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N-Acetyl Larazotide

Larazotide Acetate · AT-1001

C
Animal replicated
Research chemicalTight Junction RegulatorZonulin AntagonistPeptide
RouteOralGray-market only
C
Evidence grade: Animal replicated

Effect demonstrated in multiple animal studies; human data sparse or extrapolated. Grades summarize evidence quality, not whether a compound is appropriate, legal, or risk-free.

At a glance
What it is
Larazotide Acetate / AT-1001 Derivative — Zonulin Antagonist — Tight Junction Regulator — Gut Permeability — Tight Junction Regulator, Zonulin Antagonist, Peptide.
Why people use it
Used primarily for tissue repair and healing and gut health.
What the evidence supports
Competitive zonulin antagonism; prevents TJ opening; blocks paracellular permeability increase
If you only read one thing

Larazotide acetate completed four Phase 2 randomized controlled trials and entered Phase 3 as the first pharmacological agent for celiac disease. The Phase 2 data was positive: significantly reduced GI symptoms vs placebo during gluten challenge; well-tolerated; no safety signal. The Phase 3 trial found symptom improvement but failed to demonstrate improvement in the primary endpoint of intestinal barrier integrity. 9 Meters Biopharma discontinued the program in 2022. The compound that was supposed to be precision gut-barrier therapy didn't demonstrate the barrier mechanism it was built on — at least not at the measured endpoint in the Phase 3 design. The community now uses N-acetyl larazotide from Limitless for the leaky gut applications that were the clinical rationale for developing the drug. The evidence for these community applications is the Phase 2 symptom data, not a validated barrier restoration claim.

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Route / form

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Evidence fit
Route-specific

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Route caveat
Protocol not standardized

No route-matched protocol rows were parsed for this form; use the route notes and full dosing chapter before comparing options.

Protocol anchor
Full dosing section

Open the full report at the dosing chapter for protocol rows, cycle context, and administration notes.

Typical dose snapshot
See route notes
Evidence varies by use case
Published literature
2human RCTs0human studies0animal0in vitro
Evidence reality check
Human evidence
2 human studies
2 randomized; 0 observational.
Preclinical base
0 lab signals
0 animal; 0 in-vitro/mechanistic.
Evidence snapshot
Competitive zonulin antagonism; prevents TJ opening; blocks paracellular permeability increase
From the chapter quick-reference block.
Categories
Healing & RecoveryGut & DigestiveImmune & Thymic
Properties
✓ Human RCTSingle-lab provenanceNot injectable
Evidence
CAnimal replicated
The Origin — Vibrio Cholerae to Celiac Drug
Larazotide acetate was derived from the zonula occludens toxin (Zot) of Vibrio cholerae — the bacterium that causes cholera. Zot disrupts intestinal tight junctions to enable cholera toxin absorption. Alessio Fasano's group at Harvard identified an 8-amino acid sequence within the Zot structure that corresponds to the human zonulin protein's receptor-binding region. This sequence, rather than opening tight junctions like the full Zot toxin, actually competes with zonulin at its receptor and blocks tight junction opening. The blocking sequence became larazotide.
The Clinical Evidence Summary
4 Phase 2 RCTs (n=626 total; meta-analysis): larazotide acetate superior to placebo for gastrointestinal symptom reduction during gluten challenge in celiac disease; well-tolerated; no significant safety signal. Phase 3 (NCT03569007; 9 Meters Biopharma): DISCONTINUED in 2022 — led to symptom improvement but failed to improve barrier integrity on the primary endpoint. Program discontinued. Not FDA-approved. The compound improved symptoms without demonstrating the tight junction integrity improvement that was the pharmacological rationale.
vs BPC-157 and KPV in Gut Healing
BPC-157 (oral): rebuilds gut mucosa structurally — VEGF angiogenesis, mucosal cell proliferation, tight junction upregulation. KPV: suppresses inflammatory signaling (NF-kB, COX-2, mast cells). N-Acetyl Larazotide: specifically blocks zonulin-mediated paracellular permeability increase. Three different mechanisms at the intestinal barrier; potentially complementary. N-Acetyl Larazotide is the most targeted and specific of the three for the permeability mechanism but has the narrowest evidence base for community use.
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Gut Peptide Stack
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Shared goal · gut

Scope appropriateness is the question: local gut peptides are being stacked for barrier integrity and inflammatory signaling, not for systemic regeneration claims.

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