Overview
Larazotide is classified as a zonulin antagonist peptide. Gut barrier repair, tight junction integrity, celiac disease symptom reduction, leaky gut.
Synthetic octapeptide that acts as a zonulin antagonist. Zonulin is the body's primary regulator of intestinal tight junction permeability; elevated zonulin (triggered by gliadin/gluten and dysbiosis) opens tight junctions and causes intestinal permeability ('leaky gut'). Larazotide competitively blocks zonulin receptor binding, preventing tight junction opening and reducing gut permeability without systemic absorption.
Also known as: Larazotide acetate, AT-1001, INN-202
Category
Zonulin Antagonist
Half-Life
1.5h
Route
Oral
FDA Status
Not Approved
How Does Larazotide Work?
Synthetic octapeptide that acts as a zonulin antagonist. Zonulin is the body's primary regulator of intestinal tight junction permeability; elevated zonulin (triggered by gliadin/gluten and dysbiosis) opens tight junctions and causes intestinal permeability ('leaky gut'). Larazotide competitively blocks zonulin receptor binding, preventing tight junction opening and reducing gut permeability without systemic absorption.
At the molecular level, Larazotide operates through pathways characteristic of the Zonulin Antagonist class, interacting with target receptors and downstream signaling cascades to produce its observed effects.
Published Research
The following studies are indexed from PubMed and peer-reviewed journals:
[1]Larazotide acetate in persistent symptoms of celiac disease: Phase 2b trial
Leffler et al. (JAMA Internal Medicine): Phase 2b RCT — larazotide 0.5mg TID significantly reduced overall celiac disease symptom severity vs placebo in patients on a gluten-free diet, with an excellent safety profile.
Evidence: strong[2]Larazotide acetate regulates epithelial tight junctions via a zonulin-independent mechanism
Paterson et al.: Larazotide stabilizes tight junctions and reduces epithelial permeability induced by gliadin, demonstrating its molecular mechanism of action in intestinal barrier protection.
Evidence: preclinicalSafety Profile
Has completed Phase 2b and Phase 3 human trials with excellent safety profile. Minimal systemic absorption (acts locally in gut lumen). Not FDA-approved. Investigational. Phase 3 results have been mixed; FDA application pending review.
| Side Effect | Incidence | Severity |
|---|---|---|
| Headache | ~8% | mild |
| Diarrhea | ~6% | mild |
Sourcing Larazotide for Research
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Full Research Profile
Larazotide — dosing, interactions, timelines & more
Comprehensive compound profile with sourcing information, stacking synergies, and outcome timelines.