#1
JOURNAL ARTICLE
(no author information available yet)
No abstract text is available yet for this article.
November 27, 2023: Medical Letter on Drugs and Therapeutics
#2
JOURNAL ARTICLE
(no author information available yet)
No abstract text is available yet for this article.
November 14, 2022: Medical Letter on Drugs and Therapeutics
#3
JOURNAL ARTICLE
Caroline Twarog, Elias Fattal, Magali Noiray, Brigitte Illel, David Brayden, Myriam Taverna, Hervé Hillaireau
A common approach to tackle the poor intestinal membrane permeability of peptides after oral administration is to formulate them with a permeation enhancer (PE). Increased oral bioavailability for oral peptide candidates has been reported from clinical trials when either salcaprozate sodium (SNAC) or sodium caprate (C10 ) is incorporated in the formulation. However, little is known about how they physically interact with peptides in solution. Our objective was to compare the biophysical interactions between the GLP-1 analogue exenatide (Byetta®, Lilly), and C10 or SNAC using a variety of advanced analytical techniques...
August 23, 2022: International Journal of Pharmaceutics
#4
RANDOMIZED CONTROLLED TRIAL
Nicklas J Johansen, Thomas F Dejgaard, Asger Lund, Camilla Schlüntz, Bolette Hartmann, Jens J Holst, Tina Vilsbøll, Henrik U Andersen, Filip K Knop
AIM: To evaluate the efficacy of the short-acting glucagon-like peptide-1 receptor agonist, exenatide, added to insulin therapy in type 1 diabetes on bone mineral density and bone turnover markers. MATERIALS AND METHODS: In a randomized, double-blinded, parallel-group trial, 108 individuals with type 1 diabetes aged 18 years or older on basal-bolus therapy with HbA1c 59-88 mmol/mol (7.5%-10.0%) and body mass index of more than 22.0 kg/m2 were randomized (1:1) to preprandial subcutaneous injection of 10 μg exenatide (Byetta) before breakfast, lunch, and dinner over 26 weeks as add-on treatment to insulin therapy...
February 2022: Diabetes, Obesity & Metabolism
#5
JOURNAL ARTICLE
Alexander Benet, Troy Halseth, Jukyung Kang, April Kim, Rose Ackermann, Santhanakrishnan Srinivasan, Steven Schwendeman, Anna Schwendeman
Exenatide, a glucagon-like peptide-1 receptor agonist, is the active pharmaceutical ingredient in Byetta® and Bydureon® , two type 2 diabetes drug products that have generics and multiple follow-up formulations currently in development. Even though exenatide is known to be chemically and physically unstable at pH 7.5, there lacks a systematic evaluation of the impact of pH and excipients on the peptide solution stability. In this study, we established analytical methods to measure the chemical and physical degradation of the peptide in solution...
August 16, 2021: Pharmaceutics
#6
REVIEW
Carol M Trim, Lee J Byrne, Steven A Trim
Difficult drug targets are becoming the normal course of business in drug discovery, sometimes due to large interacting surfaces or only small differences in selectivity regions. For these, a different approach is merited: compounds lying somewhere between the small molecule and the large antibody in terms of many properties including stability, biodistribution and pharmacokinetics. Venoms have evolved over millions of years to be complex mixtures of stable molecules derived from other somatic molecules, the stability comes from the pressure to be ready for delivery at a moment's notice...
2021: Progress in Medicinal Chemistry
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JOURNAL ARTICLE
Merve Celik-Tekeli, Nevin Celebi, M Yasin Tekeli, Yesim Aktas
The objective of this study is to develop a new self-nanoemulsifying system containing exendin-4 with or without enzyme inhibitor chymostatin and to evaluate the effects of oral administration of exendin-4 and exendin-4/chymostatin loaded self nanoemulsifying system on plasma exendin-4, plasma insulin, blood glucose levels and to compare with the oral and subcutaneous administration of exendin-4 in non-diabetic and streptozotocin-induced type 2 diabetic rats. Exendin-4 and exendin-4/chymostatin loaded self-nanoemulsifying system containing ethyl oleate as the oil phase, Cremophor EL®/Labrasol® as the surfactants and propylene glycol as the co-solvent were prepared...
March 1, 2021: European Journal of Pharmaceutical Sciences
#8
RANDOMIZED CONTROLLED TRIAL
Nicklas J Johansen, Thomas F Dejgaard, Asger Lund, Camilla Schlüntz, Emil L Larsen, Henrik E Poulsen, Jens P Goetze, Holger J Møller, Tina Vilsbøll, Henrik U Andersen, Filip K Knop
AIMS: To investigate the effect of adding the short-acting glucagon-like peptide 1 receptor agonist (GLP-1RA) exenatide to insulin treatment on markers of cardiovascular risk in type 1 diabetes. MATERIALS AND METHODS: In a randomized, double-blind, parallel-group trial, 108 individuals with type 1 diabetes aged ≥18 years on multiple daily injection therapy with a body mass index >22.0 kg/m2 and glycated haemoglobin concentration of 59 to 88 mmol/mol (7...
September 2020: Diabetes, Obesity & Metabolism
#9
RANDOMIZED CONTROLLED TRIAL
Jin Yang, Wenhua Xiao, Lixin Guo, Quanmin Li, Liyong Zhong, Jinkui Yang, Jing Yang, Yongyi Gao, Qing Tian, Tianpei Hong
AIMS: This study aimed to compare the efficacy and safety of generic exenatide with branded exenatide Byetta® in Chinese patients with type 2 diabetes mellitus (T2DM) inadequately controlled on monotherapy or combination therapy of metformin and insulin secretagogues. METHODS: A multicenter, randomized, controlled, non-inferiority trial was performed. A total of 240 patients with T2DM and glycated hemoglobin (HbA1c) ≥ 7% (53 mmol/mol) to ≤ 9.0% (75 mmol/mol) on monotherapy or combination therapy of metformin and insulin secretagogues for at least 3 months were randomized into generic exenatide or branded exenatide groups with a 1:1 ratio for 16 weeks of treatment...
August 2020: Acta Diabetologica
#10
RANDOMIZED CONTROLLED TRIAL
Nicklas J Johansen, Thomas F Dejgaard, Asger Lund, Camilla Schlüntz, Christian S Frandsen, Julie L Forman, Nicolai J Wewer Albrechtsen, Jens J Holst, Ulrik Pedersen-Bjergaard, Sten Madsbad, Tina Vilsbøll, Henrik U Andersen, Filip K Knop
BACKGROUND: In type 2 diabetes, long-acting GLP-1 receptor agonists lower fasting plasma glucose and improve glycaemic control via their insulinotropic and glucagonostatic effects. In type 1 diabetes, their efficacy as an add-on treatment to insulin therapy is modest. Short-acting GLP-1 receptor agonists also lower postprandial glucose excursions in type 2 diabetes by decelerating gastric emptying rate. We aimed to test the efficacy of a short-acting GLP-1 receptor agonist in type 1 diabetes...
April 2020: Lancet Diabetes & Endocrinology
#11
JOURNAL ARTICLE
Elena V Shekunova, Vladimir A Kashkin, Arman А Muzhikyan, Marina N Makarova, Vadim Y Balabanyan, Valery G Makarov
Diabetes mellitus is characterized by metabolic dysregulation associated with a number of health complications. More than 50% of patients with diabetes mellitus suffer from diabetic polyneuropathy, which involves the presence of peripheral nerve dysfunction symptoms. The aim of this study was to evaluate the potential of a new synthetic arginine-rich exendin-4 (Peptide D) in the treatment of complications caused by diabetes, including peripheral neuropathy, in rats. Diabetes was induced by administering streptozotocin (STZ)...
January 5, 2020: European Journal of Pharmacology
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JOURNAL ARTICLE
Liat Soudry-Kochavi, Natalya Naraykin, Rosanna Di Paola, Enrico Gugliandolo, Alessio Peritore, Salvatore Cuzzocrea, Ehud Ziv, Taher Nassar, Simon Benita
One of the major disadvantages associated with macromolecules therapy is that most of them can only be administered parenterally. Exenatide, an efficient anti-diabetic drug, incretin mimetic, is currently administered subcutaneously (SC) causing compliance issues. Nanoparticles (NPs) are considered a promising solution for oral delivery of this drug. In order to overcome exenatide's inability to cross the enterocytes and to increase its stability in the gastrointestinal (GI) tract, we encapsulated exenatide into a nano-in-micro delivery system...
December 2018: European Journal of Pharmaceutics and Biopharmaceutics
#13
JOURNAL ARTICLE
Sebastian Wiberg, Jesper Kjaergaard, Henrik Schmidt, Jakob Hartvig Thomsen, Martin Frydland, Matilde Winther-Jensen, Matias Greve Lindholm, Dan Eik Høfsten, Thomas Engstrøm, Lars Køber, Jacob Eifer Møller, Christian Hassager
OBJECTIVES: To investigate the effects of the glucagon-like peptide-1 analog exenatide on blood glucose, lactate clearance, and hemodynamic variables in comatose, resuscitated out-of-hospital cardiac arrest patients. DESIGN: Predefined post hoc analyzes from a double-blind, randomized clinical trial. SETTING: The ICU of a tertiary heart center. PATIENTS: Consecutive sample of adult, comatose patients undergoing targeted temperature management after out-of-hospital cardiac arrest from a presumed cardiac cause, irrespective of the initial cardiac rhythm...
February 2018: Critical Care Medicine
#14
JOURNAL ARTICLE
Bhargav Prasad Kodaganti, Pavithra Mukunda, Pravinkumar Dakshinamurthy, Yogendra Manjunath, Bharath Ravindra Shenoy, Veeresha Kamanagowda, Bairavabalakumar Natarajan, Amol Maliwalave, Divya Unnikrishnan, Sathyabalan Murugesan, Vivek Halan, Maloy Ghosh, Sunit Maity
Exendin-4 is a GLP 1 agonist incretin-mimetic peptide hormone comprising 39 amino acids. Exenatide (Byetta® ) is a chemically synthesized version of Exendin-4 with an additional C-terminal amidation. Exenatide acts as a GLP-1 receptor agonist. This paper illustrates the method adopted for cloning, fermentation and purification of recombinant Exendin-4 analog expressed in Escherichia coli. The biologically expressed analog was extensively characterized using different orthogonal methods to confirm their biological activity and physicochemical properties...
July 2017: Biologicals: Journal of the International Association of Biological Standardization
#15
JOURNAL ARTICLE
Qing Qiao, Kristina Johnsson, Susan Grandy, Karel Kostev
BACKGROUND: The aim was to investigate real-world treatment outcomes and tolerability of GLP-1 receptor agonist (GLP-1RA) therapy in patients with type 2 diabetes in Germany. METHODS: Patients from 323 primary care practices who started any GLP-1RA therapy (89 Byetta, 108 Bydureon, 347 Victoza patients) between January 1, 2011, and December 31, 2013 (index date) were analyzed retrospectively (Disease Analyzer database, Germany). Changes from baseline in HbA1c, weight, and hypoglycemia were evaluated in 3 follow-up periods of 0-6, 7-12, and 13-18 months...
March 2017: Journal of Diabetes Science and Technology
#16
JOURNAL ARTICLE
P Salehi, I Hsu, C G Azen, S D Mittelman, M E Geffner, D Jeandron
BACKGROUND: Prader-Willi syndrome (PWS) is associated with hyperphagia and hyperghrelinemia with major morbidity because of obesity without effective medical treatment targeting hyperphagia. Exenatide (Byetta [synthetic Exendin-4]; AstraZeneca, Wilmington DE) is a GLP-1 receptor agonist which reduces appetite and weight and may be an effective treatment in PWS. OBJECTIVE: The objective of this study is to determine the effect of a 6-month trial of exenatide on appetite, weight and gut hormones in youth with PWS...
June 2017: Pediatric Obesity
#17
REVIEW
Christian Hölscher
Type 2 diabetes has been identified as a risk factor for Alzheimer's disease (AD) and Parkinson's disease (PD). In the brains of patients with AD and PD, insulin signaling is impaired. This finding has motivated new research that showed good effects using drugs that initially had been developed to treat diabetes. Preclinical studies showed good neuroprotective effects applying insulin or long lasting analogues of incretin peptides. In transgenic animal models of AD or PD, analogues of the incretin GLP-1 prevented neurodegenerative processes and improved neuronal and synaptic functionality and reduced the symptoms of the diseases...
October 25, 2014: Sheng Li Xue Bao: [Acta Physiologica Sinica]
#18
COMPARATIVE STUDY
A J Scheen
Bydureon is a new galenic formulation (long-acting release) of exenatide, the first agonist of Glucagon-Like Peptide-1 (GLP-1) receptors having been commercialized for the management of type 2 diabetes. The microsphere technology permits a prolonged absorption of exenatide from the subcutaneous depot, which allows one injection per week instead of two injections per day with the initial formulation of exenatide (Byetta). The clinical development programme DURATION showed that exenatide 2 mg once weekly more markedly reduces glycated haemoglobin (HbA(1c)), with a similar weight loss but a better digestive tolerance profile (less nausea and vomiting after treatment initiation), compared with the twice daily 10 microg exenatide...
April 2014: Revue Médicale de Liège
#19
JOURNAL ARTICLE
Udo Stauder, Diplom Enginee, Hina Elton, Alfred Penfornis, Steve Edelman
BACKGROUND: Glucagon-like peptide-1 (GLP-1) receptor agonists are a relatively recent addition to the treatment options for type 2 diabetes mellitus (T2DM) and are administered using prefilled pen devices. METHOD: In this open-label task and interview-based pilot study, 3 GLP-1 receptor agonist pen devices-exenatide (Byetta® , Bristol-Myers Squibb/AstraZeneca), liraglutide (Victoza® , Novo Nordisk), and lixisenatide (Lyxumia® , Sanofi-Aventis)-were comparatively assessed in a randomized order in 30 participants with T2DM for ease of use, using a series of key performance measures (time taken to complete a series of tasks, number of user errors [successful performance], and user satisfaction rating)...
January 2014: Journal of Diabetes Science and Technology
#20
JOURNAL ARTICLE
E I Shakhmatova, E V Pimenova, Zh V Shchutskaia
The renal osmoregulatory function was studied in patients with type 2 diabetes mellitus (DM). The renal response to water loading (0.7% b.w.) and simultaneous exenatide (byetta) injection (5 microg) exhibited variation and was dependent on the degree of hyperglycemia. Effective solute-free water excretion was observed in patients with well-controlled DM (HbAlc 6.0 +/- 0.1%), in which CH20 changed from -0.67 +/- 0.2 mL/min to 0.72 +/- 0.2 mL/min. This reaction was absent in patients with poorly controlled DM (HbAlc 8...
2014: Eksperimental'naia i Klinicheskaia Farmakologiia
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