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Larazotide

AT-1001 · Larazotide Acetate

Immune SystemPhase III
From$1.35/mgCompare prices
MW
725.8g/mol
Formula
C32H55N9O10

Larazotide acetate is an 8-mer peptide derived from the zonula occludens toxin, classified as a tight junction modulator. Researchers primarily study it for its potential role in enhancing intestinal barrier integrity and its implications in autoimmune diseases such as celiac disease and inflammatory bowel disease. Key findings indicate that larazotide acetate promotes the assembly of tight junctions in epithelial cells, thereby reducing intestinal permeability and preventing the detrimental effects of gliadin and inflammatory cytokines. Additionally, preclinical evidence suggests that larazotide acetate may inhibit the transition from autoimmunity to inflammatory conditions by restoring intestinal barrier function. Current research continues to explore its therapeutic potential and mechanisms of action in various gastrointestinal disorders.

Chemical Profile

Chemical Profile

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

Half-Life

INIntranasal

Not applicable

POOral

Poor bioavailability

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

Mechanism

Mechanism of Action

Larazotide acetate, an 8-mer peptide, enhances tight junction (TJ) assembly and integrity in intestinal epithelial cells by promoting actin rearrangement and the redistribution of TJ proteins such as zonula occludens-1 (ZO-1) and occludin. It inhibits the disassembly of TJs induced by gliadin fragments and cytokines through modulation of the Rho family GTPase and aPKC signaling pathways, ultimately reducing paracellular permeability. While its precise receptor interactions remain to be fully elucidated, larazotide's ability to counteract the effects of inflammatory stimuli suggests a multifaceted role in maintaining epithelial barrier function.

Research

35 Research Publications

2,111

Total Citations

6

Human/RCT

5.8

Avg. Influence

2026

Latest

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#01

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

Tajik Narges, et al. · Nature communications · 2020

AnimalInfluence28.0
434
The study demonstrated that treatment with the zonulin antagonist larazotide acetate effectively reduces arthritis onset by restoring intestinal barrier integrity in autoimmune mice.

Key findings

  1. 01Zonulin is highly expressed in autoimmune conditions and is linked to a leaky gut and inflammation.
  2. 02Restoring the intestinal barrier using certain compounds can inhibit the development of arthritis.
  3. 03A specific zonulin antagonist was effective in reducing the onset of arthritis by improving intestinal barrier function.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#02

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

HumanInfluence15.0
244
Researchers observed that larazotide acetate at a 0.5 mg dose significantly reduced gastrointestinal symptoms in adults with celiac disease on a gluten-free diet compared to placebo.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#03

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

HumanInfluence14.0
220
Researchers observed that larazotide acetate treatment in a child with multisystem inflammatory syndrome led to decreased plasma SARS-CoV-2 antigen levels and clinical improvement.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#04

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

HumanInfluence8.0
196
The study demonstrated that larazotide acetate reduced gluten-induced immune reactivity and gastrointestinal symptoms in patients with coeliac disease undergoing a gluten challenge, although no significant difference in intestinal permeability was observed.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#05

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

HumanInfluence10.0
181
Researchers observed that larazotide acetate limited gluten-induced gastrointestinal symptom severity in patients with coeliac disease during a gluten challenge, despite variability in intestinal permeability measurements.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#06

Larazotide acetate regulates epithelial tight junctions in vitro and in vivo.

AnimalInfluence2.0
106
Researchers observed that larazotide acetate inhibits gliadin-induced tight junction disruption and preserves junction structure in Caco-2 and IEC6 cells.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#07

Evolving Therapy for Celiac Disease.

ReviewInfluence5.0
80
The review emphasizes the exploration of alternative therapies for celiac disease, including zonulin antagonists like larazotide acetate to prevent gluten uptake.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#08

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

Khaleghi Shahryar, et al. · Therapeutic advances in gastroenterology · 2016

ReviewInfluence3.0
80
The study demonstrated that larazotide acetate functions as a permeability regulator, potentially improving treatment outcomes for patients with celiac disease.

Key findings

  1. 01Researchers observed that gluten increases gut permeability in celiac disease, leading to various symptoms.
  2. 02The study highlighted larazotide acetate's ability to inhibit changes in gut cell structure caused by gluten.
  3. 03Clinical studies have been conducted to evaluate larazotide acetate as a potential therapy for managing celiac disease.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#09

Larazotide acetate promotes tight junction assembly in epithelial cells.

AnimalInfluence1.0
71
The study demonstrated that larazotide acetate enhances tight junction assembly and decreases paracellular permeability in Caco-2 cells by promoting actin rearrangement.
0.25, 1, 4, or 8 mgoral(human)14 days0.5, 1, or 2 mg 3 times dailyoral(human)12 weeks1 μMunknown(pig)240 minutes
PubMed
#10

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

Yang Xueyuan, et al. · European heart journal · 2023

HumanInfluence4.0
70
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.

Key findings

  1. 01Researchers observed abnormal expressions of endothelial tight junctions in patients with TAAD.
  2. 02In a mouse model, early disruption of endothelial tight junction function was linked to the development of TAAD.
  3. 03The use of a specific inhibitor improved tight junction function and reduced the occurrence of TAAD in the mouse model.
PubMed
Safety

Safety & Handling

Research Gaps

No randomized controlled human trials assessing the long-term safety and efficacy of larazotide acetate in diverse populations have been published. Additionally, the precise molecular mechanisms by which larazotide acetate regulates tight junction assembly and its interactions with other signaling pathways remain unclear.

Solubility

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

Storage & Handling

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

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

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.

Community Insights

Community Insights

Publications per Year

31 total
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Pricing

Price Comparison

  • BESTRoyal Peptides WholesaleUS
    100mg
    $135.00
    Price/mg
    $1.35/mg
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  • Behemoth LabzUS
    10mg
    —
    Price/mg
    —
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Mechanism

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer