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Larazotide

AT-1001 · Larazotide Acetate

Immune SystemPhase III

MW: 725.8g/mol
Formula: C32H55N9O10

Larazotide, also known as larazotide acetate or AT-1001, 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 role in restoring intestinal barrier function, particularly in conditions such as celiac disease and autoimmune disorders. Key findings from recent studies indicate that larazotide effectively reduces intestinal permeability associated with zonulin, thereby improving barrier integrity and potentially mitigating the onset of inflammatory diseases like arthritis and colitis. Furthermore, preclinical evidence suggests larazotide may have broader applications in various inflammatory conditions beyond celiac disease. Currently, larazotide is undergoing phase III clinical trials to evaluate its efficacy and safety in human subjects.

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, primarily targeting the regulation of tight junctions in intestinal epithelial cells. It inhibits the myosin light chain kinase (MLCK) pathway, reducing tension on actin filaments and promoting tight junction closure, thereby restoring intestinal barrier integrity. While its precise interactions and all downstream effects are not fully elucidated, it is associated with the modulation of epithelial permeability and the prevention of inflammatory responses linked to dysbiosis.

Research

35 Research Publications

2,042

Total Citations

Human/RCT

6.0

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

AnimalInfluence24.0

411

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.

250 mg/100 g bmintraperitoneal(rat)not mentioned1 μMnot mentioned(not mentioned)not mentioned1 mgoral(not mentioned)not mentioned0.32-1.76 μMnot mentioned(not mentioned)not mentioned0.02-0.47 μMnot mentioned(not mentioned)not mentioned1 μMnot mentioned(not mentioned)not mentioned0.1 μMnot mentioned(not mentioned)not mentioned0.25, 1, 4, or 8 mgnot mentioned(human)14 days

PubMed

02Top

#02

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

HumanInfluence15.0

241

The study demonstrated that larazotide acetate at a 0.5 mg dose significantly reduced gastrointestinal symptoms in celiac disease patients 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 ReportInfluence14.0

213

Researchers observed that treatment with larazotide acetate in a child with multisystem inflammatory syndrome resulted in decreased plasma SARS-CoV-2 antigen levels and improved clinical symptoms.

PubMed

#04

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

HumanInfluence8.0

194

The study demonstrated that larazotide acetate reduced gluten-induced immune reactivity and gastrointestinal 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

178

Researchers observed that larazotide acetate limited gluten-induced worsening of gastrointestinal symptoms in celiac disease patients, although its 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 changes in tight junction structure and function in intestinal epithelial cells caused by gliadin fragments and cytokines.

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

ReviewInfluence3.0

The review emphasized larazotide acetate's role as a permeability regulator in celiac disease, inhibiting actin rearrangement caused by gliadin.

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 discussed various emerging therapies for celiac disease, emphasizing the role of zonulin antagonists like larazotide in managing gluten-induced intestinal permeability.

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 effects of larazotide acetate treatment have been thoroughly investigated in human populations, raising concerns about its safety and efficacy over extended periods. Additionally, while the mechanism of action involving myosin light chain kinase inhibition has been suggested, detailed molecular pathways and interactions in various inflammatory diseases remain unclear and require further elucidation.

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

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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