| Pharmacological profile of lixisenatide: A new GLP-1 receptor agonist for the treatment of type 2 diabetes. | |
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MedLine Citation:
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PMID: 20570597 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The glucagon-like peptide-1 (GLP-1) receptor represents an established therapeutic target in type 2 diabetes mellitus (T2DM). Agents that activate this receptor improve glucose tolerance alongside a low risk of hypoglycaemia, and have the potential to modify disease progression. Lixisenatide is a new potent and selective GLP-1 receptor agonist currently in development. The preclinical pharmacological profile of Lixisenatide suggests actions that are highly relevant to the long-term maintenance of glucose homeostasis. Lixisenatide protected Ins-1 cells (a rat-derived beta-cell line) from both lipid- and cytokine-induced apoptosis. More importantly, Lixisenatide also prevented lipotoxicity-induced insulin depletion in human islets and preserved insulin production, storage and pancreatic beta-cell function in vitro. Enhancement of insulin biosynthesis and pancreatic beta-cell volume could also be demonstrated in animal models of type 2 diabetes. The improvement of glucose-stimulated insulin secretion provided by Lixisenatide occurred in a strictly glucose-dependent manner. In animal models of diabetes, Lixisenatide improved basal blood glucose and HbA(1c) with a rapid onset and sustained duration of action, and prevented the deterioration of pancreatic responsiveness and glucose homeostasis. Lixisenatide also delayed gastric emptying and reduced food intake. The efficacy/safety profile of Lixisenatide is currently being studied further in an extensive ongoing Phase III clinical study programme. This article reviews the preclinical pharmacological profile of Lixisenatide. |
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Authors:
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Ulrich Werner; Guido Haschke; Andreas W Herling; Werner Kramer |
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Publication Detail:
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Type: Journal Article; Review Date: 2010-06-02 |
Journal Detail:
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Title: Regulatory peptides Volume: 164 ISSN: 1873-1686 ISO Abbreviation: Regul. Pept. Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-08-23 Completed Date: 2011-01-12 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8100479 Medline TA: Regul Pept Country: Netherlands |
Other Details:
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Languages: eng Pagination: 58-64 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier B.V. All rights reserved. |
Affiliation:
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Sanofi-Aventis Deutschland GmbH, Frankfurt am Main, Germany. ulrich.werner@sanofi-aventis.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Diabetes Mellitus, Type 2 / drug therapy* Humans Hypoglycemic Agents / therapeutic use* Peptides / therapeutic use* Receptors, Glucagon / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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0/Hypoglycemic Agents; 0/Peptides; 0/Receptors, Glucagon; 0/ZP10A peptide; 0/glucagon-like peptide receptor |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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