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glp-1 agonist

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https://www.readbyqxmd.com/read/29134607/the-cost-effectiveness-of-dulaglutide-1-5mg-versus-exenatide-qw-for-the-treatment-of-patients-with-type-2-diabetes-mellitus-in-france
#1
Mickael Basson, Dionysios Ntais, Ruba Ayyub, Donna Wright, Julia Lowin, Florence Chartier, Stéphane Roze, Kirsi Norrbacka
INTRODUCTION: Dulaglutide is a novel onceweekly administered glucagon-like peptide 1 receptor agonist (GLP-1 RA) for the management of type 2 diabetes mellitus (T2DM). The objective of this analysis was to estimate the cost-effectiveness of dulaglutide 1.5 mg versus exenatide QW for the management of T2DM in France. METHODS: The QuintilesIMS CORE Diabetes Model was used to estimate the expected lifetime direct medical costs and outcomes of T2DM from the perspective of the French National Health Service...
November 13, 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29133778/glucagon-like-peptide-1-glp-1-receptor-agonist-liraglutide-alters-bone-marrow-exosome-mediated-mirna-signal-pathways-in-ovariectomized-rats-with-type-2-diabetes
#2
Jin Li, Ling-Zhi Fu, Lu Liu, Fen Xie, Ru-Chun Dai
BACKGROUND Compared with normal postmenopausal women, estrogen deficiency and hyperglycemia in postmenopausal women with type 2 diabetes (T2DM) lead to more severe bone property degradation. Liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, has been reported to improve bone condition among people with T2DM but the precise mechanisms remain unclear. Exosomes work as mediators in cell-to-cell communication, delivering functional miRNAs between cells. We aimed to explore the role of exosomes in T2DM-related bone metabolic disorders and the bone protective mechanisms of liraglutide...
November 14, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29132091/effect-of-anti-diabetic-drugs-on-bone-metabolism-evidence-from-preclinical-and-clinical-studies
#3
REVIEW
Mohammad Adil, Rashid Ali Khan, Abul Kalam, Shiva Kumar Venkata, Amit Dattatraya Kandhare, Pinaki Ghosh, Manju Sharma
Diabetes mellitus is associated with abnormal bone health and an increased risk of fracture even though patients have normal or higher BMD. The mechanisms behind diabetes mellitus- induced various skeletal disorders remain unclear. Anti-diabetic drugs may have negative or positive impact on bone metabolism. For instance, thiazolidinediones increases the bone loss and risk of fracture possibly through PPARγ activation in bone marrow cells and hamper osteoblastogenesis via decreasing Runx2 transcription factor, IGF-1 and Wnt signalling pathways...
May 25, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29130686/thioamide-substitution-selectively-modulates-proteolysis-and-receptor-activity-of-therapeutic-peptide-hormones
#4
Xing Chen, Elizabeth G Mietlicki-Baase, Taylor M Barrett, Lauren E McGrath, Kieran Koch-Laskowski, John J Ferrie, Matthew R Hayes, E James Petersson
Peptide hormones are attractive as injectable therapeutics and imaging agents, but they often require extensive modification by mutagenesis and/or chemical synthesis to prevent rapid in vivo degradation. Alternatively, the single-atom, O-to-S modification of peptide backbone thioamidation has the potential to selectively perturb interactions with proteases while preserving interactions with other proteins, such as target receptors. Here, we use the validated diabetes therapeutic, glucagon-like peptide-1 (GLP-1), and the target of clinical investigation, gastric inhibitory polypeptide (GIP), as proof-of-principle peptides to demonstrate the value of thioamide substitution...
November 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29119712/impact-of-delaying-treatment-intensification-with-a-glucagon-like-peptide-1-receptor-agonist-in-patients-with-type-2-diabetes-uncontrolled-on-basal-insulin-a-longitudinal-study-of-a-us-administrative-claims-database
#5
L Tong, C Pan, H Wang, M Bertolini, E Lew, L F Meneghini
AIM: To evaluate the effect of delaying treatment intensification with a glucagon-like peptide-1 receptor agonist (GLP-1 RA) on clinical and economic outcomes in patients with type 2 diabetes (T2D). METHODS: We conducted a retrospective observational claims study using IMPACT(TM) , in adult patients with T2D who initiated basal insulin between 1 January 2005 and 31 December 2012 with or without OADs, but remained uncontrolled (glycated haemoglobin [HbA1c] ≥7.0%)...
November 8, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29113708/efficacy-and-safety-of-glucagon-like-peptide-1-agonists-on-macrovascular-and-microvascular-events-in-type-2-diabetes-mellitus-a-meta-analysis
#6
P Gargiulo, G Savarese, C D'Amore, F De Martino, L H Lund, F Marsico, S Dellegrottaglie, C Marciano, B Trimarco, P Perrone-Filardi
AIMS: Glucagon-like peptide-1 (GLP-1) agonists improve glycaemic control in type 2 diabetes mellitus (DM). Outcome trials investigating macro and microvascular effects of GLP-1 agonists reported conflicting results. The aim of this study was to assess, in a meta-analysis, the effects of GLP-1 agonists on mortality, major nonfatal cardiovascular (CV) events, renal and retinal events. DATA SYNTHESIS: MEDLINE, Cochrane, ISI Web of Science, SCOPUS and ClinicalTrial...
September 28, 2017: Nutrition, Metabolism, and Cardiovascular Diseases: NMCD
https://www.readbyqxmd.com/read/29113464/a-new-treatment-strategy-for-parkinson-s-disease-through-the-gut-brain-axis-the-glucagon-like-peptide-1-receptor-pathway
#7
Dong Seok Kim, Ho-Il Choi, Yun Wang, Yu Luo, Barry J Hoffer, Nigel H Greig
Molecular communications in the gut-brain axis, between the central nervous system and the gastrointestinal tract, are critical for maintaining healthy brain function, particularly in aging. Epidemiological analyses indicate type 2 diabetes mellitus (T2DM) is a risk factor for neurodegenerative disorders including Alzheimer's disease (AD) and Parkinson's diseases (PD) for which aging shows a major correlative association. Common pathophysiological features exist between T2DM, AD, and PD, including oxidative stress, inflammation, insulin resistance, abnormal protein processing, and cognitive decline, and suggest that effective drugs for T2DM that positively impact the gut-brain axis could provide an effective treatment option for neurodegenerative diseases...
September 2017: Cell Transplantation
https://www.readbyqxmd.com/read/29110715/liraglutide-dictates-macrophage-phenotype-in-apolipoprotein-e-null-mice-during-early-atherosclerosis
#8
Robyn Bruen, Sean Curley, Sarina Kajani, Daniel Crean, Marcella E O'Reilly, Margaret B Lucitt, Catherine G Godson, Fiona C McGillicuddy, Orina Belton
BACKGROUND: Macrophages play a pivotal role in atherosclerotic plaque development. Recent evidence has suggested the glucagon-like peptide-1 receptor (GLP-1R) agonist, liraglutide, can attenuate pro-inflammatory responses in macrophages. We hypothesized that liraglutide could limit atherosclerosis progression in vivo via modulation of the inflammatory response. METHODS: Human THP-1 macrophages and bone marrow-derived macrophages, from both wild-type C57BL/6 (WT) and apolipoprotein E null mice (ApoE(-/-)) were used to investigate the effect of liraglutide on the inflammatory response in vitro...
November 6, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29107284/superior-reductions-in-hepatic-steatosis-and-fibrosis-with-co-administration-of-a-glucagon-like-peptide-1-receptor-agonist-and-obeticholic-acid-in-mice
#9
Hani Jouihan, Sarah Will, Silvia Guionaud, Michelle L Boland, Stephanie Oldham, Peter Ravn, Anthony Celeste, James L Trevaskis
OBJECTIVE: Nonalcoholic steatohepatitis (NASH) is an unmet need associated with metabolic syndrome. There are no approved therapies for NASH; however, glucagon-like peptide-1 receptor (GLP-1R) and farnesoid-X receptor (FXR) agonists are promising drug targets. We investigated the therapeutic effects of co-administration of a GLP-1R agonist, IP118, with FXR agonist obeticholic acid (OCA) in mice. METHODS: OCA and IP118 alone and in combination were sub-chronically administered to Lep(ob)/Lep(ob) mice with diet-induced NASH or diet-induced obese (DIO) mice...
November 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/29107282/the-autonomic-nervous-system-and-cardiac-glp-1-receptors-control-heart-rate-in-mice
#10
Laurie L Baggio, John R Ussher, Brent A McLean, Xiemin Cao, M Golam Kabir, Erin E Mulvihill, Alexandra S Mighiu, Hangjun Zhang, Andreas Ludwig, Randy J Seeley, Scott P Heximer, Daniel J Drucker
OBJECTIVES: Glucagon-like peptide-1 (GLP-1) is secreted from enteroendocrine cells and exerts a broad number of metabolic actions through activation of a single GLP-1 receptor (GLP-1R). The cardiovascular actions of GLP-1 have garnered increasing attention as GLP-1R agonists are used to treat human subjects with diabetes and obesity that may be at increased risk for development of heart disease. Here we studied mechanisms linking GLP-1R activation to control of heart rate (HR) in mice...
November 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/29106046/retrospective-analysis-of-liraglutide-and-basal-insulin-combination-therapy-in-japanese-type-2-diabetes-the-association-between-remaining-%C3%AE-cell-function-and-the-achievement-of-the-hba1c-target-one-year-after-initiation
#11
Ryota Usui, Yui Sakuramachi, Yusuke Seino, Kenta Murotani, Hitoshi Kuwata, Hisato Tatsuoka, Yoshiyuki Hamamoto, Takeshi Kurose, Yutaka Seino, Daisuke Yabe
BACKGROUND AND AIMS: The glucose-lowering effects of the GLP-1 receptor agonist liraglutide have been shown to rely on remaining β-cell function. However, the possible associations of remaining β-cell function with the glucose-lowering effects of liraglutide in combination with basal insulin remain unknown and warrant investigation. METHODS: This is a single-center, retrospective, observational study conducted in a private hospital in Osaka, Japan. Type 2 diabetes patients who received a prescription change from insulin therapy, both multiple-dose insulin (MDI) and basal insulin-supported oral therapy (BOT), to liraglutide/basal insulin combination and continued the therapy for 54 weeks without additional oral anti-diabetic drugs (OAD) or bolus insulin were retrospectively analyzed...
November 6, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/29095968/characterization-of-the-glucagon-like-peptide-1-receptor-in-male-mouse-brain-using-a-novel-antibody-and-in-situ-hybridization
#12
Casper Bo Jensen, Charles Pyke, Morten Grønbech Rasch, Anders Bjorholm Dahl, Lotte Bjerre Knudsen, Anna Secher
Glucagon-like peptide-1 (GLP-1) is a physiological regulator of appetite and long-acting GLP-1 receptor agonists (GLP-1RA) lower food intake and bodyweight in both human and animal studies. The effects are mediated through brain GLP-1Rs, and several brain nuclei expressing the GLP-1R may be involved. To date, mapping the complete location of GLP-1R protein in the brain has been challenged by lack of good antibodies and the discrepancy between mRNA and protein especially relevant in neuronal axonal processes...
October 30, 2017: Endocrinology
https://www.readbyqxmd.com/read/29094257/the-effects-of-exendin-4-on-bone-marrow-derived-mesenchymal-cells
#13
Paola Luciani, Benedetta Fibbi, Benedetta Mazzanti, Cristiana Deledda, Lara Ballerini, Alessandra Aldinucci, Susanna Benvenuti, Riccardo Saccardi, Alessandro Peri
PURPOSE: GLP-1 receptor agonists are antidiabetic drugs currently used in the therapy of type 2 diabetes. Despite several in vitro and in vivo animal studies suggesting a beneficial effect of GLP-1 analogues on bone, in humans their skeletal effects are not clear and clinical studies report conflicting results. METHODS: We differentiated human mesenchymal stromal cells (hMSC) toward the adipogenic and the osteoblastic lineages, analysing the effect of Exendin-4 (EXE) before, during and after specific differentiations...
November 1, 2017: Endocrine
https://www.readbyqxmd.com/read/29091882/incretin-hormones-receptor-signaling-plays-the-key-role-in-antidiabetic-potential-of-pty-2-against-stz-induced-pancreatitis
#14
Shivani Srivastava, Priya Shree, Harsh Pandey, Yamini Bhusan Tripathi
AIMS: Incretin therapy is one of the most potential approaches in the treatment of diabetes. In contrast to markedly available drugs, the herbal incretin modulators have lesser side effects with low economic cost. The main aim of this work was to analyze the potential of previously reported DPPIV inhibitor, aqueous extract of Pueraria tuberosa tubers (PTY-2) as incretin hormones receptor agonist against streptozotocin (STZ)-induced diabetes. METHODS: Chronic diabetes was induced with STZ (65mg/kg bw) in rats for 60days and grouped into diabetic control and PTY-2...
October 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29091313/exenatide-upregulates-gene-expression-of-glucagon-like-peptide-1-receptor-and-nerve-growth-factor-in-streptozotocin-nicotinamide-induced-diabetic-mice
#15
Esen Gumuslu, Naci Cine, Merve Ertan, Oguz Mutlu, Ipek Komsuoglu Celikyurt, Guner Ulak
Glucagon like peptide-1 (GLP-1) is an incretine hormon that has modulating effects on insulin release. GLP-1 and receptors for GLP-1 are widely expressed throughout the body including brain.The expression of GLP-1 receptors is very specific to large neurons in hippocampus, neocortex and cerebellum. GLP-1 receptor stimulation enhances glucose-dependent insulin secretion and lowers blood glucose in type 2 diabetes mellitus. Studies on adipobiology of neurotrophins have focused on nerve growth factor (NGF) as an example of adipose-derived neurotrophins...
November 1, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/29084156/the-dietary-furocoumarin-imperatorin-increases-plasma-glp-1-levels-in-type-1-like-diabetic-rats
#16
Lin-Yu Wang, Kai-Chun Cheng, Yingxiao Li, Chiang-Shan Niu, Juei-Tang Cheng, Ho-Shan Niu
Imperatorin, a dietary furocoumarin, is found not only in medicinal plants, but also in popular culinary herbs, such as parsley and fennel. Recently, imperatorin has been shown to activate GPR119 in cells. Another GPR, GPR131, also called TGR5 or G-protein-coupled bile acid receptor 1 (GPBAR1), is known to regulate glucose metabolism. Additionally, TGR5 activation increases glucagon-like peptide (GLP-1) secretion to lower blood sugar levels in animals. Therefore, the present study aims to determine whether the effects of imperatorin on GLP-1 secretion are mediated by TGR5...
October 30, 2017: Nutrients
https://www.readbyqxmd.com/read/29077992/population-pharmacokinetics-of-exendin-9-39-and-clinical-dose-selection-in-patients-with-congenital-hyperinsulinism
#17
Chee M Ng, Fei Tang, Steven Seeholzer, Yixuan Zou, Diva D De León
AIMS: Congenital hyperinsulinism (HI) is the most common cause of persistent hypoglycaemia in infants and children. Exendin-(9-39), an inverse glucagon-like peptide 1 (GLP-1) agonist, is a novel therapeutic agent for HI that has demonstrated glucose-raising effect. We reported the first population pharmacokinetic (PopPK) model of the exendin-(9-39) in patients with HI and proposed the optimal dosing regimen for future clinical trials in neonates with HI. METHODS: 182 pharmacokinetic (PK) observations from 26 subjects in three clinical studies were included for constructing the PopPK model using FOCE with interaction method in NONMEM...
October 27, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29076038/long-term-effectiveness-of-liraglutide-in-association-with-patients-baseline-characteristics-in-real-life-setting-in-croatia-an-observational-retrospective-multicenter-study
#18
Maja Cigrovski Berkovic, Ines Bilic-Curcic, Davorka Herman Mahecic, Marina Gradiser, Mladen Grgurevic, Tomislav Bozek
INTRODUCTION: Glucagon-like peptide-1 (GLP-1) receptor agonists (RAs) are recommended therapy for type 2 diabetes (T2DM) and liraglutide is the most used worldwide. We assessed the glycemic efficacy and extra-glycemic effects of liraglutide during 36 months' follow-up of individuals with poorly regulated T2DM under routine clinical practice and sought to identify the phenotype of treatment responders. METHODS: A total of 207 individuals were included. The primary endpoint was the proportion of participants with HbA1c < 7...
December 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29074588/glp-1-elicits-an-intrinsic-gut-liver-metabolic-signal-to-ameliorate-diet-induced-vldl-overproduction-and-insulin-resistance
#19
Rituraj Khound, Jennifer Taher, Chris Baker, Khosrow Adeli, Qiaozhu Su
OBJECTIVE: Perturbations in hepatic lipid and very-low-density lipoprotein (VLDL) metabolism are involved in the pathogenesis of obesity and hepatic insulin resistance. The objective of this study is to delineate the mechanism of subdiaphragmatic vagotomy in preventing obesity, hyperlipidemia, and insulin resistance. APPROACH AND RESULTS: By subjecting the complete subdiaphragmatic vagotomized mice to various nutritional conditions and investigating hepatic de novo lipogenesis pathway, we found that complete disruption of subdiaphragmatic vagal signaling resulted in a significant decrease of circulating VLDL-triglyceride compared with the mice obtained sham procedure...
October 26, 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/29071110/real-world-weight-change-among-patients-treated-with-glucagon-like-peptide-1-receptor-agonist-dipeptidyl-peptidase-4-inhibitor-and-sulfonylureas-for-type-2-diabetes-and-the-influence-of-medication-adherence
#20
G S Carls, R Tan, J Y Zhu, E Tuttle, J Yee, S V Edelman, W H Polonsky
AIMS: The study aims to examine real-world weight change and the role of medication adherence among patients with type 2 diabetes who initiated one of three drug classes: glucagon-like peptide-1 receptor agonist (GLP-1RA), dipeptidyl peptidase-4 inhibitor (DPP4) and sulfonylureas (SUs). MATERIALS AND METHODS: A cohort of patients initiating one of the three drug classes was selected from a large US database of integrated electronic medical record and administrative claims...
September 2017: Obesity Science & Practice
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