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How triple agonists work

Last reviewed: September 2026
Next generationInvestigational

Triple agonists add a glucagon signal on top of GLP-1 and GIP. That tackles obesity from three angles. The glucagon part is what sets them apart: it raises energy expenditure, so the body burns more calories at rest, on top of reduced appetite.

How each generation adds a new signal

GLP-1 drugs~15%
GLP-1
—
—
Dual agonists~20%
GLP-1
GIP
—
Triple agonists~28%*
GLP-1
GIP
Glucagon
*Phase 3 trial data — retatrutide not yet approved. Results may change.

What glucagon receptor activation adds

Glucagon is usually associated with raising blood sugar. It is the hormone that tells the liver to release glucose when blood sugar drops. But glucagon receptors sit in many other tissues, and switching those on has effects beyond blood sugar:

Increases energy expenditure

The glucagon signal raises the calories the body burns at rest. That is a thermogenic effect, and it is not seen with GLP-1 or dual agonists.

Reduces appetite

Glucagon also suppresses appetite, through receptors in the brain and spinal cord. That adds to the GLP-1 and GIP effects.

Breaks down fat

Stimulates fat breakdown (lipolysis) in the liver and in fat tissue. That speeds up fat loss beyond eating less alone.

Reduces liver fat

Blocks the liver from making new fat, and pushes it to burn fat instead. That matters for fatty liver disease.

How the three signals combine

Plain English:

Triple agonists work on three appetite and metabolism signals at once. On top of the appetite suppression of GLP-1/GIP drugs, the added glucagon signal tells the body to burn more energy and break down fat more efficiently. This may explain why early trial results show even greater weight loss than dual agonists.

GLP-1

Appetite reduction + gut slowing + insulin secretion

GIP

Boosts the appetite effect + fat metabolism + tolerability

Glucagon

Increased energy expenditure + fat breakdown + liver fat reduction

Investigational — not yet approved

Retatrutide (the leading triple agonist) is in Phase 3 trials. In one Phase 3 trial in people with obesity and knee osteoarthritis, participants lost an average of 28.7% of body weight at 68 weeks. That was approximately 71 lbs on average. FDA approval is estimated 2027, subject to full trial results and regulatory review. These results are from a single Phase 3 trial and are subject to change. Source

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