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GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus.Nat Rev Endocrinol.2012 Dec;8(12):728-42.
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2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
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Improved glycemic control and reduction of cardiometabolic risk factors in subjects with type 2 diabetes and metabolic syndrome treated with exenatide in a clinical practice setting. Diabetes TechnolTher. 2009 Jun;11(6):353-9.
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Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
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URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 249).
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Dual GIP and GLP-1 Receptor Agonist Tirzepatide Improves Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes. J Clin Endocrinol Metab. 2021 Jan 23;106(2):388-396.
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Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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Clinical pipeline report, company report or official report of Gmax Biopharm.
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Clinical pipeline report, company report or official report of Gmax Biopharm.
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Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist. Proc Natl Acad Sci U S A. 2020 Nov 24;117(47):29959-29967.
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Clinical pipeline report, company report or official report of PegBio
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Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity? Expert Opin Investig Drugs. 2023 May;32(5):355-359.
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Pharmacokinetic and pharmacodynamic properties of taspoglutide, a once-weekly, human GLP-1 analogue, after single-dose administration in patients with Type 2 diabetes. Diabet Med. 2009 Nov;26(11):1156-64.
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PREVENT: A Randomized, Placebo-controlled Crossover Trial of Avexitide for Treatment of Postbariatric Hypoglycemia. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3235-e3248.
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Clinical pipeline report, company report or official report of Boehringer Ingelheim.
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Emerging glucagon-like peptide 1 receptor agonists for the treatment of obesity. Expert Opin Emerg Drugs. 2021 Sep;26(3):231-243.
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Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
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Role and development of GLP-1 receptor agonists in the management of diabetes. Diabetes Metab Syndr Obes. 2009; 2: 37-49.
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Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
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LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.
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GLP-1 Receptor Agonist NLY01 Reduces Retinal Inflammation and Neuron Death Secondary to Ocular Hypertension. Cell Rep. 2020 Nov 3;33(5):108271.
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Clinical pipeline report, company report or official report of Novo Nordisk A/S.
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Novel glucagon-like peptide-1 analog delivered orally reduces postprandial glucose excursions in porcine and canine models. J Diabetes Sci Technol. 2010 Nov 1;4(6):1516-23.
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On-target Effects of GLP-1 Receptor Agonists on Thyroid C-cells in Rats and Mice. Toxicol Pathol February 2013 vol. 41 no. 2 303-309.
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Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists. Mol Cell. 2020 Nov 5;80(3):485-500.e7.
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ClinicalTrials.gov (NCT05579977) A PHASE 2, RANDOMIZED, DOUBLE-BLIND, PLACEBO CONTROLLED, DOSE RANGING, DOSE FINDING, PARALLEL GROUP STUDY TO ASSESS EFFICACY AND SAFETY OF PF-07081532, AND OPEN LABEL ORAL SEMAGLUTIDE, IN ADULTS WITH TYPE 2 DIABETES MELLITUS (T2DM) INADEQUATELY CONTROLLED ON METFORMIN, AND SEPARATELY PF-07081532 COMPARED TO MATCHING PLACEBO IN ADULTS WITH OBESITY BUT WITHOUT T2DM. U.S.National Institutes of Health.
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Clinical pipeline report, company report or official report of Regor Therapeutics
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Antibody semorinemab reduces tau pathology in a transgenic mouse model and engages tau in patients with Alzheimer's disease. Sci Transl Med. 2021 May 12;13(593):eabb2639.
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Relationship between systemic cytokines and complement factor H Y402H polymorphism in patients with dry age-related macular degeneration. Am J Ophthalmol. 2013 Dec;156(6):1176-83.
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Small Molecule Drug Discovery at the Glucagon-Like Peptide-1 Receptor. Exp Diabetes Res. 2012; 2012: 709893.
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Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics)--preclinical and clinical results. Best Pract Res Clin Endocrinol Metab. 2009 Aug;23(4):463-77.
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Clinical pipeline report, company report or official report of AstraZeneca
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GLP-1 receptor activation inhibits VLDL production and reverses hepatic steatosis by decreasing hepatic lipogenesis in high-fat-fed APOE*3-Leiden mice. PLoS One. 2012;7(11):e49152.
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Clinical pipeline report, company report or official report of Carmot Therapeutics.
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Chemically programmed antibodies. Trends Biotechnol. 2014 April; 32(4): 186-197.
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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
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GZR18, a novel long-acting GLP-1 analog, demonstrated positive in vitro and in vivo pharmacokinetic and pharmacodynamic characteristics in animal models. Eur J Pharmacol. 2022 Aug 5;928:175107.
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IBI362?(LY3305677), a weekly-dose GLP-1 and glucagon receptor dual agonist, in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple ascending dose phase 1b study. EClinicalMedicine. 2021 Aug 13;39:101088.
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Clinical pipeline report, company report or official report of Addex Pharmaceuticals.
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Clinical pipeline report, company report or official report of Novo Nordisk A/S.
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Effects of ALT-801, a GLP-1 and glucagon receptor dual agonist, in a translational mouse model of non-alcoholic steatohepatitis. Sci Rep. 2022 Apr 23;12(1):6666.
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Company report (Sanofi) (drug: LIXisenatide)
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Company report (Zealandpharma)
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2011 Pipeline of Zydus Cadila Group.
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Pharmacokinetics and tolerability of a novel long-acting glucagon-like peptide-1 analog, CJC-1131, in healthy and diabetic subjects. Int J Clin Pharmacol Ther. 2008 Sep;46(9):443-52.
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Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Sep;25(7):565-97.
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Company report (Roche pipeline: October 16, 2012)
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Reversal of diabetes in rats using GLP-1-expressing adult pancreatic duct-like precursor cells transformed from acinar to ductal cells. Stem Cells Dev. 2009 Sep;18(7):991-1002.
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Glucagon-like peptide-1 analogue LY315902: effect on intestinal motility and release of insulin and somatostatin. Regul Pept. 2002 Jun 15;106(1-3):89-95.
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Clinical pipeline report, company report or official report of CinFina Pharma
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US patent application no. 2011,0171,312, Modified therapeutic peptides, methods of their preparation and use.
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2005 approvals: Safety first. Nature Reviews Drug Discovery 5, 92-93 (February 2006).
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A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification. Nat Chem Biol. 2014 Aug;10(8):629-31.
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Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo acti... J Med Chem. 2008 May 8;51(9):2758-65.
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Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4395-8.
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Search for alpha-helical propensity in the receptor-bound conformation of glucagon-like peptide-1. Bioorg Med Chem. 2008 Dec 1;16(23):10106-12.
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