Semaglutide is a new generation GLP-1 (glucagon-like peptide-1) analogue developed by NovoNordisk, a Danish company. Semaglutide is a long-acting formulation based on the basic structure of Liraglutide, which is more effective in the treatment of type 2 diabetes. Novo Nordisk has completed six studies for Somarutide Injection and submitted an application to the U.S. Food and Drug Administration (FDA) for New drug registration for Somarutide injection once a week on December 5, 2016. An application for Marketing Authorization (MAA) has also been submitted to the European Medicines Agency (EMA). On the other hand, the once-daily oral formulation of sommarutide is currently in phase III.
Semaglutide is a long-acting formulation based on the basic structure of liraglutide, which is more effective in the treatment of type 2 diabetes.
Semaglutide was prepared by solid-liquid synthesis method. Straight chain peptide Aib8, Arg34GLP-1(7-37) and aliphatic side chain acylating agent were prepared by solid phase synthesis. Under alkaline conditions, the aliphatic acylating agent formed by was used to modify the straight chain peptide Lys26 to obtain Semaglutide. The bioactivity of the self-made samples was determined by time-resolved fluorescence resonance energy transfer immunoassay.
Semeglutide is a novel GLP-1 analogue injected subcutaneously once a week. Semeglutide is a long-acting GLP-1 analogue developed by Novo Nordisk with a 1 /w subcutaneous injection. Compared with Liraglutide, Semeglutide has longer fat chain and increased drophobicity, but Semeglutide is modified with short chain PEG, which greatly enhances drophilicity. After PEG modification, it can not only bind with albumin closely, cover the drolysis site of DPP-4 enzyme, but also reduce renal excretion and prolong biological half-life, so as to achieve the effect of long cycle. Novo Nordisk’s Sommarutide hits 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). High dose decreased A1C1.6% and decreased body weight by up to 6kg. The trial examined the efficacy and safety of 1.0mg of sommarutide compared with a weekly dose of 2.0mg of exenatide in 813 patients with type 2 diabetes over a period of 56 weeks with one or two oral antidiabetic agents. In December 2017, the FDA officially approved NovoNordisk’s once-a-week GLP-1 drug, Sommarutide, marketed as Ozempic. Ozempic reduced HbA1c levels compared with placebos such as Merck’s Januvia, Astrazeneca’s Bydureon and Sanofi’s Lantus, according to clinical trial data. The drug has also shown the ability to help patients lose weight.