Retatrutide is a new triple-receptor agonist peptide originated from the GLP-1-based dual agonist Tirzepatide. It selectively targets three key metabolic receptors: the glucagon receptor (जीसीजीआर), the glucose-dependent insulinotropic polypeptide receptor (GIPR), और ग्लूकागन जैसा पेप्टाइड-1 रिसेप्टर (जीएलपी-1आर). This new peptide drug shows strong potential in treating obesity-related metabolic disorders and type 2 diabetes due to its unique structure.
आगे, Scientists developed Retatrutide peptide on an optimized GLP-1 analog scaffold and it consists of 39 अमीनो अम्ल. Its sequence incorporates three non-natural amino acids to enhance resistance to degradation by dipeptidyl peptidase-4 (DPP-4). इसके अतिरिक्त, the introduction of AIB (2-Aminoisobutyric acid) significantly improves both biological activity and pharmacokinetics.
इसके अतिरिक्त, the attachment of a C20 fatty diacid chain a लाइसिन residue extends its हाफ लाइफ and improves its pharmacological profile. एक साथ, these advanced features support once-weekly subcutaneous dosing.
अनुक्रम
टायर-{एआईबी}-Gln-ग्लाइ-थ्र-पीएचई-थ्र-सेर-एस्प-टायर-सेर-इले-{α-मी-लियो}-ल्यू-एस्प-लिस-{डायएसिड-C20-गामा-ग्लू-(हाँ)-लिस}-पथ-Gln-{एआईबी}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
सीएएस संख्या
2381089-83-2
आण्विक सूत्र
C221H342N46O68
आणविक वजन
4731.33 जी/मोल
Research Of Retatrutide Benefits:
1. Suppresses Appetite, Delays Gastric Emptying, and Stimulates Insulin
1)Mechanism of Action in Appetite Control:
In an animal study, researchers fasted male obese mice के लिए 16 hours and treated them with long-acting glucagon receptor agonists, रेटट्रूटाइड, galectin peptides, and other GLP-1 analogs for weight management. The study evaluated gastric emptying (GE) delay, body weight, and food intake.
2)Glucose-Dependent Gastric Emptying Delay:
विशेष रूप से, Retatrutide delayed GE in a glucose-dependent manner. विशेष रूप से, the group receiving 10 nmol/L Retatrutide showed the highest reduction in body weight and the largest decrease in food consumption.
3)Central Nervous System Effects:
Similarly to other GLP-1 receptor agonist, Retatrutide acts directly on the central nervous system, enhancing satiety and slowing gastric emptying. नतीजतन, it supports effective obesity treatment.
4)Clinical Trial Weight Loss Results:
उदाहरण के लिए, a Phase 2 clinical trial reported significant weight loss in overweight and obese adults: 17.5% पर 24 weeks and 24.4% पर 48 हफ्तों.
2. Treats Type 2 मधुमेह
- A Phase 1b multiple ascending-dose study involved type 2 diabetes patients receiving weekly doses of Retatrutide or other glucose-lowering drugs, with a control group receiving no treatment.
- Remarkably, Retatrutide achieved 100% of the weight loss target, compared to only 2.1% in the control group. इसके विपरीत, no other diabetes drug reached 50% प्रभावकारिता.
- These findings clearly demonstrate Retatrutide’s superior effectiveness in managing type 2 मधुमेह. तथापि, the most common side effects were gastrointestinal.
- एक ही समय पर, in obese adults, Retatrutide treatment also led to significant weight loss over 48 हफ्तों.
3. Promotes Energy Expenditure
- As a triple agonist, Retatrutide activates the glucagon receptor similarly to glucagon. विशेष रूप से, it directly stimulates thermogenesis and fat breakdown.
- It is important to note that glucagon receptors are present in the liver and वसा ऊतक. By activating these receptors, Retatrutide increases energy expenditure and heat production in the liver.
- फलस्वरूप, it boosts metabolic rate and promotes fat oxidation.
4. Reduces Inflammation and Treats Fatty Liver Disease
1)Anti-Inflammatory Benefits:
Retatrutide offers multi-faceted anti-inflammatory benefits. उदाहरण के लिए, studies show it improves glucose tolerance, reduces body weight and fat mass, and enhances lipid profiles.
2)Reversal of Steatohepatitis in Mice:
इसके अतिरिक्त, it reverses steatohepatitis in female mice, supporting resolution of fatty liver disease by reducing hepatic steatosis. In one study, mice that researchers fed a high-fat, high-sugar diet for 38 weeks received subcutaneous Retatrutide, and researchers fasted them for 4 घंटे.
बाद में, histological analysis showed over 80% had definite steatohepatitis. Importantly, Retatrutide improved the condition dose-dependently, with some females showing complete reversal.
3)Histological Analysis Results:
In another human trial, researchers treated 98 participants with ≥10% liver fat content. बाद 48 weeks of Retatrutide treatment, liver fat decreased by 51.3% (1 एमजी), 59% (4 एमजी), और 86% (12 एमजी), की तुलना में 4.6% in the control group.
अंत में, all treated patients achieved normal liver fat levels.
सीओए
एचपीएलसी
एमएस
आलेख/साहित्य उद्धरण नोट्स





