Sermaglutide/910463-68-2

Introduction to Sermaglutide/910463-68-2

Introduction to Semaglutide Usage and Synthesis Method Semaglutide (semaglutide)

It is a new generation of GLP-1 (glucagon-like peptide-1) analog developed by Novo Nordisk, Denmark. Somaglutide is a long-acting formulation developed based on the basic structure of liraglutide. It is more effective in treating type 2 diabetes. Novo Nordisk has completed six PhaseIIIa studies of somaglutide injections and has submitted a new drug registration application for somaglutide injections once a week to the U.S. Food and Drug Administration (FDA) on December 5, 2016.

On the other hand, the once-daily oral preparation of somaglutide is currently in clinical phase III.

The effect of semaglutide

Somaglutide is a long-acting formulation developed based on the basic structure of liraglutide, and it has a better effect on the treatment of type 2 diabetes.

Semaglutide manufacturer’s preparation

Somaglutide was prepared by solid-liquid phase synthesis method. The linear peptide Aib8, Arg34GLP-1(7-37) and the fatty side chain acylating agent were prepared by solid-phase synthesis, and the linear peptide Lys26 was modified with the synthetic fatty chain acylating agent under alkaline conditions to obtain Soma Lutide, and time-resolved fluorescence resonance energy transfer immunoassay for the biological activity of self-made samples.

GLP-1 receptor agonist new drug peptides

Semeglutide is a new type of GLP-1 analog that is injected subcutaneously once a week. Somaglutide is a long-acting GLP-1 analog developed by Novo Nordisk for subcutaneous injection once/w. Compared with liraglutide, somaglutide has a longer aliphatic chain and increased hydrophobicity, but somaglutide is modified with a short chain of PEG, and its hydrophilicity is greatly enhanced. After PEG modification, it can not only bind tightly to albumin, cover up the site of DPP-4 enzymatic hydrolysis, but also reduce renal excretion, prolong the biological half-life, and achieve the effect of long circulation. Novo Nordisk’s Somaglutide beats DPP-4 Sitagliptin, and the long-acting Exenatide, the originator of GLP-1 (it should be designed to compare head-to-head with Lilly’s truth, bully has been on the market long ago).

In the trial, the high-dose Soma reduced A1C by 1.6% and reduced body weight by up to 6 kg. The trial of semaglutide investigated the efficacy and safety of 1.0 mg semaglutide compared with a weekly injection of 2.0 mg exenatide in 813 type 2 diabetic patients. The trial period was 56 weeks. Oral 1-2 kinds of anti-diabetic drugs when same as Chemicalbook.

In December 2017, the FDA officially approved NovoNordisk’s once-a-week GLP-1 hypoglycemic drug somaglutide to be marketed under the trade name Ozempic. According to clinical trial data, compared with placebo, Merck’s Januvia, AstraZeneca’s Bydureon and Sanofi’s Lantus, Ozempic can reduce HbA1c levels. The drug also showed the ability to help patients lose weight. As a leader in the field of diabetes, NovoNordisk (NovoNordisk) is not only in the insulin field, its development of human glucagon-like peptide-1 (GLP-1) analogue Liraglutide (Liraglutide, trade name) : Victoza)

Since its listing in 2009, it has been dominating the GLP-1 market. In 2016, the global sales reached 3.2 billion U.S. dollars, which is fruitful. Liraglutide compounds have expired, and generic drug companies are eyeing them. In order to prevent problems before they happen, Novo Nordisk has already prepared the next generation of liraglutide, which is somaglutide.

From the structural point of view, Semeglutide is the GLP-1(7-37) chain with Aib at position 8 instead of Ala, Arg at position 34 instead of Lys, and Lys at position 26 connected to octadecanoic acid aliphatic chain. Compared with Liraglutide, Semeglutide has a longer aliphatic chain and increased hydrophobicity, but Semeglutide has been modified with a short chain of PEG to greatly increase its hydrophilicity.

After PEG modification, it can not only bind tightly to albumin, cover up the site of DPP-4 enzymatic hydrolysis, 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 predicts that its drug sales will reach US$2.2 billion in 2022. At the same time, Novo Nordisk is actively developing oral dosage forms of somaglutide, gradually consolidating its dominant position in the field of diabetes.

What is the biological activity of semaglutide?

Biologically active Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC0113-0217) is a long-acting glucagon-like peptide 1 (GLP-1) analogue, an agonist of GLP-1 receptor, and potential type 2 diabetes (T2DM) Therapeutic efficacy.

How to buy semaglutide in the U.S.

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