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Library/For Recovery/Larazotide
RUO · Failed Phase 3Tight Junction+2 more

Larazotide

An eight-amino-acid tight-junction regulator developed for celiac disease as an adjunct to a gluten-free diet. We read all 60 studies. The protocol is below.

Updated 03 May 2026Read 11 minEvidence ●●●○○Citations 60
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Free — puts Larazotide on your decision board.

The Larazotide Report · $19

Everything you need to start: dose, sourcing, safety, our verdict.

One purchase · yours forever

Built from 60 cited studies.

Status
Research-only
Class
Tight Junction
Evidence
3/ 5●●●○○
FDA status
$19 ↓
Phase 2b enrollment
$19 ↓
Mechanism
$19 ↓
Read this if
  • you have biopsy-confirmed celiac disease and gluten cross-contamination still wrecks you
  • you're following the "leaky gut" literature and want to know what tight-junction modulation actually means
  • you want to understand why the phase 3 failed and whether that should change your mind (it should)
Skip this if
  • you don't have celiac disease and "leaky gut" is the only diagnosis you have
  • you want a drug in active development — this program is paused
  • you're paying clinic prices for an indication the phase 3 didn't validate
The 4 ways you can buy Larazotide
Brand
✗
Not available
No FDA-approved larazotide; sponsor has exited.
Compounded 503A
✓
Off-label
$200–$400/mo where sold
Mid–high. Some compounders carry; legally exposed since indication ('leaky gut') has no validated …
RUO (research-only)
✓
Sold 'for research only'
$60–$150/mo
Oral peptide is degraded by gut proteases — RUO 'larazotide' powder is hard to dose orally without…
Gray market
✓
Unregulated overseas import
Varies — not on user's vendor list
Available via overseas raws but oral peptide without enteric coating is functionally useless — gra…
Click any lane for the full Sourcing breakdown.
First 90 days · Larazotide
Weeks 1–2
Nothing perceptible. The healing-acceleration effect — if it's going to work — isn't a week-one signal. If you 'feel something' immediately, that's expectation, not the peptide.
Weeks 4–8
Subtle improvement on the target injury if it's going to work. Range of motion, less morning stiffness, less acute pain on load.
Week 12 — decide
Honest decision point. Either the injury is materially better than the no-peptide trajectory would have been, or it isn't. The clinical literature in humans is thin enough that your n=1 trial IS the evidence base.
Quit if
  • Any unusual symptoms — especially relevant if you have a personal or family cancer history (angiogenesis mechanism for BPC-157, TB-500).
  • 12 weeks with no perceived improvement vs the no-peptide trajectory.
  • New pain or symptoms at injection site that don't resolve in 48 hours.
Identity

What it is.

Larazotide is an eight-amino-acid that tightens the junctions between gut epithelial cells — the seals that decide what crosses from your gut lumen into your bloodstream. It does this by antagonizing zonulin, a protein that loosens those tight junctions in response to gluten and certain bacterial signals.

The drug development story is unusual. Larazotide was developed by Innovate Biopharmaceuticals (later 9 Meters Biopharma) specifically for celiac disease — to be taken before meals so people with celiac could tolerate accidental gluten exposure. It went through phase 3.

It is not FDA approved. The pivotal (CeDLara) failed to hit its primary endpoint in 2022 and the program was effectively shelved. There is no legal US supply. Anything sold as larazotide on the market is gray-market.

TL;DR

TL;DR. 30-second version.

The compressed verdict — what Larazotide actually is, what the human evidence shows, and the watch-for in three bullets. Locked.

Get the report · $19 ↓
Mechanism

Mechanism.

Mechanism · in the Larazotide report

How the molecule actually works — receptor profile, downstream signaling, what to expect mechanistically.

Get the report · $19 ↓
Evidence

Evidence. What we actually know in humans.

Evidence · in the Larazotide report

The trial breakdown — phase, n, primary endpoint, who funded, what hit, what didn't.

Get the report · $19 ↓
Human-Evidence Factbox
FDA status
$19 ↓
Phase 2b enrollment
$19 ↓
Mechanism
$19 ↓
Indication studied
$19 ↓
'Leaky gut' validated in humans
$19 ↓
Years of clinical study
$19 ↓
Dose

Dose. The actual protocol.

Dose · in the Larazotide report

The specific protocol — dose, titration schedule, cycle pattern, frequency, route.

We read 60 studies to write this report.
Get the report · $19 ↓
Sourcing

Sourcing. Where the cohort actually buys.

Sourcing · in the Larazotide report

Sourcing breakdown — vendor methodology, red flags, our published test results, COA checklist.

We read 60 studies to write this report.
Get the report · $19 ↓
Safety

Safety. Side effects.

Safety · in the Larazotide report

The watch-for list — contraindications, drug interactions, monitoring labs, when to stop.

Get the report · $19 ↓
Editorial Position

Editorial position.

Editorial Position · in the Larazotide report

Our editorial position — explicit yes / no / depends, with the reasoning behind it.

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Citations

Citations.

  1. 01Yang X, et al. Targeting endothelial tight junctions to predict and protect thoracic aortic aneurysm and dissection. European heart journal. 2023;44(14):1248-1261. PMID: 36638776.
  2. 02Troisi J, 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;28(28):5788-5807. PMID: 33397225.
  3. 03Tajik N, et al. Targeting zonulin and intestinal epithelial barrier function to prevent onset of arthritis. Nature communications. 2020;11(1):1995. PMID: 32332732.
  4. 04Veres-Székely A, et al. Zonulin as a Potential Therapeutic Target in Microbiota-Gut-Brain Axis Disorders: Encouraging Results and Emerging Questions. International journal of molecular sciences. 2023;24(8). PMID: 37108711.
  5. 05Damianos JA, et al. Coeliac disease and the intestinal barrier: mechanisms of disruption and strategies for restoration. Gut. 2026;75(4):826-838. PMID: 40579122.
+Show all 60 citations
  1. 06Huang YC, et al. Preventive effects of Larazotide acetate (AT-1001) on non-alcoholic fatty liver diseases (NAFLD) in a mouse model. Pediatrics and neonatology. 2026;67(1):84-88. PMID: 40562584.
  2. 07Cippitelli A, et al. AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. British journal of pharmacology. 2015;172(7):1834-45. PMID: 25440006.
  3. 08Hoilat GJ, 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;46(1):101782. PMID: 34339872.
  4. 09Tuan EW, et al. AT-1001 Is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors. Molecular pharmacology. 2015;88(4):640-9. PMID: 26162864.
  5. 10Zaveri NT, et al. Functional characterization of AT-1001, an α3β4 nicotinic acetylcholine receptor ligand, at human α3β4 and α4β2 nAChR. Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco. 2015;17(3):361-7. PMID: 25180076.
  6. 11Serena G, et al. Nondietary Therapies for Celiac Disease. Gastroenterology clinics of North America. 2019;48(1):145-163. PMID: 30711207.
  7. 12Dipasquale V, et al. New Therapeutic Challenges in Pediatric Gastroenterology: A Narrative Review. Healthcare (Basel, Switzerland). 2025;13(8). PMID: 40281872.
  8. 13Yonker LM, et al. Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide. Science translational medicine. 2025;17(809):eadu4284. PMID: 40737433.
  9. 14Yu F, 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;387:114205. PMID: 40915363.
  10. 15Slifer ZM, et al. Larazotide acetate: a pharmacological peptide approach to tight junction regulation. American journal of physiology. Gastrointestinal and liver physiology. 2021;320(6):G983-G989. PMID: 33881350.
  11. 16Veeraraghavan G, et al. Celiac disease 2015 update: new therapies. Expert review of gastroenterology & hepatology. 2015;9(7):913-27. PMID: 25864708.
  12. 17Khaleghi S, et al. The potential utility of tight junction regulation in celiac disease: focus on larazotide acetate. Therapeutic advances in gastroenterology. 2016;9(1):37-49. PMID: 26770266.
  13. 18Freeman HJ. Emerging drugs for celiac disease. Expert opinion on emerging drugs. 2015;20(1):129-35. PMID: 25494908.
  14. 19Glinka DM, et al. 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;5(4):100369. PMID: 40330848.
  15. 20Yoosuf S, et al. Evolving Therapy for Celiac Disease. Frontiers in pediatrics. 2019;7:193. PMID: 31157194.
  16. 21Girbal-González M, et al. Is There a Future Without Gluten Restrictions for Celiac Patients? Update on Current Treatments. Nutrients. 2025;17(18). PMID: 41010485.
  17. 22Alhassan E, et al. Novel Nondietary Therapies for Celiac Disease. Cellular and molecular gastroenterology and hepatology. 2019;8(3):335-345. PMID: 31146067.
  18. 23Khroyan TV, et al. High affinity α3β4 nicotinic acetylcholine receptor ligands AT-1001 and AT-1012 attenuate cocaine-induced conditioned place preference and behavioral sensitization in mice. Biochemical pharmacology. 2015;97(4):531-541. PMID: 26256075.
  19. 24McCarville JL, et al. Pharmacological approaches in celiac disease. Current opinion in pharmacology. 2015;25:7-12. PMID: 26414923.
  20. 25Toll L, et al. AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2012;37(6):1367-76. PMID: 22278092.
  21. 26Cardoso-Silva D, et al. Intestinal Barrier Function in Gluten-Related Disorders. Nutrients. 2019;11(10). PMID: 31581491.
  22. 27Cippitelli A, et al. Pharmacological stress is required for the anti-alcohol effect of the α3β4* nAChR partial agonist AT-1001. Neuropharmacology. 2015;93:229-36. PMID: 25689019.
  23. 28Gopalakrishnan S, et al. Larazotide acetate promotes tight junction assembly in epithelial cells. Peptides. 2012;35(1):95-101. PMID: 22401910.
  24. 29Slifer ZM, et al. Larazotide acetate induces recovery of ischemia-injured porcine jejunum via repair of tight junctions. PloS one. 2021;16(4):e0250165. PMID: 33886649.
  25. 30Gopalakrishnan S, et al. Larazotide acetate regulates epithelial tight junctions in vitro and in vivo. Peptides. 2012;35(1):86-94. PMID: 22401908.
  26. 31Yuan M, et al. The α3β4 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. 2017;333:251-257. PMID: 28693859.
  27. 32Valitutti F, et al. Breaking Down Barriers: How Understanding Celiac Disease Pathogenesis Informed the Development of Novel Treatments. Digestive diseases and sciences. 2019;64(7):1748-1758. PMID: 31076989.
  28. 33Yonker LM, et al. Zonulin Antagonist, Larazotide (AT1001), As an Adjuvant Treatment for Multisystem Inflammatory Syndrome in Children: A Case Series. Critical care explorations. 2022;10(2):e0641. PMID: 35211683.
  29. 34Kelly CP, et al. Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study. Alimentary pharmacology & therapeutics. 2013;37(2):252-62. PMID: 23163616.
  30. 35Szaflarska-Popławska A. Non-dietary methods in the treatment of celiac disease. Przeglad gastroenterologiczny. 2015;10(1):12-7. PMID: 25960809.
  31. 36Leffler DA, et al. Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial. Gastroenterology. 2015;148(7):1311-9.e6. PMID: 25683116.
  32. 37Leffler DA, et al. A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge. The American journal of gastroenterology. 2012;107(10):1554-62. PMID: 22825365.
  33. 38Kulkarni A, et al. Current pharmacological approaches and potential future therapies for Celiac disease. European journal of pharmacology. 2021;909:174434. PMID: 34418405.
  34. 39Paterson BM, et al. The safety, tolerance, pharmacokinetic and pharmacodynamic effects of single doses of AT-1001 in coeliac disease subjects: a proof of concept study. Alimentary pharmacology & therapeutics. 2007;26(5):757-66. PMID: 17697209.
  35. 40Karahan D, et al. Ameliorative Effects of Larazotide Acetate on Intestinal Permeability and Bacterial Translocation in Acute Pancreatitis Model in Rats. Digestive diseases and sciences. 2024;69(4):1242-1252. PMID: 38441784.
  36. 41D'heedene M, et al. Celiac disease: Hope for new treatments beyond a gluten-free diet. Clinical nutrition (Edinburgh, Scotland). 2024;43(6):1240-1249. PMID: 38648685.
  37. 42Caio G, et al. Therapeutic options for coeliac disease: What else beyond gluten-free diet?. Digestive and liver disease : official journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver. 2020;52(2):130-137. PMID: 31831308.
  38. 43Beken S, et al. Negative Effects of Noise on NICU Graduates' Cochlear Functions. Fetal and pediatric pathology. 2021;40(4):295-304. PMID: 31984823.
  39. 44Yonker LM, et al. Multisystem inflammatory syndrome in children is driven by zonulin-dependent loss of gut mucosal barrier. The Journal of clinical investigation. 2021;131(14). PMID: 34032635.
  40. 45Enomoto H, et al. In vivo assessment of a delayed release formulation of larazotide acetate indicated for celiac disease using a porcine model. PloS one. 2021;16(4):e0249179. PMID: 33844694.
  41. 46Kurada S, et al. Current and novel therapeutic strategies in celiac disease. Expert review of clinical pharmacology. 2016;9(9):1211-23. PMID: 27322016.
  42. 47Jauregi-Miguel A. The tight junction and the epithelial barrier in coeliac disease. International review of cell and molecular biology. 2021;358:105-132. PMID: 33707052.
  43. 48Knox HJ, et al. Characterization of Binding Site Interactions and Selectivity Principles in the α3β4 Nicotinic Acetylcholine Receptor. Journal of the American Chemical Society. 2022;144(35):16101-16117. PMID: 36006801.
  44. 49Baldassarre M, et al. Celiac disease: pathogenesis and novel therapeutic strategies. Endocrine, metabolic & immune disorders drug targets. 2008;8(3):152-8. PMID: 18782011.
  45. 50Silverman GJ, et al. Sex-dependent Lupus Blautia (Ruminococcus) gnavus strain induction of zonulin-mediated intestinal permeability and autoimmunity. Frontiers in immunology. 2022;13:897971. PMID: 36032126.
  46. 51Ailioaie LM, et al. Celiac Disease and Targeting the Molecular Mechanisms of Autoimmunity in COVID Pandemic. International journal of molecular sciences. 2022;23(14). PMID: 35887067.
  47. 52Mousavi Maleki MS, 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;55(11):1601-1619. PMID: 37803248.
  48. 53Zofková I. [Celiac disease and its relation to bone metabolism]. Casopis lekaru ceskych. 2009;148(6):246-8. PMID: 19642305.
  49. 54Armandi A, et al. Tight junction regulation in celiac disease: role of larazotide acetate. Minerva gastroenterology. 2022;68(1):4-6. PMID: 33793152.
  50. 55Gharpure A, et al. Agonist Selectivity and Ion Permeation in the α3β4 Ganglionic Nicotinic Receptor. Neuron. 2019;104(3):501-511.e6. PMID: 31488329.
  51. 56Fretzen A. Peptide therapeutics for the treatment of gastrointestinal disorders. Bioorganic & medicinal chemistry. 2018;26(10):2863-2872. PMID: 29183663.
  52. 57Di Micco 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;8:628609. PMID: 33520943.
  53. 58Di Micco 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;22(17). PMID: 34502335.
  54. 59Pearce SC, et al. Marked differences in tight junction composition and macromolecular permeability among different intestinal cell types. BMC biology. 2018;16(1):19. PMID: 29391007.
  55. 60Arrieta MC, et al. Reducing small intestinal permeability attenuates colitis in the IL10 gene-deficient mouse. Gut. 2009;58(1):41-8. PMID: 18829978.
The Larazotide Report · $19

Everything you need to start.

Dose, sourcing, safety, our verdict. One purchase. Yours forever.

Built from 60 cited studies.

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