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Linagliptin

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https://www.readbyqxmd.com/read/28322073/sglt2-inhibitor-dpp-4-inhibitor-combination-therapy-complementary-mechanisms-of-action-for-management-of-type-2-diabetes-mellitus
#1
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...
March 21, 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
#2
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
#3
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...
March 14, 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
#4
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...
March 8, 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
#5
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...
March 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28273997/teneligliptin-in-management-of-diabetic-kidney-disease-a-review-of-place-in-therapy
#6
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
https://www.readbyqxmd.com/read/28244635/effect-of-linagliptin-on-pulse-wave-velocity-in-early-type-2-diabetes-release-a-randomized-double-blind-controlled-26-week-trial
#7
Stefanie A de Boer, Hiddo J L Heerspink, Luis E Juárez Orozco, Arie M van Roon, Pieter W Kamphuisen, Andries J Smit, Riemer H J A Slart, Joop D Lefrandt, Douwe J Mulder
AIMS: To evaluate the effects of the DPP-4 inhibitor linagliptin on aortic pulse wave velocity (PWV) as a surrogate marker of arterial stiffness and early atherosclerosis in early type 2 diabetes subjects. MATERIALS AND METHODS: A total of 45 type 2 diabetes subjects (median age 63 (IQR: 54-66) years, 61% male, mean hemoglobinA1c (HbA1c ) 6.3 ± 0.4 % (45 ± 4.6 mmol/mol)) without cardiovascular disease and naïve to antidiabetic treatment were randomized (1:1) to treatment with linagliptin 5 mg once daily or placebo for 26 weeks in a double-blind fashion...
February 28, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28242866/cross-over-study-comparing-postprandial-glycemic-increase-after-addition-of-a-fixed-dose-mitiglinide-voglibose-combination-or-a-dipeptidyl-peptidase-4-inhibitor-to-basal-insulin-therapy-in-patients-with-type-2-diabetes-mellitus
#8
Noriko Ihana-Sugiyama, Ritsuko Yamamoto-Honda, Takehiro Sugiyama, Tetsuro Tsujimoto, Masafumi Kakei, Mitsuhiko Noda
BACKGROUND Although the efficacy of combination therapy consisting of basal insulin and oral hypoglycemic agents (OHAs) has been shown, which OHAs are the most efficient remains unclear. MATERIAL AND METHODS Five patients with type 2 diabetes were enrolled and treated with insulin degludec and metformin as a basal therapy. The patients were randomized in a cross-over fashion to receive a combination of mitiglinide (10 mg) and voglibose (0.2 mg) (M+V) 3 times daily or linagliptin (5 mg) (L) once daily for 8 weeks...
February 28, 2017: Medical Science Monitor Basic Research
https://www.readbyqxmd.com/read/28230454/adherence-persistence-and-health-care-costs-for-patients-receiving-dipeptidyl-peptidase-4-inhibitors
#9
Karen L Rascati, Karen Worley, Yunus Meah, Damian Everhart
BACKGROUND: The dipeptidyl peptidase-4 (DPP-4) inhibitors are among the newer, yet more established, classes of diabetes medications. OBJECTIVE: To compare adherence, persistence, and health care costs among patients taking DPP-4 inhibitors. METHODS: Claims were extracted from Humana Medicare Advantage Prescription Drug (MAPD) or commercial plans for patients aged > 18 years with ≥ 1 prescription filled for a DPP-4 inhibitor between July 1, 2011, and March 31, 2013...
March 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28215601/design-and-synthesis-of-quinazoline-3-4-4h-diamine-endowed-with-thiazoline-moiety-as-new-class-for-dpp-4-and-dpph-inhibitor
#10
Zulphikar Ali, Md Jawaid Akhtar, Md Rafi Haider, Ahsan Ahmed Khan, Anees Ahmad Siddiqui, M Shahar Yar
New N3-benzylidene (substituted)-2-phenyl-N4-(thiazol-2-yl)-quinazoline-3,4-(4H)-diamine derivatives were design and synthesized by a sequence of reactions starting from appropriate 6-methyl anthranilic acid. The title compounds were screened for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity and diphenyl-2-picryl-hydrazyl (DPPH) assay and results showed significant to good activity in compared to Linagliptin for antidiabetic activity and Ascorbic acid for antioxidant activity. Compound 7g (IC50=0...
February 10, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28192751/ameliorative-potential-of-linagliptin-and-or-calcipotriol-on-bleomycin-induced-lung-fibrosis-in-vivo-and-in-vitro-study
#11
Ahmed M Kabel, Maaly A Abd Elmaaboud, Aliaa Atef, Mohammed H Baali
Pulmonary fibrosis is a serious medical problem that may significantly compromise respiratory functions. The aim of this work was to study the effect of linagliptin and/or calcipotriol on bleomycin-induced pulmonary fibrosis and to explore the possible mechanisms underlying this effect. One hundred and twenty male C57BL/6 mice were divided into 6 equal groups as follows: control group; bleomycin group; bleomycin+carboxymethylcellulose group; bleomycin+linagliptin group; bleomycin+calcipotriol group and bleomycin+linagliptin+calcipotriol group...
March 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28183314/dpp-4-inhibition-has-no-acute-effect-on-bnp-and-its-n-terminal-pro-hormone-measured-by-commercial-immune-assays-a-randomized-cross-over-trial-in-patients-with-type-2-diabetes
#12
Gian Paolo Fadini, Benedetta Maria Bonora, Mattia Albiero, Martina Zaninotto, Mario Plebani, Angelo Avogaro
BACKGROUND: Use of dipeptidyl peptidase-4 inhibitors (DPP4-i) for the treatment of type 2 diabetes (T2D) has been associated with a possible increase in the risk for heart failure (HF). B-type natriuretic peptide (BNP), which is both a biomarker of HF and a hemodynamically active hormone, is a substrate of DPP-4. We herein tested the acute effects of the DPP-4i linagliptin on BNP and NT-proBNP in a cross-over placebo-controlled trial in patients with T2D with and without chronic kidney disease (CKD)...
February 10, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28182722/hemoglobin-glycation-index-as-a-useful-predictor-of-therapeutic-responses-to-dipeptidyl-peptidase-4-inhibitors-in-patients-with-type-2-diabetes
#13
Yu-Wei Chen, Jun-Sing Wang, Wayne H-H Sheu, Shih-Yi Lin, I-Te Lee, Yuh-Min Song, Chia-Po Fu, Chia-Lin Lee
INTRODUCTION: A high hemoglobin glycation index (HGI) and glycated hemoglobin (HbA1c) level are associated with greater inflammatory status, and dipeptidyl peptidase-4 (DPP-4) inhibitors can suppress inflammation. We aimed to evaluate the relationship between HGI and the therapeutic effect of DPP-4 inhibitors. METHODS: This retrospective cohort study followed 468 patients with type 2 diabetes receiving DPP-4 inhibitor treatment for 1 year. Estimated HbA1c was calculated using a linear regression equation derived from another 2969 randomly extracted patients with type 2 diabetes based on fasting plasma glucose (FPG) level...
2017: PloS One
https://www.readbyqxmd.com/read/28177527/effects-of-linagliptin-on-human-immortalized-podocytes-a-cellular-system-to-study-dipeptidyl-peptidase-4-inhibition
#14
Gianluca Miglio, Giovanna Vitarelli, Thomas Klein, Elisa Benetti
BACKGROUND AND PURPOSE: Dipeptidyl-peptidase 4 (DPP4) is expressed by resident renal cells, including glomerular cells. DPP4 inhibitors (gliptins) exert albuminuria lowering effects, but the role of renal DPP4 as a pharmacological target has not been elucidated. To better understand the actions of gliptins, the effects of linagliptin on the behaviour of immortalized human podocytes and mesangial cells were evaluated. EXPERIMENTAL APPROACH: The expression of DPP4 was measured at both the mRNA and protein levels...
February 8, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28166651/dipeptidyl-peptidase-4-inhibitor-associated-risk-of-bleeding
#15
Md Motiur Rahman, Michael J Scalese, Richard A Hansen
BACKGROUND: Dipeptidyl peptidase-4 (DPP-4) inhibitors improve glycemic control, and sitagliptin has been associated with a reduction in cardiovascular events. In vivo data suggest reduced platelet activation, and aggregation may play a role, and therefore, increased bleeding risk is possible. OBJECTIVE: Comparatively assess bleeding risks associated with DPP-4 inhibitors against standard treatment. METHODS: Exploratory analyses of adverse event reports (AERs) from the US Food and Drug Administration Adverse Event Reporting System (FAERS) database (2004-2012 periods) were conducted...
February 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28109295/a-randomised-active-and-placebo-controlled-three-period-crossover-trial-to-investigate-short-term-effects-of-the-dipeptidyl-peptidase-4-inhibitor-linagliptin-on-macro-and-microvascular-endothelial-function-in-type-2-diabetes
#16
Thomas Jax, Alin Stirban, Arne Terjung, Habib Esmaeili, Andreas Berk, Sandra Thiemann, Robert Chilton, Maximilian von Eynatten, Nikolaus Marx
BACKGROUND: Studies of dipeptidyl peptidase (DPP)-4 inhibitors report heterogeneous effects on endothelial function in patients with type 2 diabetes (T2D). This study assessed the effects of the DPP-4 inhibitor linagliptin versus the sulphonylurea glimepiride and placebo on measures of macro- and microvascular endothelial function in patients with T2D who represented a primary cardiovascular disease prevention population. METHODS: This crossover study randomised T2D patients (n = 42) with glycated haemoglobin (HbA1c) ≤7...
January 21, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28097882/antidiabetic-agents-and-cardiovascular-outcomes-in-patients-with-heart-diseases
#17
Judy W M Cheng, Hisham A Badreldin, Dhiren K Patel, Snehal H Bhatt
INTRODUCTION: This article reviews evidence of the benefits and risk of antidiabetic agents in cardiovascular (CV) outcomes, with a focus on medications approved by the FDA since 2008. STUDY SELECTION: Peer-reviewed articles were identified from MEDLINE and Current Content databases (both 1966 to 1 October 2016) using the search terms insulin, metformin, rosiglitazone, pioglitazone, glyburide, glipizide, glimepiride, acarbose, miglitol, albiglutide, exenatide, liraglutide, lixisenatide, dulaglutide, pramlintide, meglitinide, alogliptin, linagliptin, saxagliptin, sitagliptin, canagliflozin, dapagliflozin, empagliflozin, colesevalam, bromocriptine, mortality, myocardial infarction (MI), heart failure (HF), and stroke...
February 15, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28093794/design-synthesis-and-biological-evaluation-of-novel-quinazoline-clubbed-thiazoline-derivatives
#18
Zulphikar Ali, Md J Akhtar, Anees A Siddiqui, Ahsan A Khan, Md R Haider, Mohammad S Yar
A novel series of quinazoline clubbed thiazoline derivatives was rationally designed and synthesized. The newly synthesized compounds were evaluated for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity. Compounds that showed good to moderate activity were compared using linagliptin as standard. Compound 4x (IC50  = 1.12 nM) exhibited the most promising results. The special chemical feature of compound 4x also imparts good inhibition selectivity for DPP-4 over DPP-8/9. Moreover, docking of compound 4x into the active site of DPP-4 illustrates its possible binding interactions...
January 17, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28088030/efficacy-and-safety-of-linagliptin-metformin-single-pill-combination-as-initial-therapy-in-drug-na%C3%A3-ve-asian-patients-with-type-2-diabetes
#19
RANDOMIZED CONTROLLED TRIAL
Yiming Mu, Changyu Pan, Bei Fan, Uwe Hehnke, Xiuzhen Zhang, Xuejun Zhang, Xiaoyue Wang, Jingdong Liu, Ying Zhang, Jianling Du, Jianhua Ma, Yan Gong
AIM: To assess efficacy/safety of initial linagliptin/metformin single-pill combination (SPC) therapies versus individual drug components over 24weeks in treatment-naïve Asian patients with type 2 diabetes mellitus and insufficient glycemic control. METHODS: Patients (initial glycated hemoglobin [HbA1c] ⩾7.5% to <11.0% [58-97mmol/mol]; main group) were randomized to: linagliptin 5mg once daily (qd); metformin 500mg twice daily (bid); metformin 1000mg bid; linagliptin 2...
February 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28039605/pharmacokinetic-characteristics-and-clinical-efficacy-of-an-sglt2-inhibitor-plus-dpp-4-inhibitor-combination-therapy-in-type-2-diabetes
#20
REVIEW
André J Scheen
Type 2 diabetes (T2D) generally requires a combination of several pharmacological approaches to control hyperglycaemia. Combining a sodium-glucose cotransporter type 2 inhibitor (SGLT2I, also known as gliflozin) and a dipeptidyl peptidase-4 inhibitor (DPP-4I, also known as gliptin) appears to be an attractive strategy because of complementary modes of action. This narrative review analyzes the pharmacokinetics and clinical efficacy of different combined therapies with an SGLT2I (canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, ipragliflozin, luseogliflozin, tofogliflozin) and DPP-4I (linagliptin, saxagliptin, sitagliptin, teneligliptin)...
December 30, 2016: Clinical Pharmacokinetics
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