Research compounds
Larazotide acetate
AT-1001, INN-202
Larazotide acetate is an eight-amino-acid peptide developed as a tight junction regulator for coeliac disease, taken orally and acting locally in the gut lumen. Its Phase 3 trial was halted for futility in 2022 and it is not approved.
Also known as: AT-1001, AT1001, INN-202, larazotide
- Status
- Larazotide acetate is a research compound and not approved by the FDA for human use.
- Evidence
- Human trials. Published clinical trials in people report results.
- Half-life
- Not systemically absorbed to a meaningful extent; acts locally in the intestinal lumen.
- How it's taken
- Oral capsule taken before meals (investigational)
- Mechanism
- Tissue repair
How Larazotide acetate works
Gliadin exposure in coeliac disease triggers release of zonulin, which loosens intestinal epithelial tight junctions and increases paracellular permeability, allowing more gliadin peptides to reach the lamina propria. Larazotide is a zonulin antagonist intended to keep tight junctions closed, reducing that permeability and interrupting the amplification loop. It is not absorbed and acts within the intestinal lumen.
What research has looked at
- Earlier Phase 2 trials reported reduction in symptoms in patients with coeliac disease who remained symptomatic despite a gluten-free diet — the population it was aimed at.
- A luminal, non-absorbed mechanism means systemic exposure is minimal.
- It was the most advanced candidate in coeliac disease and reached Phase 3, which few therapies in the indication have.
Evidence level: Human trials. Published clinical trials in people report results. These are areas studied or reported, not promised effects.
Reported side effects and risks
- The pivotal Phase 3 trial was stopped after an interim analysis for futility — it did not demonstrate benefit on its primary endpoint. This is the single most important fact about the compound and outweighs the earlier Phase 2 signals.
- No regulator has approved it for any indication.
- Reported adverse events in trials were generally mild and included headache, nasopharyngitis, abdominal pain and flatulence.
- The broader "leaky gut" claims made for zonulin-targeting compounds in consumer contexts substantially outrun the evidence, which is confined to coeliac disease and was negative in Phase 3.
Sources
- PubMed research on larazotide zonulin coeliac Phase 3 · NIH · National Library of Medicine
- DrugBank record for larazotide · DrugBank
- Active clinical trials for larazotide · U.S. National Library of Medicine
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Related compounds
Larazotide acetate FAQ
What is Larazotide acetate?
Larazotide acetate is an eight-amino-acid peptide developed as a tight junction regulator for coeliac disease, taken orally and acting locally in the gut lumen. Its Phase 3 trial was halted for futility in 2022 and it is not approved.
How does Larazotide acetate work?
Gliadin exposure in coeliac disease triggers release of zonulin, which loosens intestinal epithelial tight junctions and increases paracellular permeability, allowing more gliadin peptides to reach the lamina propria. Larazotide is a zonulin antagonist intended to keep tight junctions closed, reducing that permeability and interrupting the amplification loop. It is not absorbed and acts within the intestinal lumen.
Is Larazotide acetate FDA approved?
No. Larazotide acetate is a research compound and not approved by the FDA for human use. Evidence level: human trials. Published clinical trials in people report results.
What is the half-life of Larazotide acetate?
Reported half-life: Not systemically absorbed to a meaningful extent; acts locally in the intestinal lumen.
How is Larazotide acetate taken?
Oral capsule taken before meals (investigational).
What side effects have been reported with Larazotide acetate?
Reported in the sources: The pivotal Phase 3 trial was stopped after an interim analysis for futility — it did not demonstrate benefit on its primary endpoint. This is the single most important fact about the compound and outweighs the earlier Phase 2 signals; No regulator has approved it for any indication; Reported adverse events in trials were generally mild and included headache, nasopharyngitis, abdominal pain and flatulence; The broader "leaky gut" claims made for zonulin-targeting compounds in consumer contexts substantially outrun the evidence, which is confined to coeliac disease and was negative in Phase 3.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.