Tissue-repair, gut & immune-signalling peptides
Larazotide Acetate
Also known as AT-1001 · INN-202
An 8-amino-acid tight-junction regulator designed to reduce intestinal permeability, studied mainly in coeliac disease.
In 60 seconds
Reached phase 3 in coeliac disease, which was discontinued; remains a reference tight-junction research compound, including in colitis and arthritis models. Clinical trials reported it as well tolerated; efficacy, not safety, ended the phase 3 programme.
- Reviews tight-junction regulation in coeliac disease with a focus on larazotide.
- In mouse models, restoring gut barrier function (including via a zonulin antagonist) delayed arthritis onset.
- Tested a hydrogel releasing larazotide in a colitis model.
Mechanism
Larazotide is proposed to antagonise zonulin-mediated opening of epithelial tight junctions, limiting paracellular passage of gliadin fragments in the gut.
Research status
Reached phase 3 in coeliac disease, which was discontinued; remains a reference tight-junction research compound, including in colitis and arthritis models.
Key studies
Reviews tight-junction regulation in coeliac disease with a focus on larazotide.
The potential utility of tight junction regulation in celiac disease: focus on larazotide acetate — Ther Adv Gastroenterol, 2016 · PMID 26770266
In mouse models, restoring gut barrier function (including via a zonulin antagonist) delayed arthritis onset.
Targeting zonulin and intestinal epithelial barrier function to prevent onset of arthritis — Nat Commun, 2020 · PMID 32332732
Tested a hydrogel releasing larazotide in a colitis model.
Antibacterial hyaluronic acid hydrogel with sustained release of larazotide as effective colitis treatment — J Control Release, 2025 · PMID 40915363
Reviews intestinal-permeability mechanisms in coeliac disease and strategies, including tight-junction modulators, to restore it.
Coeliac disease and the intestinal barrier: mechanisms of disruption and strategies for restoration — Gut, 2026 · PMID 40579122
Safety signals in the literature
Clinical trials reported it as well tolerated; efficacy, not safety, ended the phase 3 programme.
Legal status (South Africa)
Not registered as a medicine for human use in South Africa (unless stated otherwise); research use only.
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Comparisons
Questions
What is Larazotide Acetate?
An 8-amino-acid tight-junction regulator designed to reduce intestinal permeability, studied mainly in coeliac disease. Larazotide is proposed to antagonise zonulin-mediated opening of epithelial tight junctions, limiting paracellular passage of gliadin fragments in the gut.
What is the research status of Larazotide Acetate?
Reached phase 3 in coeliac disease, which was discontinued; remains a reference tight-junction research compound, including in colitis and arthritis models.
What safety signals are reported for Larazotide Acetate?
Clinical trials reported it as well tolerated; efficacy, not safety, ended the phase 3 programme.
Does Living Water Labs stock Larazotide Acetate?
Not at present. Larazotide Acetate is profiled here for reference, with citations to the published literature. You can ask to be notified if we add it. Not registered as a medicine for human use in South Africa (unless stated otherwise); research use only.
More in Repair & immune
Research reference only. This page summarises published literature; it is not medical advice and contains no guidance on human use. Products supplied by Living Water Labs are for laboratory research only.
