Larazotide
Also known as: Larazotide acetate, AT-1001, INN-202, GGVLVQPG
Synthetic eight-amino-acid peptide that acts as a zonulin antagonist and tight-junction regulator, helping restore and maintain intestinal epithelial barrier function (reducing paracellular 'leaky gut' permeability). It was developed (as larazotide acetate, AT-1001 / INN-202) primarily for celiac disease as an adjunct to a gluten-free diet. It is not FDA-approved: a Phase 3 trial (CeDLara) in celiac disease was discontinued for futility, and the compound remains investigational with no approved human indication. The acetate salt form carries CAS 881851-50-9.
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About Larazotide
CAS
258818-34-7
Molecular formula
C32H55N9O10
Sequence
GGVLVQPG
Typical dose range
0.25-0.5 mg taken orally three times daily before meals (clinical-trial dosing); acts locally in the gut lumen with minimal systemic absorption
Half-life
Minimal systemic exposure; acts locally in the gastrointestinal tract rather than via sustained plasma levels
Common research uses
Safety notes
Not FDA-approved for any indication; clinical development for celiac disease did not demonstrate efficacy in Phase 3. Reported trial adverse effects were generally mild and gastrointestinal. Not a WADA-prohibited substance.
Reconstitution
Studied as an oral formulation (capsule), not a reconstituted injectable.
COAs for Larazotide
2 third-party tests. Each card links to the full report.
20 citations indexed for Larazotide
review · 2026
Coeliac disease and the intestinal barrier: mechanisms of disruption and strategies for restoration
Coeliac disease is characterised by immune-mediated damage to the small intestine in response to dietary gluten in genetically predisposed individuals. Increased intestinal permeability is a central component to its pathophysiology.
animal · 2026
Potassium-Competitive Acid Blocker Increases Ileal Permeability and Exacerbates Ileal Inflammation under Stress Conditions in a Mouse Model of Eosinophilic Enteritis
Introduction Potassium-competitive acid blockers (P-CABs) have been empirically administered to treat non-esophageal eosinophilic gastrointestinal diseases, although their efficacy remains unproven.
review · 2026
Beyond gluten-free diet: Novel therapeutic frontiers in celiac disease armamentarium
Celiac disease is a chronic, immune-mediated enteropathy triggered by dietary gluten ingestion in a genetically susceptible individual.
review · 2026
Integrated Role of Microbial, Fungal, and Plant-Derived Interventions in the Management of Celiac Disease: A Narrative Review
Celiac disease (CeD) is a chronic autoimmune enteropathy triggered by gluten ingestion in genetically susceptible individuals carrying human leukocyte antigen (HLA)-DQ2 or HLA-DQ8 haplotypes.
animal · 2026
Preventive effects of Larazotide acetate (AT-1001) on non-alcoholic fatty liver diseases (NAFLD) in a mouse model
rct · 2025
Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide
Multisystem inflammatory syndrome (MIS) is a severe disease that occurs weeks to months after acute infection with SARS-CoV-2, often occurring in children (MISC). Symptoms include high fever, rash, nausea, diarrhea, and abdominal pain.
Research use only. Not for human consumption and not approved by the FDA. Nothing here is medical advice.