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Larazotide

A synthetic peptide that regulates intestinal tight junctions, in clinical trials for celiac disease and studied for leaky gut conditions.

ModerateWell-Studied Beginner-Friendly

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This information is for educational purposes. Peptide therapy should be guided by a licensed healthcare provider. Connect with a Noho clinician

What is Larazotide?

Larazotide acetate is a synthetic peptide derived from Vibrio cholerae zonula occludens toxin (ZOT). Unlike ZOT which opens tight junctions, larazotide acts as a tight junction regulator that prevents pathological opening of intestinal tight junctions. It has undergone multiple Phase 2 and Phase 3 clinical trials for celiac disease and is also being studied for MIS-C (multisystem inflammatory syndrome in children) and other barrier-dysfunction conditions.

Why People Talk About It

Celiac disease symptom management

Moderate

Intestinal permeability reduction

Moderate

Leaky gut support

Emerging

Gluten exposure protection

Moderate

How It Works

Larazotide acts like a gatekeeper for the spaces between cells in your gut lining. It helps keep these gates properly closed, preventing unwanted substances from leaking through the intestinal barrier into your bloodstream.

Common Questions

Safety Information

Important Safety Notes

Common Side Effects

HeadacheUpper respiratory tract infectionNauseaGenerally well-tolerated

Cautions

  • Not yet FDA-approved
  • Not a replacement for gluten-free diet
  • Clinical trial data is promising but approval pending

What We Don't Know

Long-term effects of chronic tight junction modulation are being studied. Post-marketing safety data is not yet available.

Published Research

34 studies

Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide

Randomized Controlled TrialPMID: 40737433

A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge

Randomized Controlled TrialPMID: 22825365

The safety, tolerance, pharmacokinetic and pharmacodynamic effects of single doses of AT-1001 in coeliac disease subjects: a proof of concept study

Randomized Controlled TrialPMID: 17697209

Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study

Randomized Controlled TrialPMID: 23163616

Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial

Randomized Controlled TrialPMID: 25683116

The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases

ReviewPMID: 33397225

The potential utility of tight junction regulation in celiac disease: focus on larazotide acetate

ReviewPMID: 26770266

Larazotide acetate: a pharmacological peptide approach to tight junction regulation

ReviewPMID: 33881350

The PAR2 Antagonist Larazotide Can Mitigate Acute Histamine-Stimulated Epithelial Barrier Disruption in Keratinocytes: A Potential Adjunct Treatment for Atopic Dermatitis

PreclinicalPMID: 40330848

Antibacterial hyaluronic acid hydrogel with sustained release of larazotide as effective colitis treatment

PreclinicalPMID: 40915363

Larazotide Acetate Protects the Intestinal Mucosal Barrier from Anoxia/Reoxygenation Injury via Various Cellular Mechanisms

PreclinicalPMID: 41153766

Ameliorative Effects of Larazotide Acetate on Intestinal Permeability and Bacterial Translocation in Acute Pancreatitis Model in Rats

PreclinicalPMID: 38441784

Zonulin Antagonist, Larazotide (AT1001), As an Adjuvant Treatment for Multisystem Inflammatory Syndrome in Children: A Case Series

PreclinicalPMID: 35211683

Tight junction regulation in celiac disease: role of larazotide acetate

PreclinicalPMID: 33793152

Peptide Derivatives of the Zonulin Inhibitor Larazotide (AT1001) as Potential Anti SARS-CoV-2: Molecular Modelling, Synthesis and Bioactivity Evaluation

PreclinicalPMID: 34502335

Larazotide acetate induces recovery of ischemia-injured porcine jejunum via repair of tight junctions

PreclinicalPMID: 33886649

In vivo assessment of a delayed release formulation of larazotide acetate indicated for celiac disease using a porcine model

PreclinicalPMID: 33844694

Effects of larazotide acetate, a tight junction regulator, on the liver and intestinal damage in acute liver failure in rats

PreclinicalPMID: 34791921

In silico Analysis Revealed Potential Anti-SARS-CoV-2 Main Protease Activity by the Zonulin Inhibitor Larazotide Acetate

PreclinicalPMID: 33520943

The α3β4 nAChR partial agonist AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats

PreclinicalPMID: 28693859

[Larazotide as an option in case of failure of a gluten-free diet]

PreclinicalPMID: 26983338

AT-1001 Is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors

PreclinicalPMID: 26162864

Functional characterization of AT-1001, an α3β4 nicotinic acetylcholine receptor ligand, at human α3β4 and α4β2 nAChR

PreclinicalPMID: 25180076

High affinity α3β4 nicotinic acetylcholine receptor ligands AT-1001 and AT-1012 attenuate cocaine-induced conditioned place preference and behavioral sensitization in mice

PreclinicalPMID: 26256075

AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology

PreclinicalPMID: 25440006

Pharmacological stress is required for the anti-alcohol effect of the α3β4* nAChR partial agonist AT-1001

PreclinicalPMID: 25689019

Commentary: larazotide acetate - an exciting new development for coeliac patients?

PreclinicalPMID: 23336683

Commentary: larazotide acetate - an exciting new development for coeliac patients? Authors' reply

PreclinicalPMID: 23336684

Larazotide acetate promotes tight junction assembly in epithelial cells

PreclinicalPMID: 22401910

Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials

Systematic Review, Meta-AnalysisPMID: 34339872

Larazotide acetate regulates epithelial tight junctions in vitro and in vivo

PreclinicalPMID: 22401908

Reducing small intestinal permeability attenuates colitis in the IL10 gene-deficient mouse.

PreclinicalPMID: 18829978

Targeting zonulin and intestinal epithelial barrier function to prevent onset of arthritis.

PreclinicalPMID: 32332732

Multisystem inflammatory syndrome in children is driven by zonulin-dependent loss of gut mucosal barrier.

Observational StudyPMID: 34032635

Always consult a qualified clinician

This information is for educational purposes. Peptide therapy should be guided by a licensed healthcare provider. Connect with a Noho clinician

Related Peptides

Quick Facts

Class
Tight Junction Regulator
Evidence
Moderate
Safety
Well-Studied
Updated
Mar 2026
Citations
34PubMed

Also known as

AT-1001Larazotide Acetate

Tags

Gut HealthTight JunctionsCeliac DiseaseIntestinal Barrier

Related Goals

Evidence Score

Overall Confidence75%

Clinical Trials

View Clinical Trials

Links to ClinicalTrials.gov for reference. Listing does not imply endorsement.

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