910463-68-2
Sermaglutide
CAS: 910463-68-2
Molecular Formula: C187H291N45O59
910463-68-2 - Names and Identifiers
| Name | Sermaglutide |
| Synonyms | Ozempic Sermaglutide Ozempic, Rybelsus Semaglutide impurity Semaglutide fandachem |
| CAS | 910463-68-2 |
| EINECS | 203-405-2 |
910463-68-2 - Physico-chemical Properties
| Molecular Formula | C187H291N45O59 |
| Appearance | White powder |
| Storage Condition | 2-8℃ |
| Physical and Chemical Properties | Bioactive Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217) is a long-acting glucagon-like peptide 1 (GLP-1) analog, GLP-1 receptor agonists, with potential therapeutic efficacy in type 2 diabetes mellitus (T2DM). |
| Use | Action Somaglutide is a long-acting dosage form developed based on the basic structure of liraglutide, and its effect in the treatment of type 2 diabetes is better. |
910463-68-2 - Uses and synthesis methods
Introduction
Somaglutide (semaglutide) is a new generation of GLP-1 (glucagon-like peptide -1) analog developed by Novo Nordisk (NovoNordisk) in Denmark. Somaglutide is based on the basic structure of liraglutide The long-acting dosage form developed is better for the treatment of type 2 diabetes. Novo Nordisk has completed six PhaseIIIa studies of Somaglutide injection and submitted a new drug registration application for Somaglutide injection once a week to the US Food and Drug Administration (FDA) on December 5, 2016, as well as a marketing authorization application (MAA) to the European Drug Administration (EMA). On the other hand, a once-daily oral formulation of somaglutide is currently in clinical phase III.
Preparation
Somaglutide was prepared by solid-liquid phase synthesis. The straight-chain peptide Aib8,Arg34GLP-1(7-37) and fat side chain acylating agent were prepared by solid-phase synthesis method, and the straight-chain peptide Lys26 was modified with the synthesized fat chain acylating agent under alkaline conditions to obtain Somalutide, and the biological activity of the self-made sample was determined by time-resolved fluorescence resonance energy transfer immunoassay.
Somaglutide (Semeglutide), a new drug GLP-1 receptor agonist, is a new GLP-1 analog injected subcutaneously once a week. Somaglutide is a long-acting GLP-1 analog injected subcutaneously once/w developed by Novo Nordisk. Compared with liraglutide, somaglutide is a longer fat chain and increased hydrophobicity, but somaglutide is modified by PEG of short chains and its hydrophilicity is greatly enhanced. After PEG modification, it can not only tightly bind with albumin to cover the hydrolysis site of DPP-4 enzyme, but also reduce renal excretion, prolong the biological half-life and achieve the effect of long circulation. Novo Nordisk's Somaglutide hangs DPP-4 sitagliptin, and GLP-1 originator long-acting exenatide (should be designed to be compared with lilly's trulicity head-to-head, bullying has long been on the market). In the test, high-dose SOMA reduced A1C 1.6% and weight by up to 6kg.
Somaglutide This trial examined the efficacy and safety of 1.0 mg of somaglutide compared with a weekly injection of 2.0 mg exenatide in 813 patients with type 2 diabetes. The trial period was 56 weeks, and patients took 1-2 antidiabetic drugs orally.
in December 2017, FDA officially approved the weekly GLP-1 hypoglycemic drug Somaglutide developed by Novo Nordisk under the trade name of Ozempic. According to clinical trial data, Ozempic can reduce HbA1c levels compared with placebo, Merck's Januvia, AstraZeneca's Bydureon and Sanofi's Lantus. The drug also shows the ability to help patients lose weight.
as a leader in the field of diabetes, Novo Nordisk not only has a three-part world in the field of insulin, but also has developed human glucagon-like peptide -1(GLP-1) similar to liraglutide (Liraglutide, trade name: Victoza). since its listing in 2009, Novo Nordisk has been the dominant player in the GLP-1 market, with global sales reaching 3.2 billion us dollars in 2016, which is fruitful.
liraglutide compounds have expired, generic pharmaceutical companies are eyeing up. In order to prevent problems before they occur, Novo Nordisk has already prepared the next generation of liraglutide, which is Somaglutide. From the structural point of view, the Semeglutide is that Aib at position 8 on the GLP-1(7-37) chain replaces Ala, Arg at position 34 replaces Lys, and Lys at position 26 is connected to the ocadanoic acid fat chain. Compared with Liraglutide, the fat chain of the Semeglutide is longer and the hydrophobicity is increased, but the hydrophilicity is greatly enhanced Semeglutide the PEG modification of the short chain. After PEG modification, it can not only tightly bind with albumin to cover the hydrolysis site of DPP-4 enzyme, but also reduce renal excretion, prolong the biological half-life and achieve the effect of long circulation.
according to analysis, Ozempic is expected to become 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 Somaglutide to gradually consolidate its dominant position in the field of diabetes.
Target
Target Value
GLP-1 receptor
Last Update：2024-04-09 18:58:34
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