THE SCIENCE
Retatrutide is an investigational peptide that activates three hormone receptors: glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1), and glucagon receptors. The sections below provide scientific background on its molecular characteristics, receptor activity, metabolic signaling, and clinical research.
MOLECULAR DESIGN
Retatrutide (LY3437943) is a single peptide designed to activate the GIP, GLP-1, and glucagon receptors. Its triple-receptor activity is the defining feature of its molecular pharmacology and distinguishes it from single- and dual-receptor agonists.
TRIPLE RECEPTOR ACTIVITY
Retatrutide activates three hormone receptors: glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1), and glucagon receptors. Research has examined how combined activation of these pathways may influence energy intake, metabolism, and body-weight regulation.
METABOLIC SIGNALING
Activation of the GIP, GLP-1, and glucagon receptors influences signaling pathways involved in glucose regulation, appetite, energy balance, and metabolism. Clinical research on retatrutide has examined changes in body weight and a range of metabolic measures.
BODY WEIGHT & METABOLIC EFFECTS
- Retatrutide has been studied primarily for its effects on body weight and metabolic measures. In clinical research, treatment was associated with changes in body weight, waist circumference, glycemic measures, blood pressure, and lipid measures.
BODY WEIGHT & CLINICAL RESEARCH
Clinical research on retatrutide has evaluated changes in body weight and related metabolic measures over time. The magnitude of weight reduction in the Phase 2 study varied according to dose and was measured over a 48-week treatment period.
PHASE 2 RESEARCH
A Phase 2 randomized, double-blind, placebo-controlled study evaluated retatrutide in 338 adults with obesity or overweight plus a weight-related condition. At 48 weeks, the 12 mg group had a least-squares mean reduction in body weight of 24.2% from baseline, compared with 2.1% in the placebo group. Retatrutide remains an investigational treatment.