Informational only. Not medical advice.INFORMATIONAL PLATFORM ONLY — NOT MEDICAL ADVICE, DIAGNOSIS, OR TREATMENT
Larazotide is a synthetic linear octapeptide (Gly-Gly-Val-Leu-Val-Gln-Pro-Gly) structurally derived from the Vibrio cholerae zonula occludens toxin. It is proposed to act on the zonulin/tight-junction signaling pathway, interrupting gliadin-triggered intestinal barrier disruption by preserving tight-junction integrity locally in the gut lumen. Larazotide has been studied in multiple human trials for celiac disease under the development codes AT-1001, INN-202, and SPD550, but has never received FDA or EMA approval; a Phase 3 trial (NCT03569007) was terminated by the sponsor in 2022 with no results posted. It is not systemically absorbed and is available only as a research chemical.
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Kimera Chems has the lowest single-vial Larazotide price at $2.57/mg among 1 COA-verified vendor on Disclosed Labs. Bulk or multi-vial deals may be lower.
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Research-grade Larazotide is listed at $2.57/mg from 1 verified source on Disclosed Labs.
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Larazotide has been studied in multiple completed human trials for celiac disease but has never received FDA or EMA approval. A Phase 1 single-dose study (Paterson et al. 2007, PMID 17697209) confirmed no systemic absorption. Phase 2 gluten-challenge trials (Leffler et al. 2012, PMID 22825365, n=86, doses 0.25/1/4/8 mg TID) did not meet the primary endpoint (intestinal permeability) due to high variability, though lower doses limited symptom worsening. A Phase 2b trial (Leffler et al. 2015, PMID 25683116, ~342 patients, no gluten challenge) met its primary endpoint at the 0.5 mg TID dose, showing symptom improvement versus placebo with an inverse dose-response. The Phase 3 CeDLara trial (NCT03569007, 307 patients, 0.25 mg and 0.5 mg TID) was terminated by the sponsor in 2022 for futility/impractically large required sample size, with no results posted. Across trials, no serious drug-related adverse events or hepatic/renal/bone toxicity signals were reported; headache and urinary tract infection were the most common adverse events without consistent excess versus placebo. In preclinical models, larazotide reduced gliadin-induced paracellular permeability and preserved tight-junction protein localization in Caco-2 human intestinal cell monolayers, prevented gliadin-induced permeability increases and reduced macrophage infiltration in HLA-DQ8 transgenic mice, and accelerated barrier recovery in a porcine jejunum ischemia-reperfusion injury model.
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The potential utility of tight junction regulation in celiac disease: focus on larazotide acetate
2016
The safety, tolerance, pharmacokinetic and pharmacodynamic effects of single doses of AT-1001 in coeliac disease subjects: a proof of concept study
2007
A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge
Prices verified as of July 2026. Actual prices may vary. For research use only.
2012