Glucagon-Like Peptide-1 (GLP-1) Analogues

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Information about Glucagon-Like Peptide-1 (GLP-1) Analogues

Glucagon-like peptide-1 (GLP-1) is an incretin, a gastrointestinal polypeptide hormone that binds to specific receptors on pancreatic beta cells and increases insulin release. The incretins – GLP-1 and gastric inhibitory peptide (GIP) – are secreted from the upper gastrointestinal tract in response to feeding and act on the pancreas, increasing insulin release even before blood glucose levels are elevated.

Mechanism of action of Glucagon-Like Peptide-1 (GLP-1) Analogues

The incretins also delay gastric emptying and suppress glucagon secretion, features that may increase their beneficial effects in type 2 diabetes. Both hormones are polypeptides that are rapidly cleared from the serum by the peptide cleaving enzyme, dipeptidyl peptidase-4 (DPP-4). The incretin pathway provides several potential targets for therapy of type 2 diabetes, the main ones being DPP-4 (inhibition) and GLP-1 receptors (agonist activity).

List of Glucagon-Like Peptide-1 (GLP-1) Analogues

Several GLP-1 analogues (also called GLP-1 receptor agonists) have been developed and approved for use in the United States for type 2 diabetes: exenatide (also known as exendin-4, Byetta) in 2005, liraglutide (Victoza) in 2010, albiglutide (Tanzeum) and dulaglutide (Trulicity) in 2014, and lixisenatide (Adlyxin) in 2016. All are given parenterally and are approved for use in type 2 diabetes only. The GLP-1 analogues are recombinant polypeptides, have little or no hepatic metabolism and have not been convincingly implicated in causing clinically apparent liver injury.

Drug class for Glucagon-Like Peptide-1 (GLP-1) Analogues

Drug Class: Antidiabetic Agents

Drugs in the Subclass Incretin-Based Drugs, Glucagon-Like Peptide-1 (GLP-1) Analogues: Albiglutide, Dulaglutide, Exenatide, Liraglutide, Lixisenatide


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