Larazotide Acetate
Limited human dataAlso known as: AT-1001 · zonulin-antagonist peptide
A first-in-class oral peptide designed to keep intestinal tight junctions closed, studied as an adjunct therapy for celiac disease alongside a gluten-free diet. One of the more rigorously trialed gut-health peptides, with multiple completed phase 2 RCTs.
Mechanism (plain language)
Acts locally in the gut lumen (not absorbed systemically at meaningful levels) to inhibit tight-junction opening, aiming to reduce paracellular passage of gluten peptides into the intestinal lining that triggers immune activation in celiac disease.
What research suggests
Multiple randomized, placebo-controlled trials during gluten challenge report reduced gluten-induced gastrointestinal symptoms and lower antibody responses at some doses, though the primary permeability biomarker (lactulose/mannitol ratio) has not consistently differed from placebo across trials.
Uncertainties & risks
Results are mixed across the four completed RCTs, with a systematic review noting symptom benefit during gluten challenge but no consistent effect on the core permeability endpoint. Not FDA-approved; not a substitute for a gluten-free diet in celiac disease, and there's no meaningful evidence for use in healthy people without celiac disease.
Primary sources
Secondary citations for verification. Prefer the STACKD summary above for context before opening these.
- Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study
2013 · human
Reduced gluten-induced symptoms and lower anti-tTG antibody rise versus placebo at the 1 mg dose during gluten challenge.
- Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials
2021 · review
Pooled analysis of 4 RCTs found symptomatic benefit during gluten challenge but no consistent effect on intestinal permeability.