Digestive & weight Zonulin antagonist (tight-junction regulator)
Larazotide acetate
Regulatory status
Status at a glance
503A compounding status
Not nominated
We found no pending nomination for the 503A bulks list. Unless the substance has another legal pathway (for example, a USP monograph or use in an FDA-approved drug), 503A pharmacies generally may not compound with it.
- FDA approval
- Not FDA-approved for any use
- 503B outsourcing
- Not determined
- Anti-doping (WADA)
- Not on the WADA Prohibited List
- DEA schedule
- Not a controlled substance
About peptide status
Most peptides discussed here are not FDA-approved for any use, and products labeled “research use only” are not for human use. Removal from Category 2 does not authorize compounding. PCAC votes are non-binding recommendations; FDA and HHS make the final decisions.
This is not medical or legal advice, and we do not publish dosing, sourcing or reconstitution information. Talk with a licensed clinician before using any peptide.
If you think you are having a medical emergency, call 911.
Key takeaway
Larazotide acetate is an investigational oral peptide that was studied as an add-on to the gluten-free diet for celiac disease, intended to tighten the junctions between intestinal cells. Its pivotal Phase 3 trial was stopped for futility, and pooled trial data did not show an effect on a key measure of intestinal permeability. As of 2026, it is not approved and its lead program has been halted.
At a glance
- FDA status
- Investigational peptide, not approved by the FDA
- Studied for
- Oral add-on to the gluten-free diet for celiac disease
- Phase 3 result
- Trial (CeDLara) stopped for futility and did not meet its endpoint
- Pooled data
- No effect on the intestinal permeability measure
- Evidence strength
- Low research
Summary
Larazotide acetate is an investigational peptide studied for celiac disease. Its Phase 3 trial was stopped for futility and it is not approved.
What is larazotide acetate?
Larazotide acetate is an experimental peptide of eight amino acids, taken by mouth, studied as an adjunct to the gluten-free diet in celiac disease, an autoimmune reaction to gluten that damages the small intestine. It was most recently developed by 9 Meters Biopharma under the code AT-1001. It is investigational, is not approved, and its lead development program has been discontinued.
How does it work?
Larazotide was designed to act as a "tight-junction regulator." The intestinal lining has junctions between cells that control what passes through; in celiac disease these are thought to loosen, letting gluten fragments cross and trigger inflammation.
Larazotide was proposed to counter the hormone zonulin and promote closure of these junctions, reducing the leakage. This is the proposed mechanism; as the trials below show, it did not translate into a confirmed clinical benefit.
Is it FDA-approved?
Safety note
Status: Investigational peptide, not approved by the FDA
Category: In clinical trials · Primary body area: Digestive & weight
No. Larazotide acetate is investigational and not approved. Its pivotal Phase 3 trial was discontinued, and there is no active late-stage program.
What does the research show?
Editor’s note
Evidence strength: Low research (1 human · 0 animal/cell studies)
Its pivotal Phase 3 was stopped for futility and pooled trial data show no effect on the permeability endpoint, so there is no sound human evidence that it works.
The decisive evidence is negative, as the two main human analyses show:
| Evidence | Design | Result |
|---|---|---|
| Phase 3 CeDLara trial | Interim analysis in 2022 against a primary endpoint of reducing celiac symptom severity | Stopped for futility after the analysis indicated it would not meet that endpoint |
| Meta-analysis indexed on PubMed | 4 randomized trials | No significant effect on the lactulose-to-mannitol permeability ratio, a biological measure of gut leakiness, with only inconsistent symptom signals in gluten-challenge subgroups |
A mechanistic review describes the intended tight-junction pathway. Overall, the human evidence does not support a benefit.
Sources: a meta-analysis of larazotide trials (Hoilat et al., Clinics and Research in Hepatology and Gastroenterology, 2022, DOI: 10.1016/j.clinre.2021.101782) and a mechanistic review (Slifer et al., American Journal of Physiology: Gastrointestinal and Liver Physiology, 2021, DOI: 10.1152/ajpgi.00386.2020), both indexed on PubMed; and reporting on the Phase 3 discontinuation. This document is educational, is not medical advice or a health claim, and is not an offer to sell any product.
Registered human trials
1 registered human trial on ClinicalTrials.gov that we reviewed
Sources
- [1]
- [2]
- [3]
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