Retatrutide

रेटट्रूटाइड

रेटट्रूटाइड

रेटट्रूटाइड एक क्रांतिकारी पेप्टाइड है जो तीन प्रमुख चयापचय रिसेप्टर्स को लक्षित करता है.

 

अपना प्यार बांटें

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

(1) Katsi, वी; Koutsopoulos, जी।; Fragoulis, सी।; Dimitriadis, के.; Tsioufis, के. Retatrutide—A Game Changer in Obesity Pharmacotherapy. जैविक अणुओं 2025, 15 (6). डीओआई: 10.3390/biom15060796.

(2) Naeem, एच।; Akram, एस।; Tarar, आर. एक।; Javed, एम. एक।; Shahid, एम. बी।; Shehryar, एम।; Rehman, जेड. यू; Siddiqui, एम. एक।; Ayub, एस।; Irfan, एक।; और अन्य. रेटट्रूटाइड, a Trigonal Glp-1, Gip and Glucagon Receptor Agonist, and Its Role in Weight Reduction. अमेरिकन कॉलेज ऑफ कार्डियोलॉजी का जर्नल 2024, 83 (13). डीओआई: 10.1016/s0735-1097(24)03892-0.

(3) ली, डब्ल्यू; झोउ, क्यू।; कांग्रेस, जेड; युआन, क्यू।; ली, डब्ल्यू; झाओ, एफ।; जू, एच. ई.; झाओ, एल.-एच.; कौन, डी।; वैंग, एम.-डब्ल्यू. जीएलपी-1आर पर ट्रिपल एगोनिज्म में संरचनात्मक अंतर्दृष्टि, जीआईपीआर और जीसीजीआर रेटट्रूटाइड द्वारा प्रकट होते हैं. सेल डिस्कवरी 2024, 10 (1). डीओआई: 10.1038/s41421-024-00700-0.

(4) Sanyal, ए. जे।; Kaplan, एल. एम।; Frias, जे. पी।; Brouwers, बी।; वू, क्यू।; Thomas, एम. के.; Harris, सी।; Schloot, एन. सी।; Du, वाई; Mather, के. जे।; और अन्य. Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial. प्राकृतिक चिकित्सा 2024, 30 (7), 2037-2048. डीओआई: 10.1038/s41591-024-03018-2.

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