--- title: "Larazotide" canonical_url: https://peptidelibrary.app/library/larazotide description: "Orally administered octapeptide investigated as an adjunct to a gluten-free diet in coeliac disease. It acts locally in the intestinal lumen. Not FDA-approved." updated: 2026-11-07 publisher: Peptide Library notice: "Research and educational use only. Not medical advice." --- # Larazotide Larazotide is a research peptide in the Tight Junction Regulator class. Larazotide is a synthetic peptide antagonist of zonulin, the endogenous regulator of intestinal tight junctions. By blocking zonulin-mediated tight junction disassembly it is intended to reduce paracellular permeability, limiting passage of gliadin peptides across the epithelium and the downstream immune activation. Orally administered octapeptide investigated as an adjunct to a gluten-free diet in coeliac disease. It acts locally in the intestinal lumen. Not FDA-approved. ## Classification - Type: Investigational tight junction regulator - Mechanism class: Tight Junction Regulator - Development stage: In clinical development - Regulatory class: Investigational, not FDA-approved ## Mechanism Larazotide is a synthetic peptide antagonist of zonulin, the endogenous regulator of intestinal tight junctions. By blocking zonulin-mediated tight junction disassembly it is intended to reduce paracellular permeability, limiting passage of gliadin peptides across the epithelium and the downstream immune activation. Because it is not meaningfully absorbed, its activity is confined to the gut lumen. ## Properties - Sequence: Gly-Gly-Val-Leu-Val-Gln-Pro-Gly - Length: 8 - Molecular formula: C32H55N9O10 - Molecular weight: 725.8 g/mol - CAS number: 258818-34-7 - Studied routes: Oral ## Evidence - Evidence level: Clinical Trial Evidence - Highest documented: Controlled human trials - Human trials: 3 - Controlled human trials: 3 - Preclinical sources: 0 - Latest source: 2015 Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess. ### Studies 1. Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial. Gastroenterology. 2015. 2015. Controlled human trial. Population: Adults with celiac disease on a gluten-free diet for at least 12 months with ongoing symptoms (n=342) [Source](https://pubmed.ncbi.nlm.nih.gov/25683116/) 2. A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge. Am J Gastroenterol. 2012. 2012. Controlled human trial. Population: Adults with diet-controlled celiac disease (n=86). No significant effect on the primary permeability measure (lactulose/mannitol ratio), which was highly variable; some lower doses, not the highest, appeared to limit gluten-induced symptom worsening [Source](https://pubmed.ncbi.nlm.nih.gov/22825365/) 3. NCT03569007 — Study to Evaluate the Efficacy and Safety of Larazotide Acetate for the Relief of CeD Symptoms. Controlled human trial. Population: Adults with biopsy-confirmed celiac disease on a gluten-free diet for at least 6 months with persistent symptoms (307 enrolled). Terminated by the sponsor; no results posted on ClinicalTrials.gov [Source](https://clinicaltrials.gov/study/NCT03569007) ### Registered trials - [NCT03569007](https://clinicaltrials.gov/study/NCT03569007) ## Safety Human safety basis: Clinical trial reports Key limitations: Not approved by the FDA for any use.. ## Regulatory status Larazotide has been studied under an Investigational New Drug application. It is not approved for marketing. - FDA status: Investigational New Drug (IND) - Availability: Research-Only ## Frequently asked questions ### What is Larazotide? Orally administered octapeptide investigated as an adjunct to a gluten-free diet in coeliac disease. It acts locally in the intestinal lumen. Not FDA-approved. ### How does Larazotide work? Larazotide is a synthetic peptide antagonist of zonulin, the endogenous regulator of intestinal tight junctions. By blocking zonulin-mediated tight junction disassembly it is intended to reduce paracellular permeability, limiting passage of gliadin peptides across the epithelium and the downstream immune activation. ### Is Larazotide FDA approved? No. Larazotide is investigational: it is in clinical development and has not been approved by the FDA for any indication. Investigational status means trials are ongoing or complete but regulatory review has not resulted in approval, and efficacy and safety are still being established. ### What is the amino acid sequence of Larazotide? Larazotide has the sequence Gly-Gly-Val-Leu-Val-Gln-Pro-Gly, giving a chain of 8 amino acids. Its molecular formula is C32H55N9O10. ### What peptides are similar to Larazotide? Compounds most often compared with Larazotide include Teduglutide, Linaclotide, Plecanatide and Secretin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ. ## References - [Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide — Sci Transl Med, 2025](https://pubmed.ncbi.nlm.nih.gov/40737433/) - [Celiac disease: Hope for new treatments beyond a gluten-free diet — Clin Nutr, 2024](https://pubmed.ncbi.nlm.nih.gov/38648685/) - [Larazotide acetate: a pharmacological peptide approach to tight junction regulation — Am J Physiol Gastrointest Liver Physiol, 2021](https://pubmed.ncbi.nlm.nih.gov/33881350/) - [The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases — Curr Med Chem, 2021](https://pubmed.ncbi.nlm.nih.gov/33397225/) - [Preventive effects of Larazotide acetate (AT-1001) on non-alcoholic fatty liver diseases (NAFLD) in a mouse model — Pediatr Neonatol, 2026](https://pubmed.ncbi.nlm.nih.gov/40562584/) Note: Dose figures are left out of this Markdown version. See the cited sources.