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1kits（10Vials）
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▎Retatrutide Structure
Source: PubChem | Sequence: YA¹QGTFTSDYSI-L²LDKK⁴AQA¹AFIEYLLEGGPSSGAPPPS³ Molecular Formula: C221H342N46O68 Molecular Weight: 4731 g/mol CAS Number: 2381089-83-2 PubChem CID: 171390338 Synonyms：LY3437943 |
▎Retatrutide Research
What is the research background of Retatrutide?
The research background of Retatrutide is closely related to the increasingly severe global issues of obesity and diabetes, as well as the limitations of existing therapeutic drugs: obesity and diabetes pose a serious threat to public health, with the global obesity population projected to reach 4.005 billion by 2035 and the number of diabetes patients increasing to 592 million, resulting in significant global healthcare expenditures due to diabetes. Multi-target receptor agonist peptides have emerged as a solution, capable of preventing obesity, treating diabetes, and avoiding the toxic side effects of existing drugs, making them a trend in the development of obesity and diabetes treatments.
What is the mechanism of action of Retatrutide?
Regulating energy metabolism through multi-receptor activation
Retatrutide is a triple receptor agonist targeting the glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon-like peptide-1 receptor (GLP-1R), and glucagon receptor (GCGR). It simultaneously activates these three receptors, regulating energy metabolism through multiple pathways.
GIPR agonist action:
GIP is an intestinal insulin-secreting hormone secreted by intestinal K cells and released after meals. Retatrutide activates the GIPR, promoting insulin secretion, enhancing insulin sensitivity, and thereby helping the body more effectively absorb and utilize glucose, thereby lowering blood glucose levels. Additionally, GIP may influence fat metabolism by regulating adipocyte function and reducing fat accumulation[1].
GLP-1R agonist activity:
GLP-1 is a peptide hormone secreted by intestinal L cells. After activating GLP-1R, Retatrutide produces various beneficial effects. It can stimulate insulin secretion in a glucose concentration-dependent manner, thereby lowering blood sugar levels. It can delay gastric emptying, increase satiety, and reduce food intake. GLP-1R agonism may also act on the central nervous system, regulating appetite and energy balance, thereby aiding in weight loss[2].
GCGR agonist effects:
Glucagon typically increases blood glucose levels, but under the influence of Retatrutide, GCGR agonism produces different effects. It promotes glycogenolysis and gluconeogenesis in the liver. Under the combined effects of Retatrutide, the body does not experience a simple increase in blood glucose levels but instead regulates energy metabolism to increase fat breakdown, thereby achieving weight loss and improved metabolism. GCGR agonism may also influence hepatic lipid metabolism, reducing hepatic fat accumulation[3].
Effects on Metabolism-Related Physiological Processes
By simultaneously acting on the aforementioned three receptors, Retatrutide influences multiple metabolism-related physiological processes.
Blood glucose regulation:
By activating GIPR and GLP-1R to promote insulin secretion, and appropriately regulating GCGR, Retatrutide can lower blood glucose levels. Its hypoglycemic effect is pronounced when blood glucose is elevated, while it is unlikely to cause hypoglycemia when blood glucose is normal, which is beneficial for blood glucose control in diabetic patients[4].
Weight management:
Retatrutide demonstrates significant efficacy in weight management. By activating GLP-1R, it slows gastric emptying, increases satiety, and reduces food intake; by regulating fat metabolism, it promotes fat breakdown and energy expenditure, thereby achieving weight loss. Clinical trials have shown that obese or overweight patients treated with Retatrutide experience significant weight loss over a certain period of time[5,6].
Lipid regulation:
Retatrutide treatment improves patients' lipid profiles. It reduces triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), and very low-density lipoprotein cholesterol (VLDL-C) levels, while also regulating apolipoproteins, such as lowering apolipoprotein B (apoB) and apolipoprotein C -III (apoC-III) levels, thereby reducing the number of lipoprotein particles associated with atherosclerosis and promoting cardiovascular health[7].
Improved hepatic lipid metabolism:
For patients with non-alcoholic fatty liver disease (NAFLD) associated with metabolic dysfunction, Retatrutide significantly reduces hepatic fat content. In relevant clinical trials, patients treated with different doses of Retatrutide showed a significant relative reduction in liver fat content compared to baseline, indicating that Retatrutide has a positive regulatory effect on liver fat metabolism, which is beneficial for improving liver function[3].
Figure 1 Retatrutide’s mechanisms of action[8].
What are the applications of Retatrutide?
Obesity treatment:
Obesity has become a major global public health issue, closely associated with the onset and progression of various chronic diseases. Retatrutide has demonstrated significant efficacy in obesity treatment. Obese patients treated with Retatrutide experienced a notable reduction in body weight. In a 48-week Phase 2 obesity study, patients treated with 8mg and 12mg of Retatrutide experienced weight reductions of 22.8% and 24.2%, respectively. In another Phase 2 double-blind, randomized, placebo-controlled trial, patients in different dose groups experienced varying degrees of weight loss at 24 weeks and 48 weeks. The 12mg group achieved a weight loss of 24.2% at 48 weeks, while the placebo group only saw a reduction of -2.1%. Retatrutide effectively reduces body weight in obese patients, providing a new and powerful tool for the treatment of obesity. Retatrutide therapy for obesity not only reduces body weight but may also improve other health issues associated with obesity, such as alleviating joint-bearing stress and relieving symptoms of obesity-related joint diseases through weight loss; weight reduction may also help improve obesity-related complications such as sleep apnea[3,6].
Type 2 diabetes treatment:
Type 2 diabetes is a common chronic metabolic disorder characterized by insulin resistance and insufficient insulin secretion. Retatrutide has potential application value in the treatment of type 2 diabetes. It stimulates insulin secretion by activating the GLP-1 receptor, improves insulin resistance, and lowers blood glucose levels. Its weight-reducing effects also help improve the condition of type 2 diabetes patients, as obesity is an important risk factor for type 2 diabetes, and weight loss can enhance insulin sensitivity, further aiding in blood glucose control. In studies involving patients with type 2 diabetes, Retatrutide led to significant weight loss and a notable reduction in hemoglobin A1c (HbA1c) levels, with HbA1c decreasing by 1.64% compared to placebo. This indicates that Retatrutide not only effectively controls blood glucose levels but also improves the overall condition of patients with type 2 diabetes through multiple mechanisms, including weight loss, thereby enhancing their quality of life[6].
Non-alcoholic fatty liver disease (NAFLD) treatment:
NAFLD is a metabolic stress-induced liver injury closely associated with insulin resistance and genetic susceptibility, encompassing a spectrum of conditions including non-alcoholic simple fatty liver, non-alcoholic steatohepatitis, and related cirrhosis. Retatrutide shows promising potential in NAFLD treatment. In a randomized, double-blind, placebo-controlled trial involving participants with metabolic dysfunction-associated fatty liver disease and liver fat content ≥10%, at 24 weeks, the mean relative change in liver fat content from baseline was significantly different across Retatrutide dose groups: -81.4% in the 8mg group, -82.4% in the 12 mg group, and +0.3% in the placebo group. This indicates that Retatrutide can effectively reduce liver fat content, which is of significant importance for improving the liver pathology of NAFLD patients. It holds promise as a new treatment option for NAFLD, potentially slowing disease progression and reducing the risk of severe complications such as cirrhosis[3].
Conclusion
Retatrutide shows promising potential in improving the hepatic pathological status of NAFLD patients, acting through multiple mechanisms including regulating energy metabolism, improving insulin resistance, anti-inflammatory effects, and modulating lipid metabolism.
About The Author
The above-mentioned materials are all researched, edited and compiled by Cocer Peptides.
Scientific Journal Author
Rosenstock, J is an outstanding scholar whose career is closely linked to several prestigious institutions, including the University of Texas Southwestern Medical Center, the University of Texas Dallas, and the Canadian VIGOUR Centre. His research spans numerous fields such as Endocrinology & Metabolism, General & Internal Medicine, Cardiovascular System & Cardiology, Pharmacology & Pharmacy, and Research & Experimental Medicine. His remarkable contributions to the academic community have earned him widespread recognition, as evidenced by his repeated selection as a "Highly Cited Researcher in the field of Clinical Medicine" from 2017 to 2024, highlighting his significant position and profound influence in clinical medical research. Rosenstock J is listed in the reference of citation [4].
