Semaglutide

Semaglutide (trade name Ozempic) is a medication developed by Danish company Novo Nordisk. Originally developed for the treatment of type 2 diabetes in 2012, it was found in 2017 that it can be used for the treatment of obesity. Semaglutide (trade name Ozempic) is a medication developed by Danish company Novo Nordisk. Originally developed for the treatment of type 2 diabetes in 2012, it was found in 2017 that it can be used for the treatment of obesity. The drug has been approved by the US Food and Drug Administration (FDA) in 2017, and by the European Commission, the Health Canada and the Japanese Ministry of Health, Labour and Welfare in 2018. Semaglutide acts like human glucagon-like peptide-1 (GLP-1) so that it increases insulin secretion, thereby increasing sugar metabolism. It is made as subcutaneus injection, and in prefilled pen. One of its advantages over other antidiabetic drugs is that it has a long duration of action, thus, only once-a-week injection is sufficient. Semaglutide is prepared for subcutaneous injection and is available in prefilled pen. It is recommended for once-weekly injection. Semaglutide has minor adverse effects. Nausea, vomiting, diarrhea, abdominal pain, and constipation are usually experienced. In patients with heart (cardiovascular) problem, it causes retinal (eye) damage (retinopathy). Semaglutide is a glucagon-like peptide-1 receptor agonist. It increases the production of insulin, a hormone that lowers the blood sugar level. It also appears to enhance growth of β cells in the pancreas, which are the sites of insulin production. On the other hand it inhibits glucagon, which increases blood sugar. It additionally reduces food intake by lowering appetite and slows down digestion in the stomach. In this way it works in body fat reduction. In humans semaglutide is chemically similar to human glucagon-like peptide-1 (GLP-1), with 94% similarity. The only differences are two amino acid substitutions at positions 8 and 34, where alanine and lysine are replaced by 2-aminoisobutyric acid and arginine respectively. Amino acid substitution at position 8 prevents chemical breakdown by an enzyme dipeptidyl peptidase-4. In addition, lysine at position 26 is in its derivative form (acylated with stearic diacid). Acylation with a spacer and C-18 fatty diacid chain increases the drug binding to blood protein (albumin), which enables longer presence in the blood circulation. Its half-life in the blood is about 7 days (165–184 hours), therefore, once-weekly injection is enough. Semaglutide was discovered in 2012, by a team of researchers at Novo Nordisk as a longer-acting alternative to liraglutide. It was given a brand name Ozempic. Clinical trials were started in 2015, and phase 3 was completed in 2016. Researchers at the University of Leeds and Novo Nordisk reported in 2017 that it can also be used for the treatment of obesity. It reduces hunger, food craving and body fat.