Larazotide Acetate
AT-1001 · INN-202
A tight-junction regulator studied in human celiac trials for intestinal barrier integrity.
Class
Tight-junction regulator / zonulin antagonist
Half-life
Short; acts locally in the gut lumen
Evidence
Randomized human trials
Randomized human trials
Supported by randomized controlled trials in humans. Several compounds at this level are FDA-approved for specific indications.
Overview
Larazotide is unusual in this category for actually reaching phase 3 human trials. It is an orally administered peptide that acts locally in the intestine to tighten the junctions between gut-lining cells — the mechanism behind 'leaky gut' when those junctions loosen.
It works by antagonising zonulin, a protein that regulates intestinal permeability. In celiac disease, gluten triggers zonulin release and barrier breakdown; larazotide was studied as an add-on to a gluten-free diet to reduce residual symptoms.
Its phase 3 celiac trial (CeD-002) did not meet its primary endpoint, and development stalled, but the human data on its barrier-tightening mechanism is more than almost anything else in the repair category. It is not approved, and it is being discussed here for gut-barrier support with that caveat.
How it works
- Antagonises zonulin-mediated opening of intestinal tight junctions.
- Reduces paracellular permeability ('leaky gut') in the small intestine.
- Acts locally in the gut lumen with minimal systemic absorption.
- Reduces the inflammatory cascade triggered by antigen passage across a compromised barrier.
What the research shows
Researched effects
- Reduced intestinal permeability in celiac patients in phase 2 trials
- Reduced symptom scores as an adjunct to gluten-free diet in some phase 2 endpoints
- Well-characterised human safety profile from multiple trials
- Did not meet the primary endpoint in its phase 3 celiac trial
Limitations & what it won't do
- Phase 3 primary endpoint was not met; not approved.
- Studied specifically in celiac disease — broader 'leaky gut' benefit is extrapolation.
- Must be taken before meals; timing-dependent.
Dosing protocols
These ranges reflect published trials and community protocols. They are reference information, not a prescription. Doses are per injection unless noted.
Trial dosing (celiac, reference)
0.5 mg (500 mcg)The trial dose was 0.5 mg three times daily before meals. Higher doses were not more effective in studies.
Administration
Not an injectable reconstitution compound
Side effects
Common
- Generally well tolerated in trials
- Occasional GI symptoms comparable to placebo
Serious / rare
- No significant safety signals in human trials
Contraindications & interactions
Do not use if you have
- Pregnant, breastfeeding, or trying to conceive
No pregnancy safety data.
What to monitor
- GI symptom response
Commonly combined with
References
- Leffler DA et al. — Larazotide acetate for persistent symptoms of celiac diseaseGastroenterology 2015;148:1311-1319
Research & educational information only — not medical advice.
You must be 18 or older to use this site. The peptides described are presented as research chemicals intended for research purposes only. Most are not approved by the FDA for human use. Dosing ranges reflect what has appeared in the scientific literature or community protocols and are not prescriptions. Nothing here replaces evaluation by a licensed physician who knows your full medical history.
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