Semaglutide CAS 910463-68-2
Semaglutide CAS 910463-68-2
Eric
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intro
semaglutide is a new generation GLP-1 (glucagon-like peptide-1) analogue developed by NovoNordisk, Denmark. Semaglutide is a long-acting formulation based on the basic structure of Liraglutide, which is more effective in treating type 2 diabetes. Novo Nordisk has completed six PhaseIIIa studies for its Sommarutide injection and has submitted a New drug registration application for its once-weekly injection with the U.S. Food and Drug Administration (FDA) and a marketing Authorization application (MAA) to the European Medicines Agency (EMA) on December 5, 2016. On the other hand, a once-daily oral formulation of sommarlutide is currently in phase III.
effect
Sommarlutide is a long-acting formulation based on the basic structure of Liraglutide, which is more effective in the treatment of type 2 diabetes.
preparation
Sommarutide was prepared by solid-liquid phase synthesis method. Straight chain peptide Aib8, Arg34GLP-1(7-37) and fatty side chain acylating agent were prepared by solid phase synthesis method. Straight chain peptide Lys26 was modified by synthetic fatty chain acylating agent under alkaline conditions to obtain sommarutide. The biological activity of self-made samples was determined by time-resolved fluorescence resonance energy transfer immunoassay.
New drug class of GLP-1 receptor agonists
Semeglutide is a novel GLP-1 analogue that is injected subcutaneously once a week. Sommarlutide is a long-acting GLP-1 analogue developed by Novo Nordisk with 1 /w subcutaneous injection. Compared with lilaplutide, sommarlutide has a longer fat chain and an increased hydrophobicity, but sommarlutide is modified by short chain PEG and its hydrophilicity is greatly enhanced. After PEG modification, it can not only bind to albumin closely, cover the hydrolysis site of DPP-4 enzyme, but also reduce renal excretion, prolong biological half-life, and achieve a long cycle effect. Novo Nordisk's sommarutide slings off DPP-4's Sitagliptin, and GLP-1's progenitor, long-acting exenatide (should be designed to compete head-to-head with lilly's trulicity, bullying has long been on the market). In the trial, high dose of soma decreased A1C1.6% and reduced body weight up to 6kg. The trial examined the efficacy and safety of 1.0mg of sommarutide compared with a weekly injection of 2.0mg of exenatide in 813 patients with type 2 diabetes over a 56-week period in which patients were treated with two oral antidiabetic drugs, 1-chemicalbook1. In December 2017, the FDA officially approved NovoNordisk's once-a-week GLP-1 drug, Sommarutide, under the brand name Ozempic. According to clinical trial data, Ozempic reduced HbA1c levels compared with placebos, Merck's Januvia, Astrazeneca's Bydureon and Sanofi's Lantus. The drug has also shown an ability to help patients lose weight. As a leader in the field of diabetes, NovoNordisk (NovoNordisk) not only in the field of insulin three points, its development of human glucagon like peptide-1 (GLP-1) analogue Liraglutide (trade name: Victoza, since its listing in 2009, has dominated the GLP-1 market, with global sales of up to $3.2 billion in 2016. Liraglutide has expired, and generic drug companies are eyeing it. To prevent this from happening, Novo Nordisk has already prepared the next generation of Liraglutide, which is sommarlutide. Structurally,Semeglutide is a GLP-1(7-37) chain with 8-bit Aib replacing Ala, 34-bit Arg replacing Lys, and 26-bit Lys attached to the stearic acid fatty chain. Compared to Liraglutide, Semeglutide has a longer fat chain and an increased hydrophobicity, but Semeglutide is modified by short chain PEG and its hydrophilicity is greatly enhanced. After PEG modification, it can not only bind to albumin closely, cover the hydrolysis site of DPP-4 enzyme, but also reduce renal excretion, prolong biological half-life, and achieve a long cycle effect. According to the analysis, Ozempic is expected to be one of the best-selling drugs in 2017. Novo Nordisk forecasts drug sales of $2.2 billion in 2022. At the same time, Novo Nordisk is actively developing oral dosage forms of sommarutide, gradually consolidating its dominance in the diabetes field.
Bioactive
Semaglutide (Rybelsus, Ozempic NN9535, OG217SC, NNC0113-0217) is a kind of long-term pancreatic glucagon like peptide 1 (glp-1) analogue, glp-1 receptor agonist, It has potential therapeutic efficacy for type 2 diabetes mellitus (T2DM).
