Peptide LibraryLarazotide
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.
For research use only.
Key Facts
- CAS
- 258818-34-7
- Molecular Weight (MW)
- 725.8 g/mol
- Half-life
- —
- FDA status
- Investigational New Drug (IND)
- Evidence level
- Clinical Trial Evidence
- Human dose established
- Yes
- Administration Route
- Oral
- Frequency
- Three times daily
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 2026
Vendor price snapshot
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- Vendors listing this peptide
- 1
- Listed offers
- 1
- Price per mg
- —
Research summary
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.
Research evidence
- Regulatory review (FDA label)None in reviewed sources
- Controlled human trials3 reviewed sources
- Early or uncontrolled human studiesNone in reviewed sources
- Lab & animal studiesNone in reviewed sources
How it works
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.
Peptide Library's Larazotide profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Larazotide dosage evidence
Larazotide has no approved dosage; there is no larazotide label on DailyMed. Human dosing comes from celiac disease trials of doses taken by mouth three times daily: a phase 2b trial of 0.5, 1 and 2 mg met its primary endpoint only at 0.5 mg, a gluten-challenge study tested 0.25 to 8 mg, and a phase 3 trial of 0.25 and 0.5 mg was terminated by its sponsor with no results posted.
| Human dosing established | Yes |
|---|---|
| Studied dose range | 0.25–8 mg three times daily studied in trials |
| Route | Oral |
| Frequency | Three times daily |
| Duration studied | 14 days to 12 weeks in the published trials |
| Evidence level | Clinical Trial Evidence |
| Last reviewed | 2026-11-07 |
Research-reported dosing
Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.
| Study / context | Population | Dose | Route | Frequency | Duration | Outcome studied | Source |
|---|---|---|---|---|---|---|---|
| Phase 2b, persistent symptoms despite a gluten-free diet — Gastroenterology 2015 (NCT01396213)Clinical trial · Randomised, double-blind, placebo-controlled trial | Adults with celiac disease on a gluten-free diet for at least 12 months with ongoing symptoms (n=342) | 0.5 mg, 1 mg or 2 mg, or placebo | Oral | Three times daily | 12 weeks | Primary endpoint (gastrointestinal symptom score) met with 0.5 mg; 1 mg and 2 mg were no different from placebo on any endpoint; safety comparable with placebo | Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial. Gastroenterology. 2015. |
| Gluten-challenge dose-ranging study — Am J Gastroenterol 2012Clinical trial · Randomised, double-blind, placebo-controlled dose-ranging study | Adults with diet-controlled celiac disease (n=86) | 0.25, 1, 4 or 8 mg, or placebo, with or without 2.4 g/day gluten | Oral | Three times daily | 14 days | 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 | A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge. Am J Gastroenterol. 2012. |
| Phase 3 symptom-relief trial (NCT03569007)Clinical trial · Randomised, double-blind, placebo-controlled phase 3 trial | Adults with biopsy-confirmed celiac disease on a gluten-free diet for at least 6 months with persistent symptoms (307 enrolled) | 0.25 mg or 0.5 mg capsules, or placebo | Oral | Three times daily | 12 weeks to the primary endpoint | Terminated by the sponsor; no results posted on ClinicalTrials.gov | NCT03569007 — Study to Evaluate the Efficacy and Safety of Larazotide Acetate for the Relief of CeD Symptoms |
Where sources disagree
- Larazotide acetate was given by mouth in celiac disease trials (in the phase 3 trial as enteric-coated beads in gelatin capsules), not as an injection. In the phase 2b trial only the lowest dose separated from placebo; higher doses did not.
- The only phase 3 trial was terminated by its sponsor without posted results, so no dose has been confirmed in phase 3.
Sequence & molecular data
| Amino acid sequence | Gly-Gly-Val-Leu-Val-Gln-Pro-Gly |
|---|---|
| Molecular formula | C32H55N9O10 |
| Molecular weight | 725.8 g/mol |
| CAS number | 258818-34-7 |
| PubChem CID | 9810532 |
| FDA UNII | ZN3R5560ZV |
| ChEMBL | CHEMBL2105646 |
| DrugBank | DB05645 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
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.
Studies
- Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide
- Celiac disease: Hope for new treatments beyond a gluten-free diet
- Larazotide acetate: a pharmacological peptide approach to tight junction regulation
- The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases
- Preventive effects of Larazotide acetate (AT-1001) on non-alcoholic fatty liver diseases (NAFLD) in a mouse model
Research statistics
45 PubMed publications · 15.9% human clinical research · 10 registered trials
Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted
Regulatory & research status
Larazotide has been studied under an Investigational New Drug application. It is not approved for marketing.
| FDA status | Investigational New Drug (IND) |
|---|---|
| Research status | Investigational; clinical development reported |
| Availability | Research-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | Clinical Trial |
How FDA approval, compounding and research-only status differ
Benefits
—
Larazotide side effects
No side effects listed yet for this entry.
Storage & stability
This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.
Larazotide: 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, 2025External reference
- Celiac disease: Hope for new treatments beyond a gluten-free diet — Clin Nutr, 2024External reference
- Larazotide acetate: a pharmacological peptide approach to tight junction regulation — Am J Physiol Gastrointest Liver Physiol, 2021External reference
- The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases — Curr Med Chem, 2021External reference
- Preventive effects of Larazotide acetate (AT-1001) on non-alcoholic fatty liver diseases (NAFLD) in a mouse model — Pediatr Neonatol, 2026External reference
Related research, comparisons & guides
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2
This Larazotide profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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