Exenatide (exendin-4) is sold under the brand name BYETTA to improve glycemic control in people with type 2 diabetes mellitus. Exenatide is a glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose-dependent insulin secretion by the pancreatic beta cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying. The drug also moderates peak serum glucagon levels during hyperglycemic periods following meals but does not interfere with glucagon release in response to hypoglycemia.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12629557
Curator's Comment: Referenced study was conducted in mice
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P43220 Gene ID: 2740.0 Gene Symbol: GLP1R Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | BYETTA Approved UseBYETTA (exenatide) is a glucagon-like peptide-1 (GLP-1) receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Launch Date2005 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| High fat diet and GLP-1 drugs induce pancreatic injury in mice. | 2014-04-15 |
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| Pulmonary GLP-1 receptor increases at birth and exogenous GLP-1 receptor agonists augmented surfactant-protein levels in litters from normal and nitrofen-treated pregnant rats. | 2013-03 |
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| On-target effects of GLP-1 receptor agonists on thyroid C-cells in rats and mice. | 2013-02 |
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| Oleic acid and glucose regulate glucagon-like peptide 1 receptor expression in a rat pancreatic ductal cell line. | 2012-10-15 |
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| Down-regulation of zinc transporter 8 in the pancreas of db/db mice is rescued by Exendin-4 administration. | 2010-09-01 |
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| Diabesity: therapeutic options. | 2010-06 |
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| Biochemical, pharmaceutical and therapeutic properties of long-acting lithocholic acid derivatized exendin-4 analogs. | 2010-03-03 |
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| Exendin-4 exerts osteogenic actions in insulin-resistant and type 2 diabetic states. | 2010-01-08 |
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| Preparation and structural, biochemical, and pharmaceutical characterizations of bile acid-modified long-acting exendin-4 derivatives. | 2009-11-12 |
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| Exenatide-associated ischemic renal failure. | 2009-02 |
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| Caudal brainstem processing is sufficient for behavioral, sympathetic, and parasympathetic responses driven by peripheral and hindbrain glucagon-like-peptide-1 receptor stimulation. | 2008-08 |
|
| Glucagon-like peptide 1 receptor stimulation reverses key deficits in distinct rodent models of Parkinson's disease. | 2008-05-21 |
| Substance Class |
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| Sequence Type | COMPLETE |
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9P1872D4OL
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NDF-RT |
N0000170335
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A10BJ01
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QA10BX04
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N0000178480
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N0000020058
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NBK548665
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EXENATIDE
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C65611
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_39] | SERINE | SERINAMIDE | CIJ0MD19SE |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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