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
review · 2026
Upcoming Treatments in Celiac Disease: From Luminal Enzymes to Oral Immune Tolerance
Celiac disease (CeD) is a chronic autoimmune enteropathy triggered by dietary gluten in genetically predisposed individuals. Currently, a gluten-free diet (GFD) is the only available treatment, being effective in improving mucosal health and symptoms.
Research use only — not for human consumption and not approved by the FDA. Nothing here is medical advice.