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Linagliptin

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https://www.readbyqxmd.com/read/28636754/linagliptin-and-its-effects-on-hyperglycaemia-and-albuminuria-in-patients-with-type-2-diabetes-and-renal-dysfunction-the-randomized-marlina-t2d%C3%A2-trial
#1
P-H Groop, M E Cooper, V Perkovic, B Hocher, K Kanasaki, M Haneda, G Schernthaner, K Sharma, R C Stanton, R Toto, J Cescutti, M Gordat, T Meinicke, A Koitka-Weber, S Thiemann, M von Eynatten
AIMS: The MARLINA-T2D™ study (ClinicalTrials.gov, NCT01792518) was designed to investigate the glycaemic and renal effects of linagliptin added to standard-of-care in individuals with type 2 diabetes and albuminuria. METHODS: 360 individuals with type 2 diabetes, HbA1c 6.5 - 10.0% (48 - 86 mmol/mol), estimated glomerular filtration rate (eGFR) ≥30 mL/min/1.73 m(2) , and urinary albumin-to-creatinine ratio (UACR) 30-3000 mg/g despite single agent renin-angiotensin-system blockade were randomized to double-blind linagliptin (n = 182) or placebo (n = 178) for 24 weeks...
June 21, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28635331/network-meta-analysis-of-liraglutide-versus-dpp-4-inhibitors-for-the-treatment-of-type-2-diabetes-in-japanese-patients
#2
Dieter Ayers, Steve Kanters, Rachel Goldgrub, Monica Hughes, Ryo Kato, Nana Kragh
AIMS: To determine the comparative efficacy and safety of liraglutide and dipeptidyl peptidiase-4 (DPP-4) inhibitors as antidiabetics for Japanese patients with uncontrolled type 2 diabetes (T2DM). METHODS AND MATERIALS: We searched for randomized-controlled trials (RCTs) evaluating outcomes among Japanese adults with uncontrolled T2DM and including liraglutide or DPP-4 inhibitors up to August 2016. We extracted data on trial and patient characteristics, and the following outcomes: HbA1c, weight, patients meeting HbA1c <7%, patients experiencing hypoglycemic events, microalbuminuria, estimated glomerular filtration rate (eGFR) and creatinine...
June 21, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28635324/gliptins-suppress-inflammatory-macrophage-activation-to-mitigate-inflammation-fibrosis-oxidative-stress-and-vascular-dysfunction-in-models-of-non-alcoholic-steatohepatitis-and-liver-fibrosis
#3
Xiaoyu Wang, Michael Hausding, Shih-Yen Weng, Yong Ook Kim, Sebastian Steven, Thomas Klein, Andreas Daiber, Detlef Schuppan
AIMS: Non-alcoholic steatohepatitis (NASH) is characterized by steatosis, panlobular inflammation, liver fibrosis and increased cardiovascular mortality. Dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) are indirect glucagon like peptide 1 (GLP-1) agonists with antidiabetic and anti-inflammatory activity, used for the treatment of type 2 diabetes. Their potential and underlying mechanisms to treat metabolic liver inflammation and fibrosis as well as the associated vascular dysfunction remain to be explored...
June 21, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28619389/the-promising-effect-of-linagliptin-and-or-indole-3-carbinol-on-experimentally-induced-polycystic-ovarian-syndrome
#4
Ahmed M Kabel, Aisha H Al-Shehri, Rehab A Al-Talhi, Maaly A Abd Elmaaboud
Polycystic ovarian syndrome (PCOS) is one of the most common medical conditions that lead to female infertility worldwide. The aim of this study was to assess the effect of linagliptin and/or indole-3-carbinol (I3C) on PCOS in female rats. Fifty female Wistar rats were randomly allocated into five equal groups: Control group; Letrozole-induced PCOS group; Letrozole + Linagliptin group; Letrozole + I3C group and Letrozole + Linagliptin + I3C group. Body weight, body mass index, Lee index and ovarian indices were determined...
June 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28613952/healthcare-costs-among-adults-with-type-2-diabetes-initiating-saxagliptin-or-linagliptin-a-us-based-claims-analysis
#5
Amanda M Kong, Sepehr Farahbakhshian, Trudy Pendergraft, Matthew A Brouillette, Biswarup Mukherjee, David M Smith, John J Sheehan
OBJECTIVE: To compare healthcare costs of adults with type 2 diabetes (T2D) after initiation of saxagliptin or linagliptin, two antidiabetic medications in the dipeptidyl peptidase-4 inhibitors medication class. METHODS: Patients with T2D who were at least 18 years old and initiated saxagliptin or linagliptin (index date) between 6/1/2011 and 6/30/2014 were identified in the MarketScan Commercial and Medicare Supplemental Databases. All-cause healthcare costs and diabetes-related costs (T2D diagnosis on a medical claim and/or an antidiabetic medication claim) were measured in the 1-year follow-up period...
June 14, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28581818/effect-of-linagliptin-versus-metformin-on-glycemic-variability-in-patients-with-impaired-glucose-tolerance
#6
Tonatiuh González-Heredia, Diana M Hernández-Corona, Manuel González-Ortiz, Esperanza Martínez-Abundis
BACKGROUND: Impaired glucose tolerance (IGT) and glycemic variability may be associated with increased risk of micro- and macrovascular complications. The aim of this study was to assess the effect of linagliptin versus metformin on glycemic variability in patients with IGT. MATERIAL AND METHODS: A randomized, double-blind clinical trial with parallel groups was carried out in 16 adult patients with IGT, overweight or obesity. All patients signed an informed consent...
June 5, 2017: Diabetes Technology & Therapeutics
https://www.readbyqxmd.com/read/28566414/linagliptin-associated-blistering-and-ulceration
#7
Cristina Psomadakis, Naima Shahzad, Jonathan Katz
We present the case of 60-year-old man with type 2 diabetes who developed blistering after two sequential exposures to linagliptin. Linagliptin is one of the dipeptidyl peptidase 4 (DPP-4) inhibitors, a group of oral hypoglycaemic agents used commonly for the treatment of type 2 diabetes. On the first exposure to linagliptin, he developed blisters on the hands which resolved after stopping the drug. After repeat exposure, he developed two large blisters on the left foot, which burst giving rise to secondary infection, requiring hospital admission for treatment...
May 31, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28476142/dipeptidyl-peptidase-4-dpp-4-inhibition-with-linagliptin-reduces-western-diet-induced-myocardial-traf3ip2-expression-inflammation-and-fibrosis-in-female-mice
#8
Annayya R Aroor, Javad Habibi, Hemanth Kumar Kandikattu, Mona Garro-Kacher, Brady Barron, Dongqing Chen, Melvin R Hayden, Adam Whaley-Connell, Shawn B Bender, Thomas Klein, Jaume Padilla, James R Sowers, Bysani Chandrasekar, Vincent G DeMarco
BACKGROUND: Diastolic dysfunction (DD), a hallmark of obesity and primary defect in heart failure with preserved ejection fraction, is a predictor of future cardiovascular events. We previously reported that linagliptin, a dipeptidyl peptidase-4 inhibitor, improved DD in Zucker Obese rats, a genetic model of obesity and hypertension. Here we investigated the cardioprotective effects of linagliptin on development of DD in western diet (WD)-fed mice, a clinically relevant model of overnutrition and activation of the renin-angiotensin-aldosterone system...
May 5, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28423178/head-to-head-comparison-of-structurally-unrelated-dipeptidyl-peptidase-4-inhibitors-in-the-setting-of-renal-ischemia-reperfusion-injury
#9
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 Rippmann, Thomas Klein, Berthold Hocher
BACKGROUND AND PURPOSE: Results regarding protective effects of dipeptidyl peptidase 4 (DPP4) inhibitors in renal ischaemia-reperfusion injury (IRI) are conflicting. Here we have compared structurally unrelated DPP4 inhibitors in a model of renal IRI. EXPERIMENTAL APPROACH: IRI was induced in uninephrectomized male rats by renal artery clamping for 30 min. The sham group was uninephrectomized but not subjected to IRI. DPP4 inhibitors or vehicle were given p.o. once daily on three consecutive days prior to IRI: linagliptin (1...
July 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28421983/comparative-study-between-multivariate-and-univariate-analysis-of-two-antidiabetic-combinations
#10
Maha F Abdel-Ghany, Omar Abdel-Aziz, Miriam F Ayad, Mariam M Tadros
New multivariate and univariate methods were developed for the analysis of two novel gliptin combinations by manipulating the zero-order and ratio spectra of empagliflozin and linagliptin in combination, with application on Glyxambi(®) tablets, and of alogliptin and pioglitazone in combination, with application on Oseni(®) tablets. Linearity ranges for chemometric approaches using principal component regression and partial least-squares were found to be 2–10, 2.5–12.5, 5–15, and 5–25 μg/mL for empagliflozin, linagliptin, alogliptin, and pioglitazone, respectively, whereas the respective linearity ranges for the spectrophotometric approaches were found to be 5–15, 2–12, 5–15, and 5–15 μg/mL...
April 18, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28413215/successful-withdrawal-of-insulin-therapy-after-post-treatment-clearance-of-hepatitis-c-virus-in-a-man-with-type-2-diabetes
#11
Timothy M E Davis, Wendy A Davis, Gary Jeffrey
BACKGROUND Chronic hepatitis C virus (HCV) infection is associated with increased insulin resistance and risk of type 2 diabetes. Successful antiviral treatment can improve insulin resistance and allow a reduction in blood glucose-lowering treatment. There have been case reports of a reduced insulin requirement in this situation, although 1 case in which insulin was stopped exhibited a subsequent deterioration in glycemic control. CASE REPORT A 55-year-old Italian man was diagnosed with HCV infection in 2000 at the age of 39 years and with type 2 diabetes 6 years later...
April 17, 2017: American Journal of Case Reports
https://www.readbyqxmd.com/read/28402902/cardiovascular-outcome-studies-with-incretin-based-therapies-comparison-between-dpp-4-inhibitors-and-glp-1-receptor-agonists
#12
REVIEW
André J Scheen
Dipeptidyl peptidase-4 inhibitors (DPP-4is) and glucagon-like peptide-1 receptor agonists (GLP-1RAs) represent two distinct classes of incretin-based therapies used for the treatment of type 2 diabetes. Non-inferiority versus placebo was shown in large prospective cardiovascular outcome trials in patients with high cardiovascular risk: SAVOR-TIMI 53 (saxagliptin), EXAMINE (alogliptin), and TECOS (sitagliptin); ELIXA (lixisenatide), LEADER (liraglutide) and SUSTAIN 6 (semaglutide). The promises raised by meta-analyses of phase 2-3 trials with DPP-4is were non confirmed as no cardiovascular protection could be evidenced...
May 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28375658/empagliflozin-linagliptin-single-pill-combination-therapy-for-patients-with-type-2-diabetes-mellitus
#13
Rajeev Kumar Jain
Type 2 diabetes mellitus (T2DM) is typically progressive, with sequential addition of therapies often needed to address increasing hyperglycemia over the disease course. Using treatments in combination may be preferred to sequential addition, as a means of providing a more rapid clinical response and potentially avoiding clinical inertia. In such cases, a single-pill combination can help to reduce pill burden. Although various single-pill combinations of oral glucose-lowering agents are available, empagliflozin/linagliptin was the first approved combination of a sodium glucose co-transporter 2 (SGLT2) inhibitor with a dipeptidyl peptidase 4 (DPP-4) inhibitor in the United States...
April 2017: Expert Opinion on Pharmacotherapy
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/28322073/sglt2-inhibitor-dpp-4-inhibitor-combination-therapy-complementary-mechanisms-of-action-for-management-of-type-2-diabetes-mellitus
#15
REVIEW
Jayant Dey
Type 2 diabetes mellitus is a progressive disease with multiple underlying pathophysiologic defects. Monotherapy alone cannot maintain glycemic control and leads to treatment failure. Ideally, a combination of glucose-lowering agents should have complementary mechanisms of action that address multiple pathophysiologic pathways, can be used at all stages of the disease, and be generally well tolerated with no increased risk of hypoglycemia, cardiovascular events, or weight gain. The combination should also provide conveniences for patients, such as oral dosing, single-pill formulations, and once-daily administration, potentially translating to improved adherence...
May 2017: Postgraduate Medicine
https://www.readbyqxmd.com/read/28302969/fast-and-simple-determination-of-3-aminopiperidine-without-derivatization-using-high-performance-liquid-chromatography-charged-aerosol-detector-with-an-ion-exchange-reversed-phase-mixed-mode-column
#16
Shubo Dong, Zhengyu Yan, Hanyue Yang, Zhen Long
A sensitive non-derivatization method for the determination of the highly polar compound 3-aminopiperidine was developed using a mixed-mode column combined with a charged aerosol detector (CAD). Chromatographic conditions, including the type of detector, separation mode, and mobile phase composition, were optimized to achieve high sensitivity towards and sufficient retention of 3-aminopiperidine. Compared to the precolumn derivatization UV method, the current method showed higher recovery and greater simplicify...
2017: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
https://www.readbyqxmd.com/read/28290274/relative-bioavailability-of-an-empagliflozin-25-mg-linagliptin-5-mg-fixed-dose-combination-tablet%C3%A2
#17
RANDOMIZED CONTROLLED TRIAL
Stephan Glund, Michaela Mattheus, Frank Runge, Peter Rose, Christian Friedrich
OBJECTIVE: This relative bioavailability study compared a fixed-dose combination (FDC) tablet of empagliflozin 25 mg/linagliptin 5 mg with the corresponding individual components. In addition, the effect of food on the bioavailability of the FDC was studied, and the standard-dissolving formulation FDC was compared with a slow-dissolving side batch. METHODS: An open-label, randomized, crossover study design was used (ClinicalTrials.gov Identifier NCT01189201). Healthy volunteers (n = 42) each received three single-dose treatments: FDC standard dissolution, individual tablets, and either FDC standard dissolution with food or FDC slow dissolution...
April 2017: International Journal of Clinical Pharmacology and Therapeutics
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
#18
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/28274625/apd668-a-g-protein-coupled-receptor-119-agonist-improves-fat-tolerance-and-attenuates-fatty-liver-in-high-trans-fat-diet-induced-steatohepatitis-model-in-c57bl-6-mice
#19
Umakant Ashok Bahirat, Rekha Raghuveer Shenoy, Rajan Naresh Goel, Kumar V S Nemmani
G-protein coupled receptor 119 (GPR119) receptor is a rhodopsin-like, class A Gαs-coupled receptor, predominantly expressed in pancreatic islet cells and intestinal entero-endocrine cells. GPR119 has been emerged as a novel therapeutic target for the treatment of dyslipidemia in type 2 diabetes. In this study, we investigated the effect of APD668, a GPR119 agonist alone and in combination with linagliptin, a DPPIV inhibitor on oral fat tolerance test. Our findings demonstrate that APD668, a GPR119 agonist inhibits the intestinal triglyceride absorption after acute fat load in mice...
April 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28273997/teneligliptin-in-management-of-diabetic-kidney-disease-a-review-of-place-in-therapy
#20
REVIEW
Mohammed Abubaker, Preetesh Mishra, Onkar C Swami
Diabetes is a global health emergency of this century. Diabetic nephropathy is the most common microvascular complication associated with Type 2 Diabetes Mellitus (T2DM). T2DM has been reported as a major etiological factor in almost 45% of patients undergoing dialysis due to kidney failure. Lifestyle modifications; cessation of smoking, optimum control of blood glucose, blood pressure and lipids are required to reduce the progression of Diabetic Kidney Disease (DKD). Presently, Dipeptidyl peptidase-4 (DPP-4) inhibitors are preferred in the management of T2DM due to their established efficacy; favorable tolerability including, low risk of hypoglycaemia; weight neutrality and convenient once-a-day dosage...
January 2017: Journal of Clinical and Diagnostic Research: JCDR
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