Page data last changed: . Chemistry registry snapshot: . Registry refreshes and identity assessments are separate from scientific content review.
An orally studied octapeptide aimed at the gut's tight junctions.
Also known as: larazotide acetate · AT-1001
Part of the Foundational & therapeutic peptides cluster
Overview
Larazotide (larazotide acetate, AT-1001) is a synthetic eight-amino-acid peptide studied as a regulator of intestinal tight junctions, the seals between gut lining cells. It was investigated in celiac disease research. Its Phase 3 program was discontinued and it is not approved; this page is educational only.
Source & context
Biological / chemical source: Synthetic octapeptide
Primary research or clinical context: Investigational compound; Phase 3 program discontinued, not approved
Tight-junction target
Larazotide (GGVLVQPG) is designed to act at the gut epithelial barrier, where tight junctions control how much passes between cells. It is studied as an antagonist of zonulin-driven permeability, intended to keep junctions in their closed state. It is meant to act locally in the intestine rather than being absorbed systemically.
Development and status
Larazotide was studied mainly in celiac disease, but its sponsor announced discontinuation of a Phase 3 trial in 2022, and it has not been approved by Health Canada or the FDA. It remains an investigational compound. This summary describes the peptide and its research history and makes no therapeutic claims.
Sequence
One-letter sequence commonly cited for Larazotide (educational; isoforms and modifications may differ):
GGVLVQPG
Residues plotted ~100° apart around an α-helix — clustering of one color reveals an amphipathic face.
Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
H- and -OH denote free termini around the same eight-residue GGVLVQPG chain. They are not additional residues. The reference is the free peptide, not larazotide acetate.
- Molecular form
- Larazotide, eight-residue free peptide (not acetate salt)
- Species
- Not established by this molecular identity audit
- Termini (N / C)
- Free amine / Free acid
Average reference mass · Molecular identity assessment: 2026-10-05
Reference policy updated: 2026-10-05
- IUPHAR/BPS source snapshot · 2026-10-01
- PubChem molecular record · 2026-10-01
- Molecular formula
- C32H55N9O10
- Average reference mass
- ≈ 725.8
- C-terminus
- Free acid
- PubChem CID: 9810532
- IUPHAR ligand: 13724
- ChEMBL: CHEMBL2105646
- DrugBank: DB05645
- CAS RN: 258818-34-7
- UNII: ZN3R5560ZV
Chemistry values: PubChem, IUPHAR/BPS Guide to Pharmacology · fetched 2026-10-01.
Clinical development snapshot
ClinicalTrials.gov lists 29 registered studies with “Larazotide” as an intervention (snapshot 2026-09-06). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT06904261 | A Study of Migalastat in Pediatric Subjects (2 to <12 Yrs) With Fabry Disease and Amenable GLA Variants | Phase 3 | recruiting | 2026-09-01 |
| NCT05747534 | AT1001 for the Treatment of Long COVID | Phase 2 | completed | 2026-08-18 |
| NCT04020055 | A Study to Evaluate Migalastat in Fabry Subjects With Amenable GLA Variant and Renal Disease | Phase 3 | active not recruiting | 2026-07-06 |
| NCT04049760 | Safety, Pharmacodynamics, and Efficacy of Migalastat in Pediatric Subjects (Aged >12 Years) With Fabry Disease | Phase 3 | completed | 2026-02-05 |
| NCT01476163 | Physician Initiated Expanded Access Request for Migalastat in Individual Patients With Fabry Disease | — | available | 2025-07-03 |
| NCT05022303 | AT1001 for the Treatment of COVID-19 Related MIS-C | Phase 2 | terminated | 2024-06-13 |
Larazotide — reconstitution calculator
Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.
Reference form: Larazotide, eight-residue free peptide (not acetate salt)Average reference mass: 725.8 Da
Enter an amount to see the volume it corresponds to.
Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.
FAQ about Larazotide
What is Larazotide?+
Larazotide (larazotide acetate, AT-1001) is a synthetic eight-amino-acid peptide studied as a regulator of intestinal tight junctions, the seals between gut lining cells. It was investigated in celiac disease research. Its Phase 3 program was discontinued and it is not approved; this page is educational only.
What Canadian product status is recorded for Larazotide?+
Canadian product status for Larazotide has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.
What is the typical length of Larazotide?+
Larazotide is commonly described as approximately 8 amino acids (Tight-junction regulator peptide).
Related peptides
References & further reading
- 1.Troisi et al. (2021). The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases. Curr Med Chem
- 2.Yu et al. (2025). Antibacterial hyaluronic acid hydrogel with sustained release of larazotide as effective colitis treatment. J Control Release
- 3.Yonker et al. (2025). Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide. Sci Transl Med
- 4.Gopalakrishnan et al. (2012). Larazotide acetate regulates epithelial tight junctions in vitro and in vivo. Peptides
- 5.Kelly et al. (2013). Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study. Aliment Pharmacol Ther
- 6.Gopalakrishnan et al. (2012). Larazotide acetate promotes tight junction assembly in epithelial cells. Peptides
- 7.Slifer et al. (2021). Larazotide acetate: a pharmacological peptide approach to tight junction regulation. Am J Physiol Gastrointest Liver Physiol
- 8.Hoilat et al. (2022). Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials. Clin Res Hepatol Gastroenterol
- 9.PubChem — compound summary for Larazotide (CID 9810532)
- 10.Wikipedia — Larazotide