Semalutide is a new generation of GLP-1 (glucagon like peptide-1) analog. Somaglutide is a long-acting dosage form developed based on the basic structure of Lilalutide, which has better therapeutic effect on type 2 diabetes.

Semaglutide  is a polypeptide that contains a linear sequence of 31 amino acids joined together by peptide linkages. It is an agonist of glucagon-like peptide 1 receptors (GLP1 AR) and used for the treatment of type 2 diabetes. 

It has a role as a hypoglycemic agent, a glucagon-like peptide-1 receptor agonist, an anti-obesity agent, a neuroprotective agent and an appetite depressant. It is a polypeptide and a lipopeptide.

effect

Somaglutide is a long-acting dosage form developed based on the basic structure of liraglutide, which has better effect in the treatment of type 2 diabetes.

Preparation

Somaglutide was prepared by solid-liquid phase synthesis method. Solid phase synthesis method was used to prepare straight chain peptides Aib8, Arg34GLP-1 (7-37), and fatty side chain acylating agents. Lys26 was modified with the synthesized fatty chain acylating agent under alkaline conditions to obtain Somaglutide. The biological activity of the self-made samples was determined by time-resolved fluorescence resonance energy transfer immunoassay.

New GLP-1 receptor agonist drugs

Semeglucide is a novel GLP-1 analogue that is injected subcutaneously once a week. Somaglutide is a long-acting GLP-1 analogue developed by Novo Nordisk for subcutaneous injection once per week. Compared with Liraglutide, Somaglutide has a longer fatty chain and increased hydrophobicity. However, Somaglutide is modified with short chain PEG, greatly enhancing its hydrophilicity. 

PEG modification can not only tightly bind to albumin, mask the DPP-4 enzyme hydrolysis site, but also reduce renal excretion, prolong biological half-life, and achieve long-term circulation effects.

Novo Nordisk's Somaglutide suspension beats DPP-4's Siagliptin, and GLP-1's ancestor long-acting Esenatide (should be designed to compete head-on with Lily's trustiness, bullying has long been on the market). In the experiment, high-dose Soma reduced A1C by 1.6% and resulted in a maximum weight loss of 6kg.

Somaglutide was tested in 813 patients with type 2 diabetes to investigate the efficacy and safety of 1.0 mg Somaglutide compared with 2.0 mg Exenatide injected once a week. The trial period was 56 weeks, and the patients took 1-2 anti diabetes drugs orally at the same time.