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Larazotide
Larazotide acetate, AT-1001, INN-202; zonulin-pathway (tight-junction) antagonist
Larazotide is a synthetic, orally administered octapeptide that acts locally in the gut lumen as a tight-junction regulator. It antagonizes the zonulin signaling pathway, which physiologically loosens the tight junctions between intestinal epithelial cells and increases paracellular permeability. In celiac disease, gliadin peptides are thought to trigger zonulin release and junctional opening, allowing more gluten fragments to cross the epithelium and drive immune activation. By promoting tight-junction assembly and reducing gliadin-induced permeability and cytoskeletal rearrangement, larazotide is designed to limit the amount of immunogenic gluten reaching the lamina propria and thereby dampen downstream inflammation. It is minimally absorbed, so its action is confined to the intestinal surface rather than systemic.
Larazotide is investigational and has never been approved. Early randomized trials tested it during gluten challenge: Kelly et al. (2013) evaluated its effect on gluten-induced permeability and symptoms. A larger phase 2b trial (Leffler et al., Gastroenterology 2015) in patients with persistent symptoms despite a gluten-free diet found that the lowest dose (0.5 mg three times daily) improved symptoms, while higher doses did not — an unusual inverse dose-response. A subsequent phase 3 program (CeD-2001) in non-responsive celiac disease was discontinued after an interim analysis for futility, and no marketing application succeeded.
- Investigated as an adjunct to a gluten-free diet in celiac disease with persistent symptoms
- Research tool for intestinal tight-junction and paracellular-permeability ('leaky gut') studies
- Exploratory research in other conditions involving intestinal barrier dysfunction
- Mechanistic study of the zonulin pathway in mucosal immunology
Educational overview only — no dosing instructions in the public hub.
No approved product exists, and pivotal phase 3 efficacy was not demonstrated (the trial stopped for futility), so a favorable benefit-risk profile in celiac disease has not been established. In trials the drug was generally well tolerated with mostly mild gastrointestinal adverse events, but long-term safety data are limited. For non-pharmaceutical 'research use only' material, the dominant practical risks are unverified identity, purity, and endotoxin content, and there is no clinical evidence supporting self-directed use.
Larazotide sold outside clinical research is a research-use-only material with no pharmaceutical quality assurance. A third-party certificate of analysis documenting identity, purity (HPLC), quantification, and mass-spectrometry confirmation is the minimum verification; it does not establish sterility, potency consistency, or fitness for human use. Clinical-trial larazotide acetate was produced under controlled pharmaceutical conditions that gray-market material cannot be assumed to match.
Investigational only; larazotide never received marketing approval from any regulator (FDA, EMA, MHRA) for any indication, and its late-stage celiac disease program was discontinued. Products sold 'for research use only' are not authorized for human use.
Frequently asked questions
- What is Larazotide used for?
- Investigated as an adjunct to a gluten-free diet in celiac disease with persistent symptoms. Research tool for intestinal tight-junction and paracellular-permeability ('leaky gut') studies. Exploratory research in other conditions involving intestinal barrier dysfunction. Mechanistic study of the zonulin pathway in mucosal immunology. Larazotide is investigational and has never been approved. Early randomized trials tested it during gluten challenge: Kelly et al. (2013) evaluated its effect on gluten-induced permeability and symptoms. A larger phase 2b trial (Leffler et al., Gastroenterology 2015) in patients with persistent symptoms despite a gluten-free diet found that the lowest dose (0.5 mg three times daily) improved symptoms, while higher doses did not — an unusual inverse dose-response. A subsequent phase 3 program (CeD-2001) in non-responsive celiac disease was discontinued after an interim analysis for futility, and no marketing application succeeded.
- Is Larazotide legal in Europe?
- Investigational only; larazotide never received marketing approval from any regulator (FDA, EMA, MHRA) for any indication, and its late-stage celiac disease program was discontinued. Products sold 'for research use only' are not authorized for human use.
- What are the risks and side effects of Larazotide?
- No approved product exists, and pivotal phase 3 efficacy was not demonstrated (the trial stopped for futility), so a favorable benefit-risk profile in celiac disease has not been established. In trials the drug was generally well tolerated with mostly mild gastrointestinal adverse events, but long-term safety data are limited. For non-pharmaceutical 'research use only' material, the dominant practical risks are unverified identity, purity, and endotoxin content, and there is no clinical evidence supporting self-directed use.
- How is the quality of Larazotide assessed?
- Larazotide sold outside clinical research is a research-use-only material with no pharmaceutical quality assurance. A third-party certificate of analysis documenting identity, purity (HPLC), quantification, and mass-spectrometry confirmation is the minimum verification; it does not establish sterility, potency consistency, or fitness for human use. Clinical-trial larazotide acetate was produced under controlled pharmaceutical conditions that gray-market material cannot be assumed to match.