Skip to main content
PepStack

Larazotide

Immune System
AT-1001Larazotide Acetate

Overview

Larazotide, also known as AT-1001 or Larazotide Acetate, is a synthetic peptide derived from the zonulin family of proteins. It is composed of eight amino acids and is designed to modulate tight junctions in the intestinal epithelium. The synthesis of Larazotide involves standard peptide synthesis techniques, including solid-phase peptide synthesis, which allows for precise control over its amino acid sequence. Researchers have primarily focused on its potential therapeutic applications in conditions characterized by increased intestinal permeability, such as celiac disease. Studies have shown that Larazotide can reduce intestinal permeability and inflammation, which are key factors in the pathogenesis of celiac disease. Additionally, it has been investigated for its effects on other autoimmune and inflammatory disorders. The mechanism of action of Larazotide involves the inhibition of zonulin, a protein that regulates the opening and closing of tight junctions between intestinal cells. By blocking zonulin, Larazotide helps maintain the integrity of the intestinal barrier, preventing the passage of harmful substances that can trigger immune responses. Pharmacokinetic studies of Larazotide indicate that it has a relatively short half-life and is rapidly metabolized in the body. Its stability and bioavailability can vary depending on the route of administration, with oral bioavailability being limited due to degradation in the gastrointestinal tract. Currently, Larazotide is in various stages of clinical trials for the treatment of celiac disease. It has not yet received regulatory approval as a medicinal product, but ongoing research continues to explore its potential benefits and safety profile.

Mechanism of Action

Larazotide acts by inhibiting the zonulin pathway, which regulates the opening of tight junctions in the intestinal epithelium. By blocking zonulin, it helps maintain tight junction integrity, reducing intestinal permeability and preventing the translocation of antigens that can trigger immune responses.

Molecular Data

FormulaC32H55N9O10
Molecular Weight725.8 g/mol
CAS Number258818-34-7
PubChem CID9810532

Half-Life

IntranasalNot applicable
OralPoor bioavailability

Larazotide is rapidly metabolized and has limited oral bioavailability due to degradation in the gastrointestinal tract.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

Larazotide is soluble in water and has limited solubility in organic solvents such as DMSO.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Not approved by the FDA as a medicinal product. Not a controlled substance.

🇦🇺AU

Not approved by the TGA as a medicinal product.

🇬🇧UK

Not approved by the MHRA as a medicinal product.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

10 Research Publications

Coeliac disease and the intestinal barrier: mechanisms of disruption and strategies for restoration.

Review

Gut · 2026

Researchers explored how coeliac disease, which affects the small intestine due to gluten consumption in susceptible individuals, leads to increased intestinal permeability. They reviewed various factors contributing to this condition and discussed potential therapies aimed at restoring the intestinal barrier and normalizing permeability.

  • Researchers observed that increased intestinal permeability is a key aspect of coeliac disease.
  • The study identified several mechanisms behind this increased permeability, including immune responses and changes in gut bacteria.
  • Researchers highlighted the importance of developing reliable biomarkers and further research on therapies to improve intestinal barrier function.
PubMed

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

Animal

Journal of controlled release : official journal of the Controlled Release Society · 2025

Researchers studied a new injectable hydrogel designed to mimic natural gut mucus and address issues related to colitis, a gut inflammation condition. They found that this hydrogel not only protected gut cells from harmful bacteria but also improved gut barrier function and balanced gut microbiota in mice with colitis.

  • The hydrogel effectively reduced disease activity and inflammation in mice with colitis.
  • It restored the integrity of gut cell connections and increased mucus production.
  • The hydrogel also demonstrated broad-spectrum antimicrobial activity against harmful gut bacteria.
PubMed

New Therapeutic Challenges in Pediatric Gastroenterology: A Narrative Review.

Review

Healthcare (Basel, Switzerland) · 2025

Researchers observed that pediatric gastroenterology is facing new challenges but also opportunities in treating conditions like celiac disease, eosinophilic esophagitis, inflammatory bowel disease, and autoimmune hepatitis. Advances in precision medicine and emerging therapies, including biologics and microbiota modulation, are being explored to improve care for young patients.

  • Researchers found that new therapies, such as gluten-degrading enzymes and monoclonal antibodies, are being tested for conditions like celiac disease and eosinophilic esophagitis.
  • The study highlighted the potential of personalized medicine, integrating individual patient characteristics with new treatment options for inflammatory bowel disease.
  • Researchers observed that ongoing clinical trials are essential to validate the effectiveness of these emerging therapies in pediatric populations.
PubMed

Zonulin as a Potential Therapeutic Target in Microbiota-Gut-Brain Axis Disorders: Encouraging Results and Emerging Questions.

Review

International journal of molecular sciences · 2023

Researchers observed that disruptions in gut bacteria can lead to increased intestinal permeability, which may affect brain health. They highlighted the role of zonulin, a protein that regulates the intestinal barrier, and discussed potential treatments targeting zonulin pathways. The review also raised questions about the terminology and understanding of zonulin's structure.

  • Researchers found that changes in gut bacteria are linked to brain disorders due to increased intestinal permeability.
  • The study highlighted zonulin's critical role in maintaining the blood-brain barrier function.
  • Researchers discussed potential pharmaceutical approaches to modify zonulin-related pathways, including new drug candidates.
PubMed

Targeting endothelial tight junctions to predict and protect thoracic aortic aneurysm and dissection.

Human

European heart journal · 2023

Researchers studied the role of endothelial tight junctions in the development of thoracic aortic aneurysm and dissection (TAAD). They found that changes in these junctions could serve as early indicators of TAAD and that targeting these junctions may help reduce the incidence of this condition.

  • Researchers observed abnormal expressions of endothelial tight junctions in patients with TAAD.
  • In a mouse model, early disruption of endothelial tight junction function was linked to the development of TAAD.
  • The use of a specific inhibitor improved tight junction function and reduced the occurrence of TAAD in the mouse model.
PubMed

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

Meta-Analysis

Clinics and research in hepatology and gastroenterology · 2022

Researchers studied the effects of larazotide acetate, a gut permeability regulator, on symptoms of celiac disease in patients undergoing gluten challenges. They found that while larazotide acetate did not significantly improve gut permeability, it was associated with better symptom relief compared to a placebo, particularly in patients consuming gluten. The treatment was generally well-tolerated with fewer instances of gluten-related diarrhea.

  • Larazotide acetate showed better symptom improvement in patients undergoing gluten challenges compared to a placebo.
  • No significant differences in gut permeability were observed between the treatment and placebo groups.
  • The treatment was well-tolerated, with a reduction in gluten-related diarrhea compared to placebo.
PubMed

Larazotide acetate: a pharmacological peptide approach to tight junction regulation.

Review

American journal of physiology. Gastrointestinal and liver physiology · 2021

Researchers studied larazotide acetate, a peptide that helps regulate tight junctions in the intestines, particularly for adults with celiac disease. The findings suggest that it may restore intestinal barrier function disrupted by gluten exposure and has potential benefits in other health conditions as well.

  • Larazotide acetate acts as a tight junction regulator, helping to restore intestinal barrier function.
  • It is currently being tested in phase III clinical trials for its effectiveness in patients with celiac disease.
  • Animal studies indicate that larazotide acetate may also be beneficial in other conditions, such as arthritis and intestinal injuries.
PubMed

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

Review

Current medicinal chemistry · 2021

Researchers reviewed the role of zonulin, a protein that affects the permeability of cell junctions, in various inflammatory diseases. They found that Larazotide, a zonulin inhibitor, shows potential as a treatment for conditions like celiac disease and type 1 diabetes by modulating this pathway.

  • Researchers observed a significant involvement of zonulin in multiple chronic and acute inflammatory diseases.
  • The review highlighted the potential efficacy of Larazotide in treating conditions such as celiac disease and inflammatory bowel disease.
  • New molecular targets for Larazotide were identified, suggesting further avenues for research.
PubMed

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

Animal

Nature communications · 2020

Researchers found that a protein called zonulin plays a key role in maintaining the integrity of the intestinal barrier, which is crucial in preventing the progression from autoimmunity to inflammatory arthritis. They observed that restoring this barrier can help prevent the onset of arthritis in animal models.

  • Zonulin is highly expressed in autoimmune conditions and is linked to a leaky gut and inflammation.
  • Restoring the intestinal barrier using certain compounds can inhibit the development of arthritis.
  • A specific zonulin antagonist was effective in reducing the onset of arthritis by improving intestinal barrier function.
PubMed

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

Review

Therapeutic advances in gastroenterology · 2016

Researchers reviewed the potential of larazotide acetate, a synthetic peptide, as a way to regulate gut permeability in individuals with celiac disease (CD). They found that larazotide acetate may help prevent the immune response triggered by gluten, which is a challenge for those on a strict gluten-free diet.

  • Researchers observed that gluten increases gut permeability in celiac disease, leading to various symptoms.
  • The study highlighted larazotide acetate's ability to inhibit changes in gut cell structure caused by gluten.
  • Clinical studies have been conducted to evaluate larazotide acetate as a potential therapy for managing celiac disease.
PubMed

Track Larazotide in PepStack

Log your research cycles, set reminders and visualize serum levels.

This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.