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Larazotide

Also known as: Larazotide Acetate · AT-1001

Investigational oral peptide tight-junction regulator studied for celiac disease.

B
Grade B
Human observational studies
Human studies29
PubMed citations30
Routeoral
Regulatory (US)Rx required
Last verified2 days ago

Mechanism of action

Zonulin antagonist. Regulates intestinal epithelial tight junctions to reduce paracellular permeability triggered by gluten.

Evidence summary

29
Human studies
30
PubMed citations
25
Clinical trials
B
Evidence grade

Evidence summary in progress. See the citations section below for the underlying research papers.

Dosing protocols

Educational information only. Consult a licensed provider before using any peptide.
Administration routes
oral

Side effects & safety

No FDA label or editorial side-effect profile is on file for this compound yet. See the clinical trials and citations sections for study-reported safety data.

Interactions

No documented drug interactions on file.

Regulatory status

United States
Not FDA approved

Investigational — Phase 3 trial (CeDLara) did not meet primary endpoint. Not approved.

Compounding
Not permitted

Not available via 503A/503B compounding pharmacies.

Regulatory data last verified 4/19/2026

Clinical trials

NCT04020055An Open-label Study to Evaluate the Safety and Pharmacokinetics of Migalastat HCl in Subjects With Fabry Disease and Amenable GLA Variants and Severe Renal Impairment or End-Stage Renal Disease Treated With HemodialysisActive Not Recruiting · Phase 3 · Fabry Disease · n=14NCT04049760A Long-term, Open-label Study to Evaluate the Safety, Pharmacodynamics, and Efficacy of Migalastat in Subjects > 12 Years of Age With Fabry Disease and Amenable GLA VariantsCompleted · Phase 3 · Fabry Disease · n=16NCT06904261An Open-label Study of the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of 12 Month Treatment With Migalastat in Pediatric Subjects (Aged 2 to < 12 Years) With Fabry Disease and Amenable GLA VariantsRecruiting · Phase 3 · Fabry Disease · n=8NCT05747534Phase 2a Randomized, Double-Blind, Placebo-Controlled, Multi-Center Study to Evaluate the Safety and Efficacy of Larazotide (AT1001) for the Treatment of Long COVID in Children and AdultsRecruiting · Phase 2 · Long COVID · n=150NCT01476163Physician Initiated Expanded Access Request for Treatment Use of Migalastat Hydrochloride (AT1001), an Investigational Treatment for Individual Patients With Fabry Disease (AT1001-188)Available · Fabry DiseaseNCT05022303A Phase 2a (Proof of Concept), Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of AT1001 for the Treatment of COVID-19 Related Multisystem Inflammatory Syndrome in Children (MIS-C)Terminated · Phase 2 · Covid19 · n=12NCT03569007A Phase 3, Randomized, Double-Blind, Placebo Controlled Study to Evaluate the Efficacy and Safety of Larazotide Acetate for the Relief of Persistent Symptoms in Patients With Celiac Disease on a GFDTerminated · Phase 3 · Celiac Disease · n=307NCT03500094An Open-label Study of the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of 12 Month Treatment With Migalastat in Pediatric Subjects (Aged 12 to <18 Years) With Fabry Disease and Amenable GLA VariantsCompleted · Phase 3 · Fabry Disease · n=22NCT02194985An Open-Label Extension Study to Evaluate the Long-Term Safety and Efficacy of Migalastat Hydrochloride Monotherapy in Subjects With Fabry DiseaseCompleted · Phase 3 · Fabry Disease · n=84NCT01196871An Open-label Phase 2A Study to Investigate Drug-Drug Interactions Between AT1001 (Migalastat Hydrochloride) and Agalsidase in Subjects With Fabry DiseaseCompleted · Phase 2 · Fabry Disease · n=20NCT01218659A Randomized, Open-Label Study to Compare the Efficacy and Safety of AT1001 and Enzyme Replacement Therapy (ERT) in Patients With Fabry Disease and AT1001-Responsive GLA Mutations, Who Were Previously Treated With ERTCompleted · Phase 3 · Fabry Disease · n=68NCT00283959A Phase 2, Open-Label, Single Dose Level, 12-Week Study to Evaluate the Safety, Tolerability, and Pharmacodynamics of AT1001 in Patients With Fabry DiseaseCompleted · Phase 2 · Fabry Disease · n=4

Showing 12 of 25 indexed studies. View all on ClinicalTrials.gov →

Citations

PMID 41769533Kubala K, Pietrucha T et al. · Integrated Role of Microbial, Fungal, and Plant-Derived Interventions in the Management of Celiac Disease: A Narrative Review.Cureus (2026)HumanPMID 40915363Yu F, Chen Y et al. · Antibacterial hyaluronic acid hydrogel with sustained release of larazotide as effective colitis treatment.Journal of controlled release : official journal of the Controlled Release Society (2025)HumanPMID 40281872Dipasquale V, Romano C · New Therapeutic Challenges in Pediatric Gastroenterology: A Narrative Review.Healthcare (Basel, Switzerland) (2025)HumanPMID 40737433Yonker LM, Kane AS et al. · Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide.Science translational medicine (2025)HumanPMID 39252622Mohammadi-Kordkhayli M, Mousavi MJ et al. · Elucidating the Significance of Zonulin in the Pathogenesis of Chronic Inflammatory Disorders: Emphasis on Intestinal Barrier Function and Tight Junction Regulation.Current medicinal chemistry (2025)HumanPMID 40330848Glinka DM, MacGregor GG · The PAR2 Antagonist Larazotide Can Mitigate Acute Histamine-Stimulated Epithelial Barrier Disruption in Keratinocytes: A Potential Adjunct Treatment for Atopic Dermatitis.JID innovations : skin science from molecules to population health (2025)HumanPMID 37803248Mousavi Maleki MS, Aghamirza Moghim Ali Abadi H et al. · Bromelain and ficin proteolytic effects on gliadin cytotoxicity and expression of genes involved in cell-tight junctions in Caco-2 cells.Amino acids (2023)HumanPMID 34339872Hoilat GJ, Altowairqi AK et al. · Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials.Clinics and research in hepatology and gastroenterology (2022)HumanPMID 33707052Jauregi-Miguel A · The tight junction and the epithelial barrier in coeliac disease.International review of cell and molecular biology (2022)HumanPMID 34418405Kulkarni A, Patel S et al. · Current pharmacological approaches and potential future therapies for Celiac disease.European journal of pharmacology (2022)HumanPMID 35211683Yonker LM, Swank Z et al. · Zonulin Antagonist, Larazotide (AT1001), As an Adjuvant Treatment for Multisystem Inflammatory Syndrome in Children: A Case Series.Critical care explorations (2022)PMID 33881350Slifer ZM, Krishnan BR et al. · Larazotide acetate: a pharmacological peptide approach to tight junction regulation.American journal of physiology. Gastrointestinal and liver physiology (2021)HumanPMID 33844694Enomoto H, Yeatts J et al. · In vivo assessment of a delayed release formulation of larazotide acetate indicated for celiac disease using a porcine model.PloS one (2021)HumanPMID 33520943Di Micco S, Musella S et al. · In silico Analysis Revealed Potential Anti-SARS-CoV-2 Main Protease Activity by the Zonulin Inhibitor Larazotide Acetate.Frontiers in chemistry (2021)HumanPMID 33397225Troisi J, Venutolo G et al. · The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases.Current medicinal chemistry (2021)HumanPMID 34502335Di Micco S, Musella S et al. · Peptide Derivatives of the Zonulin Inhibitor Larazotide (AT1001) as Potential Anti SARS-CoV-2: Molecular Modelling, Synthesis and Bioactivity Evaluation.International journal of molecular sciences (2021)HumanPMID 32332732Tajik N, Frech M et al. · Targeting zonulin and intestinal epithelial barrier function to prevent onset of arthritis.Nature communications (2020)HumanPMID 31146067Alhassan E, Yadav A et al. · Novel Nondietary Therapies for Celiac Disease.Cellular and molecular gastroenterology and hepatology (2020)HumanPMID 31157194Yoosuf S, Makharia GK · Evolving Therapy for Celiac Disease.Frontiers in pediatrics (2020)HumanPMID 28693859Yuan M, Malagon AM et al. · The &#x3b1;3&#x3b2;4 nAChR partial agonist AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats.Behavioural brain research (2018)Human

Showing 20 of 30 papers. View all on PubMed →