Larazotide Acetate
AT-1001 Tight Junction Regulator
Evidence grade 2 of 5, Thin. Read how the Atlas grades evidence.
Larazotide reached a positive Phase 2b readout in celiac disease (342-patient CeDLara-precursor trial, 0.5 mg dose associated with fewer symptomatic days versus placebo), but the pivotal Phase 3 CeDLara trial (9 Meters Biopharma) was discontinued in June 2022 after an independent interim analysis found the required additional enrollment too large to reach a meaningful outcome, a futility signal. A 2021 systematic review and meta-analysis pooled the RCTs and found inconsistent, dose-variable effects. Because the furthest and only pivotal trial failed on futility and no approval followed, the honest grade for the supported use is preliminary human evidence, not moderate RCT support.
- FDA
- Never approved. Reached Phase 3 (CeDLara, 9 Meters Biopharma), the furthest any celiac drug has advanced, but the Phase 3 was discontinued in June 2022 for futility after an interim analysis. FDA Fast Track designation had been granted earlier; no approval followed.
- WADA
- Not listed on the WADA Prohibited List; no performance-enhancement rationale.
Reference only. Not medical advice.
What can go wrong
Failed pivotal Phase 3 (futility); not approved. Gray-market 'leaky gut' use is unsupported by outcome data.
Talk to a clinician before taking this. The Atlas can tell you what has been studied about Larazotide Acetate. It cannot tell you how it would interact with your body, your history, or anything else you are taking, and nothing on this page is a reason to start.
A synthetic 8-amino-acid tight junction regulator (zonulin antagonist) developed for celiac disease. It reached Phase 3, the furthest of any celiac drug, but that pivotal trial (9 Meters Biopharma, CeDLara) was discontinued in 2022 for futility after an interim analysis, and it is not approved. Gray-market 'leaky gut' use is unsupported by outcome trials.
What people take it for
These are the reasons people give for taking it. They are not effects it has been shown to have.
How it is supposed to work
Larazotide is a synthetic eight-amino-acid peptide that tightens the junctions between intestinal cells, reducing the leakiness through which gluten fragments are thought to drive celiac symptoms. Taken orally, it is not absorbed but acts locally in the gut, and was developed as an add-on to the gluten-free diet for people who still have symptoms.
Larazotide acetate is a synthetic, single-chain eight-amino-acid peptide, taken orally and acting locally in the gut with little absorption. It is derived from the biology of zonulin, the body’s own tight-junction loosener, and was originally traced back to a cholera-bacterium toxin that does the opposite, opening the gut barrier.
- Type
- Tight-junction regulator
- Form
- Oral peptide
- Action
- Zonulin antagonist
- Lead status
- First celiac drug to Phase 3
- Phase 3
- Failed (2022)
- Approved
- No
The Leading "Leaky Gut" Drug, Undone In Phase 3
Larazotide is a useful drug to know precisely because it did not work out. For people with celiac disease the only treatment is a strict, lifelong, difficult gluten-free diet, so a drug that could blunt the damage from accidental gluten was a real prize, and larazotide was the front-runner: the first celiac drug into clinical trials more than fifteen years ago, the first to reach Phase 3, and backed by encouraging Phase 2 data showing it eased gluten-triggered symptoms. Then in 2022 the Phase 3 trial was stopped early for futility, unlikely to beat placebo, and the celiac program was abandoned. That failure is the honest lesson, and it doubles as a reality check on the wellness world’s favorite gut buzzword. Leaky gut, increased intestinal permeability, is real biology and a legitimate drug target, taken seriously enough to put a mechanism-specific peptide through Phase 3. But even that rigorous, safe, well-aimed drug could not clearly prove benefit, which should temper the confident claims of the supplement industry built around healing leaky gut on far less evidence. Its mechanism also still has open questions, including debate over the identity of zonulin itself.
Safety in detail
Across Phase 1 and Phase 2 trials larazotide showed a generally favorable tolerability profile as an oral, minimally absorbed peptide, with adverse events broadly comparable to placebo in the reported studies. The central limitation is efficacy, not a specific safety signal: the only Phase 3 trial was stopped for futility, so any current 'leaky gut' promotion is based on mechanism rather than proven benefit.
- As a locally acting, non-absorbed peptide, larazotide was generally well tolerated in trials.
- Its central problem is efficacy, not safety: it failed to outperform placebo in Phase 3.
- It is not approved, and its development for celiac disease was halted.
- Any consumer material would be gray-market and unverified.
Children and teenagers
Larazotide is not approved or available for anyone, having failed Phase 3, so there is no pediatric use. Pediatric celiac disease is managed with the gluten-free diet under specialist care, and leaky-gut supplement use in children is unvalidated and discouraged.
What people get wrong
Nothing recorded here yet. There is almost certainly something people get wrong about this one, and the blank space means we have not written it down, not that the record is clean.
Who profits, and who pushes back
Nobody is named here yet, because we have not done that work on this entry. Read that as unfinished. Somebody almost certainly sells this, and somebody almost certainly disputes it. Assume both until we have checked.
There is no approved-drug economy here, because larazotide failed and its developer abandoned the celiac program and moved on. Its commercial relevance is mostly as a cautionary tale next to the large, unvalidated leaky-gut supplement industry, whose confident claims its rigorous failure undercuts. Research interest persists in other barrier-injury uses.
How we got here
Larazotide is a synthetic 8-amino-acid peptide first developed as AT-1001 at Alba Therapeutics (Maryland), which studied it in celiac disease across roughly a decade and more than 800 patients. In 2016 Innovate Biopharmaceuticals licensed the full asset from Alba and renamed it INN-202, carrying it into the first-ever Phase 3 celiac trial. Innovate later became 9 Meters Biopharma, which ran the pivotal CeDLara Phase 3 and discontinued it in June 2022 after an interim futility analysis. The molecule was never approved, and its appearance on peptide-vendor and wellness sites for generic 'leaky gut' repair reflects mechanism-based marketing rather than any completed positive outcome trial.
Out of work on zonulin and tight-junction biology in celiac disease, larazotide was derived as a gut-barrier regulator and became the first celiac drug into clinical trials more than fifteen years ago. Encouraging Phase 2 data on gluten-triggered symptoms made it the front-runner, and in 2020 it became the first celiac drug to reach Phase 3. In June 2022 that trial was stopped early for futility and the celiac program was discontinued, while roughly two dozen other candidates continued and research interest shifted to other uses.
- 2000sLarazotide is derived from zonulin and tight-junction biology.
- 2000s-2010sIt becomes the first celiac drug into clinical trials.
- 2010sEncouraging Phase 2 data on gluten-triggered symptoms emerge.
- 2020It becomes the first celiac drug to reach Phase 3.
- 2022The Phase 3 trial is stopped for futility and discontinued.
The numbers behind the grade
- Type
- Tight-junction peptide (8 aa)
- Target
- Celiac disease
- Route
- Oral, non-absorbed
- Phase 3
- Failed (2022)
- Approved
- No
- Status
- Discontinued
The people taking it
Notable as the first celiac-disease drug to reach Phase 3, and as a cautionary tale after it failed there, ending years of high hopes.
Larazotide matters to people with celiac disease, the intended population still without an approved drug and reliant on the gluten-free diet, and to the celiac research and advocacy community. By contrast it also serves as a reality check for the broad leaky-gut wellness audience. The common thread is a population still waiting for a real therapy.
Developed as an oral add-on to the gluten-free diet for celiac disease, it failed its Phase 3 trial and is not in use; it has no approved consumer application.
Set against the alternatives
Against the gluten-free diet, the only accepted celiac treatment and a strict lifelong burden, larazotide aimed only to be an add-on, not a replacement or cure. Against the roughly two dozen other celiac drugs still in development, some in Phase 2, it was the front-runner whose failure left the field still searching. Against the wellness world’s leaky-gut supplements, it is the rigorous, mechanism-specific version of what they claim, and even it failed Phase 3. And against other promising-but-failed drugs, it is a textbook case of a safe, well-aimed candidate undone by late-stage efficacy testing. Its value now is as a lesson, not a therapy.
What we do not know
- Whether any celiac subgroup or symptom benefits enough to revive it.
- Why a promising Phase 2 result did not hold up in Phase 3.
- Whether the tight-junction approach to celiac disease can work at all.
What could change
Celiac pipelineRoughly two dozen other candidates continue the search for a celiac drug.Other indicationsResearch explores larazotide in other barrier-injury conditions.Zonulin scienceThe open questions about zonulin remain under study.Supplement contrastIts rigorous failure stands against the unvalidated supplement market.
Legal status
Larazotide is not approved. After becoming the first celiac drug to reach Phase 3, it failed that trial in 2022 and development was discontinued. There is no marketed product; any consumer-facing material is research-use-only.
Status current as of July 2026. Regulatory positions change, sometimes quickly.
The market for this
What follows describes how this is bought and sold. It is not a buying guide and it is not an endorsement of any seller.
There is no approved consumer route. It exists mainly as a research compound; given the limited human data, self-experimentation is not advisable.
Larazotide is not marketed and has no cost, because it is not available. The real consumer costs in this space are the gluten-free diet and the supplement industry built around leaky gut.
Not produced as an approved drug for this use; any consumer-facing material is research-use-only, typically synthesized overseas in China, with no quality assurance and frequently no certificate of analysis.
Not marketedLarazotide was discontinued for celiac and is not sold as a treatment.Research onlyMaterial exists for laboratory study, not consumer use.Separate supplement marketThe leaky-gut supplements sold online are unrelated and unvalidated.
What this entry does not yet cover
What follows is unfinished work on our side, not a finding about Larazotide Acetate.
Nothing outstanding on this one.
Sources
9 Meters discontinued the Phase 3 CeDLara larazotide trial in June 2022 after an interim analysis found completion infeasible (futility).
Phase 3 study of larazotide for celiac disease was discontinued; it was the only celiac therapeutic that had reached Phase 3.
9 Meters shares fell sharply as the Phase 3 celiac trial of larazotide was discontinued at interim analysis in 2022.
Phase 3 larazotide flopped; 9 Meters signaled it may pull the trial after disappointing results.
In a Phase 2 trial of 342 adults, the 0.5 mg larazotide dose was associated with fewer symptomatic days versus placebo; dose response was non-linear.
Am J Physiol Gastrointest Liver Physiol (review, PubMed 33881350)
Larazotide acetate is a synthetic 8-amino-acid tight junction regulator acting as a zonulin antagonist to limit gliadin-induced paracellular permeability.
Systematic review and meta-analysis of larazotide RCTs in celiac disease found variable, dose-dependent effects across trials.
Innovate Biopharmaceuticals licensed larazotide from Alba Therapeutics and renamed it INN-202, advancing toward Phase 3; the asset carried FDA Fast Track designation.
Alba Therapeutics developed larazotide acetate (AT-1001) over roughly a decade, studying it in more than 800 celiac patients before out-licensing.
Larazotide development timeline and 2022 Phase 3 discontinuation; alternative names AT-1001 and larazotide acetate.
The studies that matter
Phase 2 trial2010s
Larazotide reduced persistent celiac symptoms in patients already on a gluten-free diet, an encouraging result that advanced it to Phase 3.
Phase 3 trial (CedLara)2022
The first celiac drug ever to reach Phase 3 failed: an interim analysis found no meaningful effect, and the 525-patient trial was discontinued.
Aftermath2022 onward
The developer pivoted away from larazotide, adding it to what observers call the graveyard of failed celiac drugs.