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Study breakdown

Incretin Co-Agonists Are Transforming Cardiometabolic Treatment — A Review of Efficacy and Safety

evidence
The takeaway

Newer incretin-based peptide therapies — from dual GIP/GLP-1 agonists like tirzepatide to triple agonists like retatrutide — are achieving unprecedented weight loss and cardiometabolic improvements, reshaping treatment for diabetes and obesity.

~15%

Weight reduction achieved by orforglipron, an oral GLP-1 receptor agonist in development

What the researchers found

The review maps the incretin co-agonist landscape across multiple drug classes. GLP-1 receptor agonists improve glycated hemoglobin, weight, lipid profiles, and liver fat, with many reducing major adverse cardiovascular events (MACE). The oral GLP-1RA orforglipron achieves approximately 15% weight reduction.

Tirzepatide, the first approved dual GIP/GLP-1 agonist, offers comparable efficacy with notably fewer gastrointestinal side effects than GLP-1 monoagonists. Triple agonists targeting GLP-1, GIP, and glucagon receptors (retatrutide, efocipegtrutide) have demonstrated the highest pharmacotherapy-achievable weight loss to date. Emerging combinations include GLP-1/amylin agonists (CagriSema, amycretin) and peptide YY/GLP-1 dual agonists.

Why it matters

Obesity and type 2 diabetes are global epidemics driving cardiovascular disease. Incretin co-agonists represent the most significant pharmacological advance in metabolic medicine in decades, with each new generation of multi-receptor agonists achieving greater weight loss and broader cardiometabolic benefits. Understanding this rapidly evolving drug landscape is essential for clinicians and researchers.

How the study worked

This is an evidence review synthesizing data from clinical trials and published studies on incretin-based therapies. The authors compiled efficacy and safety data across GLP-1 receptor agonists, dual agonists, triple agonists, and emerging combination peptide drugs to provide a comprehensive overview of the cardiometabolic benefits.

What this study cannot tell us

As a review article, this paper synthesizes existing trial data rather than presenting original research. The abstract does not detail specific trial sizes, follow-up periods, or comparative effect sizes across drug classes. Many of the newer agents (retatrutide, efocipegtrutide, amycretin) are still in clinical trials, so long-term safety and real-world effectiveness data are limited.

How to read the evidence

This is a narrative evidence review synthesizing data from multiple clinical trials. While it provides a broad overview, it does not follow systematic review methodology, and many of the newer agents discussed are still in clinical trials.

When this study was published

Published in 2025, this review captures the current state of a rapidly evolving field, including drugs in late-stage clinical trials.

The bigger picture

This review captures a pivotal moment in metabolic medicine. The progression from single GLP-1 receptor agonists to dual and triple agonists mirrors a broader trend of designing peptide drugs that simultaneously engage multiple hormone pathways. The cardiometabolic benefits extend well beyond glucose control — these drugs are reducing heart attacks, strokes, and mortality, fundamentally changing how obesity and diabetes are treated.

Questions still open

  • Will triple agonists like retatrutide maintain their weight loss advantage over dual agonists in long-term real-world use?
  • How will the cardiovascular benefits of these newer co-agonists compare head-to-head with established GLP-1RAs like semaglutide?
  • Can oral formulations of incretin co-agonists achieve efficacy comparable to injectable versions?

Common questions

What is the difference between a GLP-1 agonist and an incretin co-agonist?
A GLP-1 agonist targets a single hormone receptor (GLP-1) to improve blood sugar and reduce appetite. An incretin co-agonist targets two or more receptors at once — for example, tirzepatide hits both GIP and GLP-1 receptors, while retatrutide targets three (GLP-1, GIP, and glucagon). Hitting multiple pathways simultaneously tends to produce greater weight loss and broader metabolic improvements.
Why is tirzepatide considered an advance over older GLP-1 drugs?
Tirzepatide was the first approved dual GIP/GLP-1 receptor agonist and achieves comparable or greater metabolic benefits with notably fewer gastrointestinal side effects (like nausea) compared to GLP-1 monoagonists. This improved tolerability, combined with strong efficacy for both diabetes and obesity, makes it a significant step forward.

Read the original research

Efficacy and safety of incretin co-agonists: Transformative advances in cardiometabolic healthcare.

World journal of cardiology, 17(8), 107991

Citation

Bhat, Sowrabha; Fernandez, Cornelius J; Lakshmi, Vijaya; Pappachan, Joseph M. (2025). Efficacy and safety of incretin co-agonists: Transformative advances in cardiometabolic healthcare.. World journal of cardiology, 17(8), 107991. https://doi.org/10.4330/wjc.v17.i8.107991