasma by using vildagliptin as the internal standard (IS). A precipitation procedure was used for the extraction of LIX and vildagliptin from mouse plasma. Chromatographic separation of LIX was achieved using a C18 analytical column (50 mm × 2.1 mm, 1.8 µm) at 25 °C. The mobile phase comprised of acetonitrile and ammonium formate (10 mM, pH 3...
May 10, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28489279/dipeptidyl-peptidase-dpp-4-inhibitors-and-glucagon-like-peptide-glp-1-analogues-for-prevention-or-delay-of-type-2-diabetes-mellitus-and-its-associated-complications-in-people-at-increased-risk-for-the-development-of-type-2-diabetes-mellitus
#5
REVIEW
Bianca Hemmingsen, David P Sonne, Maria-Inti Metzendorf, Bernd Richter
BACKGROUND: The projected rise in the incidence of type 2 diabetes mellitus (T2DM) could develop into a substantial health problem worldwide. Whether dipeptidyl-peptidase (DPP)-4 inhibitors or glucagon-like peptide (GLP)-1 analogues are able to prevent or delay T2DM and its associated complications in people at risk for the development of T2DM is unknown. OBJECTIVES: To assess the effects of DPP-4 inhibitors and GLP-1 analogues on the prevention or delay of T2DM and its associated complications in people with impaired glucose tolerance, impaired fasting blood glucose, moderately elevated glycosylated haemoglobin A1c (HbA1c) or any combination of these...
May 10, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28471499/efficacy-and-safety-of-single-drug-or-double-drug-antidiabetic-regimens-in-the-treatment-of-type-2-diabetes-mellitus-a-network-meta-analysis
#6
Xi-Ling Yang, Mi-Ma Duo-Ji, Zi-Wen Long
A network meta-analysis was performed in order compare the efficacy and safety of single-drug or double-drug antidiabetic regimens in the treatment of type 2 diabetes mellitus (T2DM). PubMed and Cochrane Library searches were conducted since inception to February 2017. Randomized controlled trials (RCTs) of different antidiabetic regimens in the treatment of T2DM were included in this study. Direct and indirect evidences were combined to calculate the odds ratio (OR) or weighted mean difference (WMD) and its 95% confidence interval (95% CI), and in order to draw the surface under the cumulative ranking curves (SUCRA)...
May 4, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28432754/intraclass-differences-in-the-risk-of-hospitalisazion-for-heart-failure-among-type-2-diabetic-patients-initiating-a-dipeptydil-peptidase-4-inhibitor-or-a-sulphonylurea-results-from-the-osmed-health-db-registry
#7
Gian Paolo Fadini, Stefania Saragoni, Pierluigi Russo, Luca Degli Esposti, Saula Vigili de Kreutzenberg, Mario Melazzini, Angelo Avogaro
AIMS: Heart failure (HF) is frequent in type 2 diabetes (T2D) and several glucose-lowering medications may increase HF risk. In the SAVOR-TIMI trial, patients on Saxagliptin experienced a 27% higher risk of hospitalisation for HF (HHF). In a retrospective study on 127,555 patients, we showed that DPP-4i therapy was associated with a lower HHF risk than sulphonylurea (SU) therapy. We herein re-analyzed such data to evaluate intraclass differences among DPP-4i and SU. MATERIALS AND METHODS: We included T2D patients initiating DPP-4i or SU alone or in combination with metformin...
April 21, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28423178/head-to-head-comparison-of-structurally-unrelated-dpp4-inhibitors-in-the-setting-of-renal-ischemia-reperfusion-injury
#8
Christoph Reichetzeder, Karoline von Websky, Oleg Tsuprykov, Azadeh Mohagheghi Samarin, Luise Gabriele Falke, Sulistyo Emantoko Dwi Putra, Ahmed Abdallah Hasan, Viktoriia Antonenko, Caterina Curato, Jörg Rippman, Thomas Klein, Berthold Hocher
BACKGROUND AND PURPOSE: Results regarding protective effects of DPP4 inhibitors in renal ischemia-reperfusion-injury (IRI) are conflicting. The current study performed a head-to-head comparison of structurally unrelated DPP4 inhibitors in the setting of renal IRI. EXPERIMENTAL APPROACH: IRI was induced in uninephrectomized male rats by renal artery clamping for 30 minutes. The sham group was uninephrectomized but not subjected to IRI. DPP4 inhibitors or vehicle were given p...
April 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28418203/effectiveness-of-vildagliptin-as-add-on-to-metformin-monotherapy-among-uncontrolled-type-2-diabetes-mellitus-patients-in-a-real-world-setting
#9
Cheli Melzer Cohen, Carla Davis, Varda Shalev, Gabriel Chodick
BACKGROUND: Vildagliptin is a dipeptidyl peptidase-4 inhibitor (DPP4-i) commonly used as a dual oral agent with metformin, thiazolidinediones, or sulfonylurea for type 2 diabetes mellitus (T2DM). The efficacy of dual therapy with vildagliptin and metformin has been established in randomized clinical trials but little evidence exists from observational studies. The aims of the present study were to evaluate the effectiveness of vildagliptin as an add-on therapy to metformin in reducing HbA1c as well as its influences on body weight and blood lipids in a real-life setting...
April 18, 2017: Journal of Diabetes
https://www.readbyqxmd.com/read/28408838/dpp-4-inhibitor-treatment-%C3%AE-cell-response-but-not-hba1c-reduction-is-dependent-on-the-duration-of-diabetes
#10
Plamen Kozlovski, Vaishali Bhosekar, James E Foley
INTRODUCTION: Dipeptidyl peptidase-4 (DPP-4) inhibitors reduce hyperglycemia in patients with type 2 diabetes mellitus (T2DM) by enhancing insulin and suppressing glucagon secretion. Since T2DM is associated with progressive loss of β-cell function, we hypothesized that the DPP-4 inhibitor action to improve β-cell function would be attenuated with longer duration of T2DM. METHODS: Data from six randomized, placebo-controlled trials of 24 weeks duration, where β-cell response to vildagliptin 50 mg twice daily was assessed, were pooled...
2017: Vascular Health and Risk Management
https://www.readbyqxmd.com/read/28406239/cmd-05-a-novel-promising-clinical-anti-diabetic-drug-candidate-in-vivo-and-vitro-studies
#11
Jie Ma, Huan Li, Xiangnan Hu, Lu Yang, Qi Chen, Congli Hu, Zhihao Chen, Xiaoyan Tian, Yang Yang, Ying Luo, Run Gan, Junqing Yang
Dipeptidyl peptidase IV (DPP-IV) inhibitor has been expected to be a new class of anti-diabetic agent. The present study was designed to characterize the pharmacological profiles of CMD-05, a novel DPP-IV inhibitor discovered in our laboratory, in vitro and in vivo. The IC50 of CMD-05 on DPP-IV inhibitory activity was approximately 12 nM while vildagliptin was 3.5 nM in vitro. In diabetes rat model established by high fat diet/low dose streptozotocin, CMD-05 inhibited DPP-IV activity, significantly improved glucose tolerance, increased GLP-1 and insulin levels in plasma...
April 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28403729/cost-effectiveness-of-vildagliptin-for-people-with-type-2-diabetes-mellitus-in-brazil-findings-and-implications
#12
REVIEW
Gustavo Laine Araujo De Oliveira, Augusto Afonso Guerra Júnior, Brian Godman, Francisco de Assis Acurcio
Vildagliptin is an inhibitor of the enzyme dipeptidyl peptidase 4, indicated for the treatment of type 2 diabetes mellitus, combined or not with metformin. This study aims to evaluate the cost-effectiveness of vildagliptin in the Brazilian context. Areas covered: Using MEDLINE, Cochrane Library, Lilacs and CRD, six studies were selected for the economic models. This study utilised cost data in the Brazilian health system to provide the context. Expert commentary: Type 2 diabetes mellitus is an epidemic disease and represents a challenge for all health care systems...
April 2017: Expert Review of Pharmacoeconomics & Outcomes Research
https://www.readbyqxmd.com/read/28391633/comparisons-of-cardioprotective-efficacy-between-fibroblast-growth-factor-21-and-dipeptidyl-peptidase-4-inhibitor-in-pre-diabetic-rats
#13
Pongpan Tanajak, Piangkwan Sa-Nguanmoo, Nattayaporn Apaijai, Xiaojie Wang, Guang Liang, Xiaokun Li, Chao Jiang, Siriporn C Chattipakorn, Nipon Chattipakorn
AIMS: Comparative efficacy between fibroblast growth factor 21 (FGF21) and vildagliptin on metabolic regulation, cardiac mitochondrial function, heart rate variability (HRV) and left ventricular (LV) function is not known. We hypothesized that FGF21 and vildagliptin share a similar efficacy in improving these parameters in high-fat diet (HFD) induced obese-insulin resistant rats. METHODS: Twenty-four male Wistar rats were fed with either a normal diet (ND) or a HFD for 12 weeks...
April 9, 2017: Cardiovascular Therapeutics
https://www.readbyqxmd.com/read/28367418/micro-environmental-signature-of-the-interactions-between-druggable-target-protein-dipeptidyl-peptidase-iv-and-anti-diabetic-drugs
#14
Chiranjib Chakraborty, Bidyut Mallick, Ashish Ranjan Sharma, Garima Sharma, Supriya Jagga, C George Priya Doss, Ju-Suk Nam, Sang-Soo Lee
OBJECTIVE: Druggability of a target protein depends on the interacting micro-environment between the target protein and drugs. Therefore, a precise knowledge of the interacting micro-environment between the target protein and drugs is requisite for drug discovery process. To understand such micro-environment, we performed in silico interaction analysis between a human target protein, Dipeptidyl Peptidase-IV (DPP-4), and three anti-diabetic drugs (saxagliptin, linagliptin and vildagliptin)...
April 2017: Cell Journal
https://www.readbyqxmd.com/read/28338281/cardiovascular-safety-of-vildagliptin-in-patients-with-type-2-diabetes-a-european-multi-database-non-interventional-post-authorization-safety-study
#15
R Williams, F de Vries, W Kothny, C Serban, S Lopez-Leon, C Chu, R Schlienger
This non-interventional, multi-database, analytical cohort study assessed the cardiovascular (CV) safety of vildagliptin vs. other non-insulin antidiabetic drugs (NIADs) using real-world data from five European electronic healthcare databases. Patients with type 2 diabetes aged ≥18 years on NIAD treatment were enrolled. Adjusted incidence rate ratios (IRRs) and 95% confidence intervals (95% CIs) for the outcomes of interest (myocardial infarction [MI], acute coronary syndrome [ACS], stroke, congestive heart failure [CHF], individually and as a composite) were estimated using negative binomial regression...
March 24, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28303721/effectiveness-and-safety-of-vildagliptin-and-vildagliptin-add-on-to-metformin-in-real-world-settings-in-egypt-results-from-the-guard-study
#16
Salah Shelbaya, Sameh Rakha
OBJECTIVE: The GUARD study evaluated the effectiveness, safety, and tolerability of vildagliptin treatment with or without metformin in patients with type 2 diabetes mellitus (T2DM) in real-life settings. Here we present the results of the GUARD study for the patient subset from Egypt. RESEARCH DESIGN AND METHODS: This was a 24 ± 6 weeks, prospective, non-interventional study that enrolled adult patients with T2DM receiving vildagliptin or vildagliptin + metformin combination therapy as per local prescribing information...
May 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28281660/dpp-4-inhibitor-and-estrogen-share-similar-efficacy-against-cardiac-ischemic-reperfusion-injury-in-obese-insulin-resistant-and-estrogen-deprived-female-rats
#17
Sivaporn Sivasinprasasn, Pongpan Tanajak, Wanpitak Pongkan, Wasana Pratchayasakul, Siriporn C Chattipakorn, Nipon Chattipakorn
Estrogen deprivation aggravates cardiac injury after myocardial ischemia and reperfusion (I/R) injury. Although either estrogen or the dipeptidyl peptidase-4 (DPP-4) inhibitor, vildagliptin, reduces myocardial damage following cardiac I/R, their effects on the heart in obese-insulin resistant and estrogen deprived conditions remain unknown. Ovariectomized (O) rats (n = 36) were divided to receive either normal diet (NDO) or high-fat diet (HFO) for 12 weeks, followed by treatment with a vehicle, estrogen or vildagliptin for 4 weeks...
March 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28276830/bariatric-surgery-time-to-replace-with-glp-1
#18
Dominic-Luc Webb, Niclas Abrahamsson, Magnus Sundbom, Per M Hellström
Obesity with a body mass index (BMI) over 30 kg/m(2) represents a significant risk for increased morbidity and mortality, with reduced life expectancy of about 10 years. Until now, surgical treatment has been the only effective longterm intervention. The currently standardized method of bariatric surgery, gastric bypass, means that many gastrointestinal peptide hormones are activated, yielding net reductions in appetite and food intake. Among the most important gut peptide hormones in this perspective is glucagon-like peptide-1 (GLP-1), which rises sharply after gastric bypass...
June 2017: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28275958/comparative-effectiveness-of-adding-alogliptin-to-metformin-plus-sulfonylurea-with-other-dpp-4-inhibitors-in-type-2-diabetes-a-systematic-review-and-network-meta-analysis
#19
REVIEW
Stephen Kay, Amanda Strickson, Jorge Puelles, Ross Selby, Eugene Benson, Keith Tolley
INTRODUCTION: Alogliptin is an oral antihyperglycemic agent that is a selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4), approved for the treatment of type 2 diabetes mellitus (T2DM). There currently exists no comparative data to support the use of alogliptin in combination with metformin (met) and sulfonylurea (SU). A decision-focused network meta-analysis (NMA) was performed to compare the relative efficacy and safety of alogliptin 25 mg once daily to other DPP-4 inhibitors as part of a triple therapy regimen for patients inadequately controlled on metformin and SU dual therapy...
April 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/28271502/trigonelline-and-vildagliptin-antidiabetic-effect-improvement-of-insulin-signalling-pathway
#20
Amat-Alrazaq A Aldakinah, Muhammad Y Al-Shorbagy, Dalaal M Abdallah, Hanan S El-Abhar
OBJECTIVES: Trigonelline (TRG) is known to have an antidiabetic efficacy; however, its mechanism is not entirely elucidated. METHODS: Hence, its effect on insulin signaling, besides its effectiveness in combination with vildagliptin (VLD) in a Type 2 diabetes model has been tested. KEY FINDINGS: TRG (50 mg/kg; p.o) lowered serum glucose, fructosamine, insulin, and HOMA-IR index and increased insulin sensitivity in soleus muscle via augmenting insulin receptor autophosphorylation (IR-PH), pT308-Akt, and glucose transporter 4 (GLUT4)...
March 8, 2017: Journal of Pharmacy and Pharmacology
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