Larazotide

Human clinical Healing & Recovery 2 sources

Larazotide (also known as AT-1001) is an investigational eight-amino acid peptide designed to regulate tight junctions in the intestinal lining. Research has primarily focused on its potential to treat celiac disease by preventing the paracellular leakage of gluten peptides, thereby reducing the inflammatory immune response.

01Dosing reference

Amount

0.5 mg to 2 mg

Frequency

Three times daily (before meals)

Cycle

Continuous use during gluten exposure

Reference figures, not a recommendationThese values reflect amounts described in the literature and vendor documentation this database indexes. Use the reconstitution calculator to convert them into syringe units.

02Mechanism of action

Zonulin Receptor Antagonism

Larazotide acts as a zonulin antagonist, binding to receptors on the intestinal epithelium.

Tight Junction Regulation

It prevents the disassembly and opening of tight junctions, maintaining the integrity of the intestinal mucosal barrier.

Reduced Antigen Exposure

By keeping tight junctions closed, it prevents gluten fragments and other antigens from crossing the intestinal barrier and triggering an immune response.

03Human evidence

Reduced gluten-induced symptoms in celiac patients during Phase 2 trials.

Phase 2b clinical trials showed that larazotide acetate reduced gastrointestinal symptoms in patients with celiac disease undergoing a gluten challenge.

Phase 3 trial discontinuation due to lack of efficacy.

A Phase 3 trial for celiac disease was discontinued in 2022 after an interim analysis indicated it was unlikely to meet its primary endpoint of symptom reduction compared to placebo.

04Preclinical evidence

Prevention of increased intestinal permeability.

Animal models of gluten sensitivity demonstrated that larazotide prevented the increase in intestinal permeability induced by gliadin exposure.

Reduction of inflammatory cytokines.

In vitro studies on intestinal epithelial cells showed decreased production of pro-inflammatory cytokines when treated with larazotide prior to gluten exposure.

05What is known vs. unknown

Reasonably established

Larazotide is an eight-amino acid peptide (GGVLVQPG).
It functions as a tight junction regulator and zonulin antagonist.
It is administered orally and designed to act locally in the gastrointestinal tract without systemic absorption.
It has been extensively studied in human clinical trials for celiac disease.

Unknowns & limits

The exact reasons for its failure to meet primary endpoints in Phase 3 trials remain a subject of investigation.
Its efficacy in other conditions involving intestinal permeability, such as inflammatory bowel disease, is not fully established.

06Safety & regulatory context

Regulatory statusLarazotide has generally been well-tolerated in clinical trials with a safety profile similar to placebo, largely because it acts locally in the gut and is not systemically absorbed. It is not FDA-approved and remains an investigational compound. The Phase 3 clinical trial for celiac disease was halted in 2022.

07Compared with BPC-157

Larazotide vs. BPC-157

Key difference

Larazotide specifically targets tight junctions via zonulin antagonism to prevent intestinal permeability, whereas BPC-157 promotes systemic tissue healing and angiogenesis.

When researchers discuss each

Larazotide is discussed in the context of celiac disease and specific tight junction dysfunction, while BPC-157 is discussed for general gastrointestinal healing, ulcer repair, and systemic tissue recovery.

08Glossary

Tight Junctions

Protein complexes that seal the space between adjacent cells in the intestinal lining, controlling permeability.

Zonulin

A protein that modulates the permeability of tight junctions between cells of the wall of the digestive tract.

Celiac Disease

An autoimmune disorder where ingestion of gluten leads to damage in the small intestine.

09Knowledge check

Q1What is the primary mechanism of action of larazotide?

Q2How is larazotide typically administered in clinical studies?

Q3Which statement best describes a documented limitation in larazotide’s clinical development for celiac disease?

Q4In direct comparison with BPC-157, the dossier states larazotide is primarily discussed in which research context?

Q5Which statement about larazotide’s safety and regulatory status is supported by the dossier?

10Sources

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Research and educational use onlyNothing on this site is medical advice, a prescription, or a recommendation for human use. Compounds documented here are research chemicals. Consult a qualified clinician before making any health decision.