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Retatrutide

investig.

Pronunciation: ret-a-TROO-tide

Retatrutide ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Retatrutide ballicule

What it isTriple GIP, GLP-1 and glucagon receptor agonist; obesity.

Why this oneAdding glucagon agonism raises energy expenditure as well as suppressing appetite, giving the largest weight loss yet reported.

What limits itGI intolerance and heart rate rise. Investigational; long-term safety unknown.

Retatrutide molecular structure (skeletal formula)
Molecular structure: Retatrutide

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Not stated on labelAdults2.5 mg (0.19 mL) SC once weekly, wk 1–410 mg (0.75 mL) SC once weekly from wk 1310 mg once weekly

Titration Increase every 4 weeks: 2.5 mg (wk 1–4) → 5 mg (wk 5–8) → 7.5 mg (wk 9–12) → 10 mg (wk 13+).

Renal Undefined

Hepatic Undefined

Dose given once weekly; label states no interval other than the 4-week titration steps.

Instructions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskGI intolerance and heart rate rise

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Weight-gain liability0 / 4
Direct muscarinic antagonism0 / 4

Defining liabilityDose-related gastrointestinal intolerance; investigational long-term safety

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