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Liraglutide, a so-called glucagon like peptide-1 (GLP-1) receptor agonist, is used for the treatment of Type 2 diabetes mellitus and obesity.
Released By Bachem
September 28, 2021
Liraglutide, a so-called glucagon like peptide-1 (GLP-1) receptor agonist, is used for the treatment of Type 2 diabetes mellitus (T2D) and obesity. Marketed as Victoza® and Saxenda® by Novo Nordisk, the drug is a peptide analog of the human GLP-1, a hormone with many functions in the human body. Normally, the peptide hormone GLP-1 is formed in the intestine depending upon the presence of food there and it delays gastric emptying. Interestingly, GLP-1 is lower than normal in people with T2D. Depending on the concentration of glucose in the intestine, GLP-1 inhibits the release of glucagon from the pancreas and, together with glucose, promotes the release of insulin by binding to specific GLP1-receptors on the surface of the insulin-producing cells of the pancreas. The action of GLP-1 is quickly inactivated by the enzyme dipeptidyl-peptidase–IV (DPP-IV), a protease that splits and thereby inactivates peptides or proteins circulating in the human body. Thus, insulin release is regulated by GLP-1, DPP-IV and glucose. This mechanism ensures that the amount of insulin in circulation is not excessive and that hypoglycemia will not occur. Liraglutide is a long-acting peptide analog of GLP-1, because of a better resistance to DDP-IV-mediated degradation due to the presence of a fatty acid side-chain. Compared to GLP-1 with a half-life of a few minutes1, this once-daily peptide analog given by injection under the skin offers a half-life prolonged to 13 hours2. Liraglutide enables an efficient weight loss and glycemic management. For these effects, the drug was first approved by the FDA for the management of T2D in adults in 2010, then, in 2014, for the treatment of obesity in adults who have at least one weight-related condition, and later on, in 2019, also for the treatment of children 10 years or older with T2D.
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