Pharmacological effect
1. Unique bias mechanism: Selectively activates the cAMP pathway downstream of the GLP-1 receptor, significantly reducing the recruitment of β-arrestin and the in vivo endocytosis and desensitization of GLP-1 R receptors; The receptor remains on the cell membrane for a long time, maintaining continuous efficacy and belongs to a new generation of biased GLP-1 agonists.
2. Glucose-dependent insulin secretion promotion: When blood sugar rises, it promotes the secretion of insulin by pancreatic β cells; when blood sugar is normal, it is almost not activated, and the risk of hypoglycemia is low. It inhibits glucagon release, reduces liver sugar output, and effectively lowers glycated hemoglobin and postprandial blood glucose.
3. It delays gastric emptying, acts on the appetite center of the hypothalamus, enhances satiety, reduces food intake, and has a remarkable weight loss effect.
4. Long-term modification: 8-bit Ala mutates to Val; The Lys30 side chain is linked to double AEEA+γ-Glu+C18 diacid, which binds to albumin and resizes degradation by DPP-4 /NEP enzyme, allowing for subcutaneous injection once a week.
IDA