The Gut-Barrier Drug You Cannot Buy
Larazotide acetate
Also known as INN-202 · AT-1001 (ambiguous, see the record)
At a glance
- What it is
- Zonulin receptor antagonist. Phase 3 terminated early; not purchasable.
- Evidence
- Clinical trialsHow the tiers workLarazotide has real trial data and no marketable result. Why this tier
- Half-life
- Not established in available literature
- Routes
- Oral
- Category
- Healing
- WADA
- We do not state a status
- Amino acids
- 8
Putting Larazotide acetate on a schedule, with the vial it comes from and a log of each dose, happens in the app: Claritide for iPhone.
Why this tier
Larazotide has real trial data and no marketable result. Its Phase 3 coeliac trial, CeDLara (NCT03569007, 307 enrolled, primary outcome the proportion of binary responders on the coeliac disease patient-reported abdominal domain at 12 weeks), is listed as TERMINATED with the reason on record given as "Trial terminated by Sponsor", primary completion 21 July 2022, and no results posted. Say discontinued early by the sponsor after a futility interim analysis, results never published. Do not say it missed its primary endpoint. A terminated-for-futility trial produces no efficacy readout at all, and presenting a sponsor termination as a clean published negative result is its own kind of overstatement. An earlier meta-analysis of randomised trials concluded larazotide is safe and superior to placebo for gastrointestinal symptoms during gluten challenge.
What it is
Larazotide acetate is an oral, locally acting octapeptide that blocks the zonulin receptor, the signal that opens the tight junctions between intestinal cells. It is the drug people mean when they say "leaky gut" has a pharmacological answer. Its Phase 3 coeliac trial was terminated by the sponsor and no results were ever published. A Phase 2 in long COVID at Massachusetts General Hospital is the live programme.
How it works
The cells lining your gut are stitched together by tight junctions, and how open those junctions sit is regulated rather than fixed. Zonulin is the human protein that signals them to loosen. Larazotide is a synthetic eight-amino-acid peptide that antagonises the zonulin receptor, blocking that opening signal and letting the proteins holding the gates shut rearrange back into place. It is deliberately non-systemic: it acts in the gut lumen and is not designed to be absorbed, which is unusual and is why it is formulated as enteric-coated beads in a capsule. No other gut compound in this library works this way: BPC-157 and KPV both act on inflammation and repair signalling, not on the barrier architecture itself.
Commonly researched ranges
- Phase 3 investigational dose (CeDLara)0.25–0.5 mg
The doses used in NCT03569007 against matching placebo. The earlier Phase 2b programme identified 0.5 mg three times daily as the effective dose. These are investigational doses from a discontinued programme, not a protocol, and larazotide is not available to buy.
| Phase | Amount | Frequency | Timing | Note |
|---|---|---|---|---|
| Phase 3 investigational dose (CeDLara) | 0.25–0.5 mg | Three times daily | Not established in available literature | The doses used in NCT03569007 against matching placebo. The earlier Phase 2b programme identified 0.5 mg three times daily as the effective dose. These are investigational doses from a discontinued programme, not a protocol, and larazotide is not available to buy. |
- Cycle guidance
- Not applicable. Larazotide is an investigational drug administered inside clinical trials, on trial schedules.
- Goals
- Gut
Where this sits with the FDA
Larazotide is investigational and not on any FDA compounding list. Users cannot buy it, which is worth saying out loud: "larazotide" is name-dropped constantly in leaky-gut content and appears in research kits alongside compounds that genuinely are available.
Primary sourceWADA status
Not named on the 2026 Prohibited List. We could not determine whether the S0 catch-all applies and do not state a status.
We looked and could not resolve it. This is not the same as "not prohibited". Treat it as unresolved and check with your federation before competing.
There is nothing to mix
Not applicable. None of the published routes for this compound take a diluent, so there is no concentration to calculate and no beyond-use window to track.
Week by week
Not established in available literature.
Side effects
Not established in available literature. Absence from this page does not mean absence of risk. It means our sources publish no side-effect profile for Larazotide acetate.
Contraindications and interactions
Do not use if
Not established in available literature.
Interactions
Not established in available literature.
Absence from this list does NOT mean safety. It means lack of research.
Storage and cost
- Storage
- An oral capsule in the trial formulation. There is no diluent, no concentration and no beyond-use window to track.
- Cost
- Not established in available literature
Stacks with
Larazotide acetate in full
Why this record exists
Larazotide is the compound named whenever someone wants "leaky gut" to sound pharmacological rather than vague. It has a specific, checkable mechanism and real registered trials. It is also unbuyable, and its flagship trial ended without a result. Both halves belong on the same page.
The mechanism, and why it is genuinely different
The cells lining the intestine are joined by tight junctions, and how tightly those junctions sit is actively regulated. Zonulin is the human protein that signals them to loosen, a real, measurable mechanism, not a metaphor.
Larazotide is a synthetic eight-amino-acid peptide that antagonises the zonulin receptor. Blocking that signal lets the junction proteins reassemble. It is deliberately non-systemic: it acts inside the gut lumen and is not designed to be absorbed, which is why it comes as enteric-coated beads inside a capsule and why it has no meaningful half-life to publish.
Nothing else in this library works on the barrier itself. BPC-157 and KPV both act on inflammation and repair signalling downstream of it.
The negative-evidence teaching case, stated precisely
The Phase 3 trial was CeDLara, NCT03569007, sponsored by 9 Meters Biopharma, in coeliac disease. Primary outcome: the proportion of binary responders on the coeliac disease patient-reported outcome abdominal domain at 12 weeks. Actual enrolment 307. Status on the registry: TERMINATED. Reason on record: "Trial terminated by Sponsor". Primary completion 21 July 2022. No results posted.
Here is the distinction that matters and that almost every write-up gets wrong: this is not the same as missing a primary endpoint.
A trial that is stopped early for futility does not produce an efficacy readout. There is no p-value, no effect size, no published comparison. Presenting a sponsor termination as a clean negative result implies a rigour that does not exist in the record, and doing that in the negative direction is the same failure as doing it in the positive direction. What we can say is: discontinued early by the sponsor after a futility interim analysis, results never published.
The reason cited in secondary reporting is that the interim analysis found the required treatment-group size too large to support continuation. That page is no longer reachable, so treat the reason as partial. The termination is verified on the registry itself.
What is still running
NCT05747534 · "AT1001 for the Treatment of Long COVID", Phase 2, lead sponsor Massachusetts General Hospital with Boston Children's. Larazotide orally four times daily against matching placebo, 107 participants actual, start 31 May 2023, status ACTIVENOTRECRUITING as of May 2026, estimated primary completion 5 June 2026 and estimated overall completion 30 September 2026. Primary outcomes are adverse-event profiling and time to symptom resolution at 8 weeks. The registry rationale cites earlier work in multisystem inflammatory syndrome in children under an emergency IND.
That readout has either just landed or is about to. It is the single most informative thing that will happen to this compound in the near term.
The earlier positive signal
A systematic review and meta-analysis of randomised trials concluded that larazotide is safe and superior to placebo in alleviating gastrointestinal symptoms among patients undergoing gluten challenge. That is a narrower claim than "treats coeliac disease", since gluten challenge is a controlled provocation rather than everyday exposure, but it is a real positive finding from controlled work.
The alias problem
Carry AT-1001 only with a warning attached. AT-1001 is also Amicus Therapeutics' internal code for migalastat, marketed as Galafold for Fabry disease. A trial-registry search on that alias returns predominantly migalastat studies. Anyone indexing evidence on the alias will pull the wrong compound's literature, and it happens often enough that it is worth naming.
What we do not publish
Side effects and contraindications are null on this record. We did not extract them from the trial documents in this pass, and inventing a plausible list for an investigational drug would be worse than an empty one.
Sources
- 1NCT03569007 · CeDLara, Phase 3 larazotide in coeliac disease, TERMINATED, no results posted
- 2NCT05747534 · AT1001 for the treatment of long COVID, Phase 2, Massachusetts General Hospital, ACTIVE_NOT_RECRUITING
- 3Systematic review and meta-analysis of larazotide RCTs in gluten challenge
Every record in this library is free to read, and it stays free. Your own schedule, vials and log live in the app: Claritide for iPhone.