Analysis of the target and physiological mechanism of action of tilpotide/tilsiparatide (Mufenda)

Tirzepatide (Tirzepatide) is an innovative multi-target metabolic drug that has attracted much attention in recent years. Its core mechanism is to act on the GIP receptor and the GLP-1 receptor at the same time. It is a "dual receptor agonist". These two types of receptors themselves are involved in human body blood sugar regulation, insulin secretion and appetite control. Therefore, by stimulating both pathways at the same time, drugs can further enhance metabolic regulation function on the basis of strengthening blood sugar lowering. This "dual-target" design not only improves the efficacy of hormone signaling, but also improves the comprehensiveness of overall metabolic improvement, which is the key reason why the clinical performance of tisiparatide is better than that of traditional single GLP-1 drugs.

In terms of physiological effects, tisiparatide can significantly enhance the sensitivity of beta cells to glucose, allowing the body to secrete more insulin when blood sugar rises, while reducing unnecessary activation when blood sugar is normal, thereby reducing the risk of hypoglycemia. The drug can also inhibit the secretion of glucagon, causing the liver to reduce glucose output, ultimately stabilizing and lowering blood sugar. This characteristic of "adaptive secretion regulation according to blood sugar fluctuations" enables tisiparatide to show stronger blood sugar management capabilities in the treatment of type 2 diabetes, allowing many patients to significantly improve their glycated hemoglobin values.

In addition to lowering blood sugar, tilsiparatide also has a significant effect on weight regulation. It acts on the central feeding center to reduce appetite, delay gastric emptying, and make patients more likely to feel full, thereby naturally reducing caloric intake. In addition, activation of the dual targets can promote increased energy metabolism in adipose tissue, improve fat oxidation efficiency, and help reduce visceral fat and subcutaneous fat. For this reason, tilsiparatide has shown a strong weight loss effect in clinical trials. It is not only effective for obese patients with diabetes, but also some non-diabetic obese people can achieve significant weight loss.

Taken together, tilsiparatide achieves the triple effects of hypoglycemic, food-suppressing and metabolism-promoting effects through the "dual-target linkage" mechanism. It is one of the most representative innovative drugs in the current metabolic field. Its advantages are not only reflected in precise and stable blood sugar control, but also in outstanding performance in weight management. As more research data are released, the clarity of its mechanism and applicable population will be further expanded, but tilsiparatide has shown strong therapeutic potential whether it is diabetes treatment or weight management.

Reference materials:https://pubmed.ncbi.nlm.nih.gov/36251836/