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exenatid

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https://www.readbyqxmd.com/read/28932995/pharmacokinetics-and-preliminary-pharmacodynamics-of-single-and-multiple-dose-lyophilized-recombinant-glucagon-like-peptide-1-receptor-agonist-re-4-in-chinese-patients-with-type-2-diabetes-mellitus
#1
Yitong Wang, Bingfeng Xu, Lixia Zhu, Kun Lou, Yingli Chen, Xia Zhao, Qian Wang, Ling Xu, Xiaohui Guo, Linong Ji, Yimin Cui, Yi Fang
BACKGROUND AND OBJECTIVES: Recombinant glucagon-like peptide-1 receptor agonist (rE-4) is a glucagon-like peptide-1 receptor agonist, which has the same amino acid sequence to exenatide, except for the C-terminal deamidated. This study assessed the pharmacokinetics and preliminary pharmacodynamics of rE-4, following single and multiple subcutaneous injections in Chinese patients with type 2 diabetes mellitus (T2DM). DESIGN AND METHODS: In the randomized, open-label study, Chinese patients with T2DM (n = 36) were randomly assigned to three groups of rE-4 (n = 12), rE-4 with metformin (n = 12) and exenatide (n = 12, as the control group) for 12 weeks...
September 20, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28932989/predictors-of-response-to-glucagon-like-peptide-1-receptor-agonists-a-meta-analysis-and-systematic-review-of-randomized-controlled-trials
#2
Matteo Monami, Ilaria Dicembrini, Besmir Nreu, Francesco Andreozzi, Giorgio Sesti, Edoardo Mannucci
AIMS: The aim of the present meta-analysis is the identification of the characteristics of patients, which predict the efficacy on HbA1c of glucagon-like peptide-1 receptor agonists (GLP-1 RA). METHODS: A Medline and Embase search for "exenatide" OR "liraglutide" OR "albiglutide" OR "dulaglutide" OR "lixisenatide" was performed, collecting randomized clinical trials (duration > 12 weeks) up to September 2016, comparing GLP-1 RA at the maximal approved dose with placebo or active drugs...
September 20, 2017: Acta Diabetologica
https://www.readbyqxmd.com/read/28927992/protective-effects-of-the-glp-1-mimetic-exendin-4-in-parkinson-s-disease
#3
REVIEW
Dilan Athauda, Thomas Foltynie
There is increasing interest in the potential role of glucagon-like peptide-1 (GLP-1) receptor agonists as neuroprotective treatments in neurodegenerative diseases including Parkinson's disease following the publication of the results of the Exenatide-PD trial. Of the current GLP-1 receptor agonists already licensed to treat Type 2 diabetes several including exenatide, liraglutide and lixisenatide are the subject of ongoing clinical trials in PD. The underlying rationale for using drugs licensed and effective for T2DM in PD patients therefore needs to be scrutinized, and the results obtained to date critically reviewed...
September 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28918840/neuroprotective-effects-of-eexenatide-in-a-rotenone-induced-rat-model-of-parkinson-s-disease
#4
Dürdane Aksoy, Volkan Solmaz, Türker Çavuşoğlu, Ayfer Meral, Utku Ateş, Oytun Erbaş
BACKROUND: Several studies suggest an association between Parkinson's disease (PD) and type 2 diabetes mellitus; these 2 diseases are both known to affect the common molecular pathways. As a synthetic agonist for the glucagon-like peptide 1 receptor, exenatide has been evaluated as a neuroprotective agent in multiple animal models. Rotenone models of PD have great potential for the investigation of PD pathology and motor and nonmotor symptoms, as well as the role of gene-environment interactions in PD causation and pathogenesis...
September 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28912879/a-crossover-study-of-the-combination-therapy-of-metformin-and-exenatide-or-biphasic-insulin-aspart-30-in-overweight-or-obese-patients-newly-diagnosed-with-type-2-diabetes-mellitus
#5
Huibiao Quan, Huachuan Zhang, Weiping Wei, Tuanyu Fang, Daoxiong Chen, Kaining Chen
The aim of the present study was to explore the effects of various combinations of exenatide, metformin (MET) and biphasic insulin aspart 30 (BIA30) on type 2 diabetes mellitus (T2DM). Two hundred overweight or obese patients newly diagnosed with T2DM were evenly randomized into two groups: A (twice daily for all: Phase I, 5 µg exenatide + 0.5 g MET for 4 weeks, then 10 µg exenatide + 0.5 g MET for 8 weeks; Phase II, 0.5 g MET for 12 weeks; Phase III, 0.3-0.4 U/kg/day BIA30 + 0.5 g MET for 12 weeks) and B (Phases I, II, III matched the phases III, II and I in group A)...
October 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28910237/effects-of-once-weekly-exenatide-on-cardiovascular-outcomes-in-type-2-diabetes
#6
Rury R Holman, M Angelyn Bethel, Robert J Mentz, Vivian P Thompson, Yuliya Lokhnygina, John B Buse, Juliana C Chan, Jasmine Choi, Stephanie M Gustavson, Nayyar Iqbal, Aldo P Maggioni, Steven P Marso, Peter Öhman, Neha J Pagidipati, Neil Poulter, Ambady Ramachandran, Bernard Zinman, Adrian F Hernandez
Background The cardiovascular effects of adding once-weekly treatment with exenatide to usual care in patients with type 2 diabetes are unknown. Methods We randomly assigned patients with type 2 diabetes, with or without previous cardiovascular disease, to receive subcutaneous injections of extended-release exenatide at a dose of 2 mg or matching placebo once weekly. The primary composite outcome was the first occurrence of death from cardiovascular causes, nonfatal myocardial infarction, or nonfatal stroke...
September 14, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28898436/letter-to-liu-et%C3%A2-al-2017-article
#7
Richard S Legro
I was intrigued to see the recent trial of Liu et al(1) reporting the benefits of exenatide over metformin in terms of weight loss and pregnancy rate in women with polycystic ovary syndrome. I am writing to clarify the discrepancies between the trial as registered and the trial as reported in the manuscript. According to the trial registration on the Chinese Clinical Trial Registration Site (ChiCTR-IIR-16008084) the trial was a three armed trial for exenatide, metformin, or spironolactone. This article is protected by copyright...
September 12, 2017: Clinical Endocrinology
https://www.readbyqxmd.com/read/28870261/sustained-release-study-on-exenatide-loaded-into-mesoporous-silica-nanoparticles-in-vitro-characterization-and-in-vivo-evaluation
#8
Cuiwei Chen, Hongyue Zheng, Junjun Xu, Xiaowei Shi, Fanzhu Li, Xuanshen Wang
BACKGROUND: Exenatide (EXT), the first glucagon-like peptide-1 receptor agonist, has been approved as an adjunctive therapy for patients with type 2 diabetes. Due to EXT's short half-life, EXT must be administrated by continuous subcutaneous (s.c.) injection twice daily. In previous studies, many studies on EXT loaded into polymer materials carriers for sustained release had been reported. However, these carriers have some defects, such as hydrophobicity, low surface energy, low mechanical strength, and poor chemical stability...
September 4, 2017: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/28862808/comparative-effectiveness-of-once-weekly-glp-1-receptor-agonists-on-6-month-glycemic-control-and-weight-outcomes-in-patients-with-type-2-diabetes
#9
Sudhir Unni, Eric Wittbrodt, Junjie Ma, Marisa Schauerhamer, Jeff Hurd, Natalia Ruiz-Negrón, Carrie McAdam-Marx
A retrospective cohort study was conducted in patients with type 2 diabetes (T2D) in an electronic medical record database to compare real-world, 6-month A1C and weight outcomes for exenatide QW (EQW) vs. dulaglutide and vs. albiglutide. The study included 2,133 EQW, 201 dulaglutide, and 131 albiglutide patients. Overall mean (SD) age was 60 (11) years and 54% were men; neither differed between comparison groups. Mean baseline A1C was similar for EQW [8.3 (1.7)%] and dulaglutide [8.5 (1.5)% (p=0.165)], but higher for albiglutide [8...
September 1, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28834553/efficacy-of-exenatide-on-weight-loss-metabolic-parameters-and-pregnancy-in-overweight-obese-polycystic-ovary-syndrome
#10
Xin Liu, Ying Zhang, Si-Yuan Zheng, Rong Lin, Yi-Juan Xie, Hui Chen, Yong-Xiong Zheng, En Liu, Lin Chen, Jia-He Yan, Wei Xu, Ting-Ting Mai, Yi Gong
CONTEXT: Weight loss remains one of the most important arms in obese patients with polycystic ovary syndrome (PCOS). Further studies are needed to identify the best treatment. OBJECTIVE: To evaluate the effects of exenatide (EXE) on reproductive and metabolic function in overweight/obese (OW/OB) PCOS. DESIGN: This is a 24-week open-label prospective, randomized, clinical study. PATIENTS AND MEASUREMENTS: This study randomized 176 OW/OB women diagnosed with PCOS to receive either EXE 10 μg BID (n = 88) or metformin (MET) 1000 mg BID (n = 88) for the first 12 weeks...
August 23, 2017: Clinical Endocrinology
https://www.readbyqxmd.com/read/28820780/clinical-effectiveness-of-intravenous-exenatide-infusion-in-perioperative-glycemic-control-after-coronary-artery-bypass-graft-surgery-a-phase-ii-iii-randomized-trial
#11
Guillaume Besch, Andrea Perrotti, Frederic Mauny, Marc Puyraveau, Maude Baltres, Guillaume Flicoteaux, Lucie Salomon du Mont, Benoit Barrucand, Emmanuel Samain, Sidney Chocron, Sebastien Pili-Floury
BACKGROUND: We aimed to assess the clinical effectiveness of intravenous exenatide compared to insulin in perioperative blood glucose control in coronary artery bypass grafting surgery patients. METHODS: Patients more than 18 yr old admitted for elective coronary artery bypass grafting were included in a phase II/III nonblinded randomized superiority trial. Current insulin use and creatinine clearance of less than 60 ml/min were exclusion criteria. Two groups were compared: the exenatide group, receiving exenatide (1-h bolus of 0...
August 18, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28794822/overview-of-glucagon-like-peptide-1-receptor-agonists-for-the-treatment-of-patients-with-type-2-diabetes
#12
Kelvin Lingjet Tran, Young In Park, Shalin Pandya, Navin John Muliyil, Brandon David Jensen, Kovin Huynh, Quang T Nguyen
BACKGROUND: It is estimated that 29.1 million people or 9.3% of the US population have diabetes, which contributes to considerable medical and financial burden. Type 2 diabetes mellitus is characterized by insulin resistance and insulin secretion impairment leading to hyperglycemia. The presence of insulin resistance is strongly correlated with obesity. OBJECTIVE: This article reviews the available glucagon-like peptide-1 (GLP-1) receptor agonists and their role in the management of patients with diabetes, to help guide the selection of the most suitable agent for the individualized treatment of patients with type 2 diabetes...
June 2017: American Health & Drug Benefits
https://www.readbyqxmd.com/read/28781108/exenatide-once-weekly-versus-placebo-in-parkinson-s-disease-a-randomised-double-blind-placebo-controlled-trial
#13
Dilan Athauda, Kate Maclagan, Simon S Skene, Martha Bajwa-Joseph, Dawn Letchford, Kashfia Chowdhury, Steve Hibbert, Natalia Budnik, Luca Zampedri, John Dickson, Yazhou Li, Iciar Aviles-Olmos, Thomas T Warner, Patricia Limousin, Andrew J Lees, Nigel H Greig, Susan Tebbs, Thomas Foltynie
BACKGROUND: Exenatide, a glucagon-like peptide-1 (GLP-1) receptor agonist, has neuroprotective effects in preclinical models of Parkinson's disease. We investigated whether these effects would be apparent in a clinical trial. METHODS: In this single-centre, randomised, double-blind, placebo-controlled trial, patients with moderate Parkinson's disease were randomly assigned (1:1) to receive subcutaneous injections of exenatide 2 mg or placebo once weekly for 48 weeks in addition to their regular medication, followed by a 12-week washout period...
August 3, 2017: Lancet
https://www.readbyqxmd.com/read/28777758/is-exenatide-a-treatment-for-parkinson-s-disease
#14
Dilan Athauda, Richard Wyse, Patrik Brundin, Thomas Foltynie
There is growing interest in the use of glucagon-like peptide-1 agonists as treatments for Parkinson's disease following the recent publication of the results of the Exenatide-PD trial. In this randomized, double-blind, placebo controlled trial, patients with moderate stage Parkinson's disease treated with once-weekly subcutaneous injections of exenatide 2 mg (Bydureon) for 48 weeks, had a 3.5-point advantage over the placebo group in the Movement Disorders Society Unified Parkinson's Disease Rating Scale (MDS-UPDRS) motor subscale (Part 3) in the practically defined OFF medication state, 12 weeks after cessation of the trial drug...
2017: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/28755389/no-calcitonin-change-in-a-person-taking-dulaglutide-diagnosed-with-pre-existing-medullary-thyroid-cancer
#15
S I Sherman, R T Kloos, R M Tuttle, A Pontecorvi, H Völzke, K Harper, C Vance, J T Alston, A L Usborne, K W Sloop, M Lakshmanan
BACKGROUND: Glucagon-like peptide-1 receptor agonists, such as dulaglutide, exenatide and liraglutide, are approved to treat Type 2 diabetes mellitus. Although these drugs provide substantial glycaemic control, studies in rodents have prompted concerns about the development of medullary thyroid carcinoma. These data are reflected in the US package insert, with boxed warnings and product labelling noting the occurrence of these tumours after clinically relevant exposures in rodents, and contraindicating glucagon-like peptide-1 receptor agonist use in people with a personal or family history of medullary thyroid carcinoma or in people with multiple endocrine neoplasia type 2...
July 29, 2017: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/28748377/microvascular-effects-of-glucagon-like-peptide-1-receptor-agonists-in-type-2-diabetes-a-meta-analysis-of-randomized-controlled-trials
#16
Ilaria Dicembrini, Besmir Nreu, Alessia Scatena, Francesco Andreozzi, Giorgio Sesti, Edoardo Mannucci, Matteo Monami
AIMS: Results with GLP1-receptor agonists (GLP-1RA) on microvascular complications of diabetes are contrasting. In trials designed for cardiovascular outcomes, both liraglutide and semaglutide were associated with a relevant reduction in the incidence and progression of nephropathy. On the other hand, in the same trials, semaglutide was associated with an increased progression of retinopathy, and a similar trend was observed for liraglutide. This meta-analysis is aimed at assessing the effects of GLP-1RA on retinopathy and nephropathy...
July 27, 2017: Acta Diabetologica
https://www.readbyqxmd.com/read/28734203/exenatide-mitigated-diet-induced-vascular-aging-and-atherosclerotic-plaque-growth-in-apoe-deficient-mice-under-chronic-stress
#17
Guang Yang, Yanna Lei, Aiko Inoue, Limei Piao, Lina Hu, Haiying Jiang, Takeshi Sasaki, Hongxian Wu, Wenhu Xu, Chenglin Yu, Guangxian Zhao, Shinyu Ogasawara, Kenji Okumura, Masafumi Kuzuya, Xian-Wu Cheng
BACKGROUND AND AIMS: Exposure to psychosocial stress is a risk factor for cardiovascular disorders. Because the glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonist prevents cardiovascular injury, we investigated the beneficial effects and mechanism of the GLP-1 analogue exenatide on stress-related vascular senescence and atherosclerosis in apolipoprotein E-deficient (ApoE(-/-)) mice fed a high-fat (HF) diet. METHODS: ApoE(-/-) mice fed the HF diet were assigned to non-stressed and immobilized-stress groups for 12 weeks...
July 13, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28730824/glucagon-like-peptide-1-analogues-exenatide-and-liraglutide-exert-inhibitory-effect-on-the-early-phase-of-liver-regeneration-after-partial-hepatectomy-in-rats
#18
J Fontana, O Kučera, V Mezera, M Anděl, Z Červinková
Glucagon-like peptide-1 (GLP-1) is an incretin known for proliferative and antiapoptotic effects on various tissues. Exenatide and Liraglutide are GLP-1 analogues used in clinical practice as antidiabetic drugs. Since GLP-1 and its analogues exert significant effect on liver metabolism and since changes in intermediary metabolism play an important role in the process of liver regeneration, we decided to determine the effect of Exenatide and Liraglutide on the early phase of liver regeneration and selected metabolic parameters in a model of 2/3 partial hepatectomy (PHx) in rats...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28724607/renal-hemodynamic-effects-of-glucagon-like-peptide-1-agonist-are-mediated-by-nitric-oxide-but-not-prostaglandin
#19
Scott Culver Thomson, Ali Kashkouli, Zhi Zhao Liu, Prabhleen Singh
The incretin hormone, glucagon like peptide-1 (GLP-1), is known for responding to dietary fat and carbohydrate. It elicits effects on pancreas, gut, and brain to stabilize blood glucose levels. We have previously reported that the GLP-1 agonist, exenatide, vasodilates the kidney and suppresses proximal reabsorption. The present study was undertaken to determine whether the renal effects of exenatide are mediated by nitric oxide (NO) and/or prostaglandins. Inulin clearance (GFR) and urine flow rate (UV) were measured in anesthetized rats before and during exenatide infusion (1 nmol/h iv)...
July 19, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28721043/preparation-of-exenatide-loaded-linear-poly-ethylene-glycol-brush-poly-l-lysine-block-copolymer-potential-implications-on-diabetic-nephropathy
#20
Fei Tong
The poly(ethylene glycol)-b-brush poly(l-lysine) polymer (PEG-b-(PELG50-g-PLL3)) was synthesized and evaluated as a nanocarrier for prolonging delivery of exenatide through the abdominal subcutaneous injection route. The isoelectric point of exenatide was 4.86, and exenatide could combine with PEG-b-(PELG50-g-PLL3) polymers via electrostatic interactions at pH 7.4. This polymer was a good candidate for achieving prolonged drug delivery for exenatide, considering its high molecular weight. Besides the physicochemical characterization of the polymer, in vitro and in vivo applications were researched as a sustained exenatide delivery system...
2017: International Journal of Nanomedicine
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