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Larazotide

AT-1001 · Larazotide Acetate

Immune SystemPhase III

MW: 725.8g/mol
Formula: C32H55N9O10

Larazotide acetate is an eight-amino acid peptide classified as a zonulin antagonist, derived from the zonulin family of proteins that regulate intestinal tight junctions. Researchers primarily study larazotide for its potential to restore intestinal barrier function in conditions such as celiac disease and autoimmune disorders. Key findings indicate that larazotide can reduce intestinal permeability associated with gliadin-induced immune responses and enhance tight junction integrity by modulating the activity of myosin light chain kinase. Additionally, studies suggest that larazotide may play a role in preventing the transition from autoimmunity to inflammatory diseases, such as arthritis, by maintaining intestinal barrier integrity. Currently, larazotide is undergoing phase III clinical trials, highlighting its promise as a therapeutic candidate for managing intestinal permeability-related disorders.

Chemical Profile

Chemical Structure

Formula	C32H55N9O10
Molecular Weight	725.8 g/mol
CAS Number	258818-34-7
PubChem CID	9810532

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 acts as a zonulin antagonist, specifically inhibiting the signaling pathways associated with zonulin-induced tight junction disruption, which involves the myosin light chain kinase (MLCK) pathway. By reducing MLCK activity, larazotide promotes the redistribution and rearrangement of tight junction proteins, such as ZO-1 and occludin, thereby restoring intestinal barrier integrity and reducing permeability. The precise molecular interactions and additional signaling pathways involved in its action remain to be fully elucidated.

Research

35 Research Publications

2,067

Total Citations

Human/RCT

5.9

Avg. Influence

2026

Latest

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01Top

#01

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

Tajik Narges, et al. · Nature communications · 2020

AnimalInfluence25.0

416

Researchers observed that treatment with the zonulin antagonist larazotide acetate effectively reduces arthritis onset by restoring intestinal barrier integrity in autoimmune mice.

Key findings

01Zonulin is highly expressed in autoimmune conditions and is linked to a leaky gut and inflammation.
02Restoring the intestinal barrier using certain compounds can inhibit the development of arthritis.
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 weeks250 mg/100 g bmintraperitoneal(rat)2 times with an hour interval1 μMnot specified(porcine)not specified0.1 μMnot specified(porcine)not specified

PubMed

02Top

#02

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

HumanInfluence14.0

243

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.

PubMed

03Top

#03

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

Case ReportInfluence16.0

216

The study demonstrated that treatment with larazotide in a child with multisystem inflammatory syndrome led to a decrease in plasma SARS-CoV-2 antigen levels and inflammatory markers.

PubMed

#04

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

HumanInfluence8.0

194

Researchers observed that larazotide acetate reduced gluten-induced immune reactivity and symptoms in patients with celiac disease during a gluten challenge.

PubMed

#05

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

HumanInfluence12.0

179

Researchers observed that larazotide acetate appeared to limit gluten-induced worsening of gastrointestinal symptom severity in patients with celiac disease, although the effect on intestinal permeability was not statistically significant.

PubMed

#06

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

In VitroInfluence2.0

105

The study demonstrated that larazotide acetate inhibits tight junction disruption caused by gliadin and cytokines, preserving intestinal barrier function in vitro and in vivo.

PubMed

#07

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

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

In VitroInfluence3.0

Researchers observed that larazotide acetate effectively inhibits actin rearrangement caused by gliadin, indicating its potential as a permeability regulator in celiac disease.

Key findings

01Researchers observed that gluten increases gut permeability in celiac disease, leading to various symptoms.
02The study highlighted larazotide acetate's ability to inhibit changes in gut cell structure caused by gluten.
03Clinical studies have been conducted to evaluate larazotide acetate as a potential therapy for managing celiac disease.

PubMed

#08

Evolving Therapy for Celiac Disease.

ReviewInfluence5.0

The review discusses various emerging therapies for celiac disease, including zonulin antagonists like larazotide acetate, which may supplement the gluten-free diet.

PubMed

#09

Larazotide acetate promotes tight junction assembly in epithelial cells.

In VitroInfluence1.0

The study demonstrated that larazotide acetate promotes tight junction assembly and decreases paracellular permeability in epithelial cells.

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

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

01Researchers observed abnormal expressions of endothelial tight junctions in patients with TAAD.
02In a mouse model, early disruption of endothelial tight junction function was linked to the development of TAAD.
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 long-term studies have been published to assess the sustained effects of larazotide acetate on intestinal barrier function and overall health in humans. Additionally, the precise mechanisms by which larazotide acetate inhibits myosin light chain kinase and its broader implications in conditions beyond celiac disease 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

🇩🇪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

Publications per Year

31 total

Pricing

Price Comparison

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

Vendor	Amount	Price	Price/mg	Link
BESTRoyal Peptides WholesaleUS	100mg	$135.00	$1.35/mg	View
Behemoth LabzUS	10mg	—	—	View

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Mechanism

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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