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Gastrointestinal · Investigational

Larazotide

No lawful US pathway

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Written by Peptide Association Editorial TeamLast reviewed Editorial policy

01 · Overview

A synthetic octapeptide tight junction regulator derived from a Vibrio cholerae toxin, described as a zonulin antagonist (PMID 33397225). In laboratory studies larazotide acetate prevents opening of intestinal epithelial tight junctions (PMID 22825365).

By reducing paracellular permeability, it was intended to limit gluten peptide passage across the intestinal barrier in celiac disease and the immune response that follows.

02 · Research summary & key findings

In a phase 2b trial in 342 celiac patients with persistent symptoms despite a gluten-free diet, the lowest dose reduced gastrointestinal symptoms vs. placebo, while higher doses did not differ from placebo (Leffler et al., Gastroenterology, 2015) (PMID 25683116). In gluten challenge studies, larazotide limited symptoms and antibody responses at some doses, but did not change the lactulose-to-mannitol permeability ratio (PMID 22825365) (PMID 23163616). A phase 3 celiac trial (NCT03569007) was terminated by its sponsor in 2022, so there is still no approved drug therapy for celiac disease. Recent small studies have tested larazotide in post-COVID conditions, including a phase 2a trial in 12 children with MIS-C (PMID 40737433).

03 · Regulatory status

Larazotide is in the investigational stage. While preclinical and early-phase data exist, it has not received regulatory approval for clinical use in the United States.

No lawful pathway today

Larazotide is not FDA-approved and does not currently have a lawful prescription or compounding pathway in the United States, so we do not sell it and will not book a consultation for it. That can change: in 2026 FDA began reviewing several peptides for compounding.

See the 7 FDA-approved compounds in Gastrointestinal

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04 · Administration routes

  • Oral

References

  1. [1]A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge Am J Gastroenterol, 2012. PMID 22825365
  2. [2]Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study Aliment Pharmacol Ther, 2013. PMID 23163616
  3. [3]Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial Gastroenterology, 2015. PMID 25683116
  4. [4]The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases Curr Med Chem, 2021. PMID 33397225
  5. [5]Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide Sci Transl Med, 2025. PMID 40737433

Primary literature

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Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol. See our editorial policy for how this content is produced and reviewed. Clinicians: join the network.