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https://read.qxmd.com/read/30759365/exenatide-once-weekly-improves-metabolic-parameters-endothelial-dysfunction-and-carotid-intima-media-thickness-in-patients-with-type-2-diabetes-an-8-month-prospective-study
#1
Angelo Maria Patti, Dragana Nikolic, Antonio Magan-Fernandez, Rosaria Vincenza Giglio, Giuseppa Castellino, Roberta Chianetta, Roberto Citarrella, Egle Corrado, Francesca Provenzano, Vincenzo Provenzano, Giuseppe Montalto, Ali A Rizvi, Manfredi Rizzo
AIM: To evaluate the effect of exenatide long acting release (LAR) on carotid intima-media thickness (IMT) and endothelial function in patients with type 2 diabetes mellitus. METHODS: Sixty subjects with type 2 diabetes mellitus were treated with exenatide LAR as add-on to stable doses of metformin for 8 months in an open label study. Anthropometric variables, lipid profile and glycemic parameters were assessed by routine analysis. Carotid IMT by Doppler ultrasound and endothelial function by flow-mediated dilation of the brachial artery were also assessed...
February 10, 2019: Diabetes Research and Clinical Practice
https://read.qxmd.com/read/30756511/relative-contribution-of-basal-and-post-prandial-hyperglycaemia-stratified-by-hba-1c-categories-before-and-after-treatment-intensification-with-dulaglutide
#2
Guillermo Umpierrez, Kevin M Pantalone, Charles M Atisso, Laura Fernández Landó, Hiren Patel
OBJECTIVE: There is limited information regarding the effect of glucagon-like peptide-1 receptor agonists (GLP-1 RAs) on the relative contribution of basal hyperglycaemia (BHG) and post-prandial hyperglycaemia (PPHG) to overall hyperglycaemia across HbA1c categories. RESEARCH DESIGN AND METHODS: Data from five phase 3 studies (N=673) were pooled to assess the change in relative contributions of BHG and PPHG to overall hyperglycaemia across different HbA1c categories after 6 months of treatment intensification with dulaglutide 1...
February 12, 2019: Diabetes, Obesity & Metabolism
https://read.qxmd.com/read/30732592/patterns-and-trends-of-utilization-of-incretin-based-medicines-between-2008-and-2014-in-three-italian-geographic-areas
#3
Giuseppe Roberto, Francesco Barone-Adesi, Francesco Giorgianni, Valeria Pizzimenti, Carmen Ferrajolo, Michele Tari, Claudia Bartolini, Roberto Da Cas, Marina Maggini, Stefania Spila-Alegiani, Paolo Francesconi, Gianluca Trifirò, Elisabetta Poluzzi, Fabio Baccetti, Rosa Gini
BACKGROUND: The incretin-based medicines GLP1 analogues (GLP1a) and dipeptidyl peptidase-4 inhibitors (DPP4i) are hypoglycaemic agents licensed for the treatment of type 2 diabetes mellitus (T2DM). Although these drugs possess comparable efficacy and low risk of hypoglycaemia, differences in terms of route of administration (subcutaneous versus oral), effect on body weight and gastrointestinal tolerabily can impact their actual use in clinical practice. This study aimed to describe the real-world utilization of incretin-based medicines in the Italian clinical practice...
February 7, 2019: BMC Endocrine Disorders
https://read.qxmd.com/read/30720240/redox-active-injectable-gel-using-polyion-complex-to-achieve-sustained-release-of-exenatide-and-enhance-therapeutic-efficacy-for-the-treatment-of-type-2-diabetes
#4
Shiro Ishii, Shou Sakaue, Yukio Nagasaki
To provide sustained release of exenatide and enhance therapeutic efficacy for the treatment of type 2 diabetes compared to the existing products for exenatide, we developed an exenatide-loaded, redox-active, injectable gel (Exe@RIG). This injectable gel is formed by a polyion complex (PIC) comprising three components, (1) cationic polyamine-poly(ethylene glycol)-polyamine triblock copolymer possessing reactive oxygen species (ROS)-scavenging moieties as side chains, (2) anionic poly(acrylic acid), and (3) exenatide...
February 5, 2019: Journal of Biomedical Materials Research. Part A
https://read.qxmd.com/read/30700996/effect-of-tcf7l2-polymorphism-on-pancreatic-hormones-after-exenatide-in-type-2-diabetes
#5
Mari Cassol Ferreira, Maria Elizabeth Rossi da Silva, Rosa Tsuneshiro Fukui, Maria do Carmo Arruda-Marques, Salman Azhar, Rosa Ferreira Dos Santos
Background: Glucagon-like peptide 1 (GLP-1) stimulates insulin secretion and reduces blood glucose in type 2 diabetes mellitus (T2DM). TCF7L2 rs7903146 polymorphism has been associated with decreased insulin secretion, reduced GLP-1 action, and possible impaired peripheral insulin sensitivity. Objectives: To evaluate the postprandial pancreatic hormone response in patients with T2DM carriers of the TCF7L2 variant rs7903146 (CT/TT) compared with noncarriers of this variant (CC) after treatment with the GLP-1 agonist exenatide...
2019: Diabetology & Metabolic Syndrome
https://read.qxmd.com/read/30690693/exenatide-delays-gastric-emptying-in-patients-with-type-2-diabetes-mellitus-but-not-in-those-with-gastroparetic-conditions
#6
Christelle Beti, Bernd Stratmann, Georgy Bokman, Jens Dreier, Michael Hauber, Young Hee Lee-Barkey, Manfred Fischer, Cornelius Knabbe, Diethelm Tschoepe
The effect of the treatment with glucagon-like peptide (GLP)-1 receptor agonists on gastric emptying in patients with diabetes with and without gastroparesis is analysed. Patients with type 2 diabetes mellitus subjected to GLP-1 receptor agonist therapy with exenatide were examined before and shortly after initiation of treatment. Gastric half-emptying time was determined by 13 C-octanoic breath test; routine laboratory parameter as well as active GLP-1, ghrelin, leptin, insulin, proinsulin and C-peptide levels were determined in fasting state as well as postprandial secretion within 1 h after a standardised meal...
January 28, 2019: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://read.qxmd.com/read/30679302/a-randomized-controlled-trial-on-the-safety-and-efficacy-of-exenatide-therapy-for-the-inpatient-management-of-general-medicine-and-surgery-patients-with-type-2-diabetes
#7
Maya Fayfman, Rodolfo J Galindo, Daniel J Rubin, Dara L Mize, Isabel Anzola, Maria A Urrutia, Clementina Ramos, Francisco J Pasquel, J Sonya Haw, Priyathama Vellanki, Heqiong Wang, Bonnie S Albury, Rita Weaver, Saumeth Cardona, Guillermo E Umpierrez
OBJECTIVE: This multicenter, open-label, randomized trial examined the safety and efficacy of exenatide alone or in combination with basal insulin in non-critically ill patients with type 2 diabetes (T2D). RESEARCH DESIGN AND METHODS: A total of 150 patients with blood glucose (BG) between 140 and 400 mg/dL, treated at home with diet, oral agents, or insulin at a total daily dose <0.5 units/kg, were randomized to exenatide alone (5 μg twice daily), exenatide plus basal insulin, or a basal-bolus insulin regimen...
January 24, 2019: Diabetes Care
https://read.qxmd.com/read/30663560/endothelium-as-a-therapeutic-target-in-diabetes-mellitus-from-basic-mechanisms-to-clinical-practice
#8
Anastasios Tentolouris, Ioanna Eleftheriadou, Evangelia Tzeravini, Dimitrios Tsilingiris, Stavroula A Paschou, Gerasimos Siasos, Nikolaos Tentolouris
Endothelium plays an essential role in human homeostasis by regulating arterial blood pressure, distributing nutrients and hormones as well as providing a smooth surface that modulates coagulation, fibrinolysis and inflammation. Endothelial dysfunction is present in diabetes mellitus (DM) and contributes to the development and progression of macrovascular disease, while it is also associated with most of the microvascular complications such as diabetic retinopathy, nephropathy and neuropathy. Hyperglycemia, insulin resistance, hyperinsulinemia and dyslipidemia are the main factors involved...
January 19, 2019: Current Medicinal Chemistry
https://read.qxmd.com/read/30641721/long-term-effects-of-glp-1-receptor-agonists-in-type-2-diabetic-patients-a-retrospective-real-life-study-in-131-patients
#9
A Hemmer, D Maiter, M Buysschaert, V Preumont
AIM: We evaluate retrospectively long-term effects of GLP-1 receptor agonists in type 2 diabetic patients treated between 2008 and 2016. METHODS: 131 patients treated by GLP-1 receptor agonists (GLP-1RAs) were included. The objective was to evaluate the evolution of glycated hemoglobin (HbA1c ) during a period up to 4 years. The secondary objectives consisted of analysing the long-term effects of treatment on body mass index (BMI), blood pressure and lipids; reporting the proportion of patients who reached HbA1c objectives; estimating the time before treatment failure and determining predictive factors of failure...
January 2019: Diabetes & Metabolic Syndrome
https://read.qxmd.com/read/30640362/utility-of-neuronal-derived-exosomes-to-examine-molecular-mechanisms-that-affect-motor-function-in-patients-with-parkinson-disease-a-secondary-analysis-of-the-exenatide-pd-trial
#10
Dilan Athauda, Seema Gulyani, Hanuma Karnati, Yazhou Li, David Tweedie, Maja Mustapic, Sahil Chawla, Kashfia Chowdhury, Simon S Skene, Nigel H Greig, Dimitrios Kapogiannis, Thomas Foltynie
Importance: Exenatide, a glucagon-like peptide 1 agonist used in type 2 diabetes, was recently found to have beneficial effects on motor function in a randomized, placebo-controlled trial in Parkinson disease (PD). Accumulating evidence suggests that impaired brain insulin and protein kinase B (Akt) signaling play a role in PD pathogenesis; however, exploring the extent to which drugs engage with putative mechnisms in vivo remains a challenge. Objective: To assess whether participants in the Exenatide-PD trial have augmented activity in brain insulin and Akt signaling pathways...
January 14, 2019: JAMA Neurology
https://read.qxmd.com/read/30635783/combination-of-insulin-with-a-glp1-agonist-is-associated-with-better-memory-and-normal-expression-of-insulin-receptor-pathway-genes-in-a-mouse-model-of-alzheimer-s-disease
#11
Ari Robinson, Irit Lubitz, Dana Atrakchi-Baranes, Avital Licht-Murava, Pavel Katsel, Derek Leroith, Sigal Liraz-Zaltsman, Vahram Haroutunian, Michal Schnaider Beeri
Disruption of brain insulin signaling may explain the higher Alzheimer's disease (AD) risk among type 2 diabetic (T2D) patients. There is evidence from in vitro and human postmortem studies that combination of insulin with hypoglycemic medications is neuroprotective and associated with less amyloid aggregation. We examined the effect of 8-month intranasal administration of insulin, exenatide (a GLP-1 agonist), combination therapy (insulin + exenatide) or saline, in wild-type (WT) and an AD-like mouse model (Tg2576)...
January 11, 2019: Journal of Molecular Neuroscience: MN
https://read.qxmd.com/read/30627822/formation-mechanism-in-vitro-and-in-vivo-evaluation-of-dimpled-exenatide-loaded-plga-microparticles-prepared-by-ultra-fine-particle-processing-system
#12
Chune Zhu, Tingting Peng, Di Huang, Disang Feng, Xinyi Wang, Xin Pan, Wen Tan, Chuanbin Wu
Spherical poly (D, L-lactic-co-glycolic acid) microparticles (PLGA-MPs) have long been investigated in order to achieve sustained delivery of proteins/peptides. However, the formation mechanism and release characteristics of the specific shape MPs were still unknown. This study aimed to develop a novel-dimpled exenatide-loaded PLGA-MPs (Exe-PLGA-MPs) using an ultra-fine particle processing system (UPPS) and investigate the formation mechanism and release characteristics. Exe-PLGA-MPs were prepared by UPPS and optimized based on their initial burst within the first 24 h and drug release profiles...
January 9, 2019: AAPS PharmSciTech
https://read.qxmd.com/read/30609236/heart-failure-and-type-2-diabetes-from-cvots-with-hope
#13
REVIEW
Dario Giugliano, Juris J Meier, Katherine Esposito
An excess heart failure (HF) risk persists in patients with type 2 diabetes (T2D) despite optimal control of an array of conventional risk factors, including hyperglycaemia. Twelve cardiovascular outcome trials (CVOTs) have been so far published, although none, with the exception of DECLARE with dapagliflozin, has included HF in the primary endpoint. The four trials with dipeptidyl-peptidase inhibitors (DPP-4i) (SAVOR-TIMI 53 with saxagliptin, EXAMINE with alogliptin, TECOS with sitagliptin, and CARMELINA with linagliptin) failed to show any significant effect on HF risk in patients with T2D, with the notable exception of saxagliptin that was associated with a 27% increased risk...
January 4, 2019: Diabetes, Obesity & Metabolism
https://read.qxmd.com/read/30604598/asian-subpopulations-may-exhibit-greater-cardiovascular-benefit-from-long-acting-glucagon-like-peptide-1-receptor-agonists-a-meta-analysis-of-cardiovascular-outcome-trials
#14
Yu Mi Kang, Yun Kyung Cho, Jiwoo Lee, Seung Eun Lee, Woo Je Lee, Joong Yeol Park, Ye Jee Kim, Chang Hee Jung, Michael A Nauck
BACKGROUND: Based on reported results of three large cardiovascular outcome trials (CVOTs) of glucagon-like peptide 1 receptor agonists (GLP-1 RAs), we aimed to investigate the overall effect of GLP-1 RAs on major adverse cardiovascular events (MACEs) and to identify subpopulations exhibiting the greatest cardiovascular (CV) benefit. METHODS: Three CVOTs reporting effects of long-acting GLP-1 RAs were included: LEADER (liraglutide), SUSTAIN-6 (semaglutide), and EXSCEL (exenatide once weekly)...
December 27, 2018: Diabetes & Metabolism Journal
https://read.qxmd.com/read/30601014/synthesis-of-csk-dex-plga-nanoparticles-for-oral-delivery-of-exenatide-to-improve-its-mucus-penetration-and-intestinal-absorption
#15
Yina Song, Yanan Shi, Liping Zhang, Haiyan Hu, Chunyan Zhang, Miaomiao Yin, Liuxiang Chu, Xiuju Yan, Mingyu Zhao, Xuemei Zhang, Hongjie Mu, Kaoxiang Sun
Oral absorption of exenatide, a drug for type 2 diabetes treatment, can be improved by using nanoparticles (NPs) for its delivery. To improve the mucus penetration and intestinal absorption of exenatide, we designed a block copolymer, CSKSSDYQC-dextran-poly (lactic-co-glycolic acid) (CSK-DEX-PLGA), and used it for preparation of exenatide-loaded NPs. The functionalized exenatide-loaded NPs composed of CSK-DEX-PLGA were able to target intestinal epithelial cells and reduce the mucus-blocking effect of the intestine...
January 2, 2019: Molecular Pharmaceutics
https://read.qxmd.com/read/30600137/efficacy-and-tolerability-of-exenatide-once-weekly-over-7-years-in-patients-with-type-2-diabetes-an-open-label-extension-of-the-duration-1-study
#16
Athena Philis-Tsimikas, Carol H Wysham, Elise Hardy, Jenny Han, Nayyar Iqbal
AIMS: To investigate the glycemic efficacy, effects on cardiovascular risk factors, and safety of exenatide once weekly (QW) in patients with type 2 diabetes over 7 years in the DURATION-1 study. METHODS: Patients were initially randomized to exenatide QW 2 mg or exenatide twice daily for 30 weeks, after which they received open-label, open-ended treatment with exenatide QW 2 mg for up to 7 years. Efficacy analyses included changes from baseline in glycated hemoglobin (HbA1C ) and cardiovascular risk factors...
December 5, 2018: Journal of Diabetes and its Complications
https://read.qxmd.com/read/30578607/comparative-effectiveness-of-exenatide-once-weekly-versus-liraglutide-in-routine-clinical-practice-a-retrospective-multicenter-study-and-meta-analysis-of-observational-studies
#17
Gian Paolo Fadini, Benedetta Maria Bonora, Annunziata Lapolla, Bruno Fattor, Paola Silvia Morpurgo, Natalino Simioni, Angelo Avogaro
In this study, we retrospectively compared effectiveness of exenatide once weekly (ExeOW) versus liraglutide in non-insulin treated patients with type 2 diabetes followed under routine care. We also present a meta-analysis of similar observational studies available in the literature. In our multicentre retrospective study, patients initiating ExeOW (n=204) or liraglutide (n=410) had similar baseline clinical characteristics. Change in HbA1c at 6 months was superimposable in the two groups (-0.7±1.0%) and changes in body weight were also similar (ExeOW -2...
December 21, 2018: Diabetes, Obesity & Metabolism
https://read.qxmd.com/read/30572079/vesicular-phospholipid-gels-as-drug-delivery-systems-for-small-molecular-weight-drugs-peptides-and-proteins-state-of-the-art-review
#18
Michaela Breitsamer, Gerhard Winter
Lipid-based drug delivery has been investigated for a long time when it comes to liposomes and solid-lipid implants or solid-lipid nanoparticles. The promising, characteristic properties of these systems have led to the development of newer lipid-based drug delivery systems for the sustained release of drugs like liposomes for sustained delivery of substances, DepoFoamTM technology, phospholipid-based phase separation gels and vesicular phospholipid gels. Vesicular phospholipid gels (VPGs) are highly concentrated, viscous dispersions of high amounts of phospholipids in aqueous drug solution...
December 17, 2018: International Journal of Pharmaceutics
https://read.qxmd.com/read/30554037/exenatide-modulates-expression-of-metalloproteinases-and-their-tissue-inhibitors-in-tnf-%C3%AE-stimulated-human-retinal-pigment-epithelial-cells
#19
Wojciech Garczorz, Enrique Gallego-Colon, Agnieszka Kosowska, Krzysztof Siemianowicz, Agnieszka Kłych-Ratuszny, Michał Woźniak, Mohammad Reza F Aghdam, Tomasz Francuz, Mariola Dorecka
BACKGROUND: Diabetic retinopathy (DR) is one of the most common complications of diabetes and the leading cause of acquired blindness in adults. In diabetic patients hyperglycemia induces complex metabolic abnormalities affecting retinal homeostasis, and promotes retinal inflammation and angiogenesis. Incretin mimetic drugs such exenatide, are a relatively new group of drugs used in the treatment of diabetes. We investigated the potential direct effects of exenatide on human retinal pigment epithelium (HRPE)...
October 3, 2018: Pharmacological Reports: PR
https://read.qxmd.com/read/30546390/exenatide-reduces-oxidative-stress-and-cell-death-in-testis-in-iron-overload-rat-model
#20
Suleyman Yesil, Nuran Sungu, Aydan Kilicarslan, Serife Mehlika Kuskonmaz, Halil Kara, Aysegul Kucuk, Fazli Polat, Mustafa Kavutcu, Mustafa Arslan
Glucagon-like peptide-1 (GLP-1) has been demonstrated to affect the oxidative stress status in several in vitro, in vivo and clinical studies. The aim of the present study was to evaluate the effect of a GLP-1 analogue, exenatide, on oxidative stress parameters and apoptotic markers in testicular cells in an iron overload rat model. To obtain this model, the animals were randomly divided into three groups (n=6/group). Rats in the control group received intraperitoneal injections of saline. Intraperitoneal iron dextran (60 mg/kg/day) was given to Group FE for 5 days a week for 4 weeks...
December 2018: Experimental and Therapeutic Medicine
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