Larazotide
Larazotide Acetate (AT-1001)
Overview
Larazotide acetate is a synthetic 8-amino-acid peptide derived from Zonula Occludens Toxin that acts as a tight junction regulator reducing intestinal permeability. It has completed Phase 2 clinical trials for celiac disease demonstrating significant reductions in intestinal permeability and symptoms. Larazotide is notable as a targeted pharmacological approach to intestinal barrier function — addressing the leaky gut mechanism that underlies multiple inflammatory and autoimmune conditions beyond celiac disease.
Mechanism of Action
Larazotide acts as a competitive antagonist of zonulin — an endogenous protein that regulates tight junction permeability in the intestinal epithelium. Zonulin triggers the disassembly of tight junction proteins (claudins occludin ZO-1) increasing intestinal permeability and allowing luminal antigens to cross the epithelial barrier and trigger immune activation. By blocking the zonulin receptor on epithelial cells larazotide prevents tight junction disruption maintaining the intestinal barrier integrity. This mechanism is particularly relevant in celiac disease where gliadin triggers zonulin release causing the intestinal permeability that allows gluten peptides to trigger the immune response. Clinical trials have demonstrated reductions in intestinal permeability markers and symptom improvements even during gluten exposure.
Dosage Information
Typical Dose
0.5-2 mg three times daily (Phase 2 trial doses)
Frequency
Three times daily before meals
Administration
Oral capsule
Notes
Phase 2 trials completed for celiac disease. Not yet FDA approved. Research use as a tight junction stabilizer for leaky gut applications. Oral bioavailability is intentionally limited — local gut action is the therapeutic target.
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Evidence Score
0.70
Compound Data
Molecular Formula
C32H55N9O10
Molecular Weight
725.80 g/mol
IUPAC Name
2-[[(2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]acetic acid
PubChem CID
9810532Potential Side Effects
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Quick Facts
- Administration
- Oral capsule
- Typical Dose
- 0.5-2 mg three times daily (Phase 2 trial doses)
- Frequency
- Three times daily before meals
- References
- 0 curated + 49 from PubMed
- Clinical Trials
- 28 registered
- Evidence Score
- 0.7 / 100