MetabolicPhase III

Retatrutide

LY3437943

A first-in-class triple agonist of GIP, GLP-1, and glucagon receptors showing unprecedented weight loss in clinical trials. Currently in Phase 3 development by Eli Lilly.

What is Retatrutide?

Retatrutide is a triple agonist of GIP, GLP-1, and glucagon receptors—making it the first "triple G" agonist in development. Developed by Eli Lilly, retatrutide has shown unprecedented weight loss results in Phase 2 trials, exceeding even tirzepatide.

By activating three metabolic hormone receptors simultaneously, retatrutide represents the next evolution beyond dual agonists like tirzepatide.


Mechanism of Action

Triple Receptor Activation

GLP-1 Receptor:

  • Appetite reduction
  • Glucose-dependent insulin secretion
  • Delayed gastric emptying

GIP Receptor:

  • Enhanced insulin secretion
  • Metabolic effects
  • May improve tolerability

Glucagon Receptor:

  • Increased energy expenditure
  • Hepatic glucose regulation
  • Additional weight loss mechanism

Clinical Trial Results

Phase 2 (Published 2023)

Record-breaking weight loss:

DoseWeight Loss at 48 weeks
1 mg~8%
4 mg~17%
8 mg~22%
12 mg~24.2%

This exceeds results from:

  • Semaglutide (~15-17%)
  • Tirzepatide (~22%)

Development Status

  • Phase 3 trials ongoing
  • Studying obesity and diabetes
  • Potential approval: 2026-2027
  • Eli Lilly development

Side Effects (Phase 2)

Common:

  • Nausea
  • Diarrhea
  • Vomiting
  • Constipation

Similar to other incretin agonists, with dose-dependent GI effects.


Comparison

AgonistReceptorsWeight Loss
SemaglutideGLP-1~15-17%
TirzepatideGIP + GLP-1~22%
RetatrutideGIP + GLP-1 + Glucagon~24%

Summary

Retatrutide represents the cutting edge of metabolic peptide therapy, with triple agonism producing the highest weight loss results seen in clinical trials.

Key Points:

  • Classification: Triple agonist (GIP/GLP-1/Glucagon)
  • Developer: Eli Lilly
  • Status: Phase 3 trials
  • Weight Loss: Up to 24% in Phase 2

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