Larazotide
Also known as: AT-1001, Larazotide acetate
Larazotide is a synthetic octapeptide that blocks zonulin-mediated intestinal permeability, specifically designed to treat celiac disease by preventing gluten-induced tight junction disruption. This peptide works by inhibiting the MyD88-dependent pathway that leads to increased intestinal permeability.
Larazotide is a 879.05 g/mol research peptide. Larazotide is a synthetic octapeptide that blocks zonulin-mediated intestinal permeability, specifically designed to treat celiac disease by preventing gluten-induced tight junction disruption. This peptide works by inhibiting the MyD88-dependent pathway that leads to increased intestinal permeability.
Also called: AT-1001, Larazotide acetate
879.05 g/mol
Molecular Weight
Daltons
0
Strong Evidence
benefits
3
Studies Cited
peer-reviewed
1-4
Typical Dose
mg
Overview
Larazotide represents a targeted therapeutic approach for celiac disease management through its unique mechanism of tight junction regulation. The peptide functions as a zonulin receptor antagonist, binding to CXCR3 chemokine receptors and blocking the cascade of events that normally leads to intestinal barrier dysfunction when gluten peptides trigger zonulin release. Clinical development has focused on its ability to reduce symptoms and intestinal damage in celiac patients who experience inadvertent gluten exposure despite maintaining a strict gluten-free diet. The peptide's structure allows it to resist degradation in the harsh gastrointestinal environment while maintaining its biological activity at the intestinal epithelium.
Key Takeaways: Larazotide
- Research doses typically range from 1 to 4 mg via oral
- 0 benefits with strong evidence, 3 moderate, 3 preliminary
- Half-life: 2-3 hours (oral administration)
- 3 cited research studies in this guide
Mechanism of Action
Larazotide functions as a competitive antagonist of zonulin at CXCR3 receptors on intestinal epithelial cells. When gliadin peptides trigger zonulin release, larazotide prevents zonulin binding and subsequent activation of the MyD88-dependent signaling pathway. This blockade prevents the phosphorylation cascade that leads to tight junction protein disassembly, maintaining intestinal barrier integrity and preventing the increased permeability that characterizes celiac disease pathophysiology.
Research Benefits
Larazotide at a Glance
Larazotide functions as a competitive antagonist of zonulin at CXCR3 receptors on intestinal epithelial cells.
Intestinal Barrier Protection
Moderate EvidencePrevents zonulin-mediated tight junction opening, maintaining intestinal barrier function during gluten exposure by blocking CXCR3 receptor activation
Celiac Symptom Reduction
Moderate EvidenceReduces gastrointestinal symptoms including abdominal pain, bloating, and diarrhea in celiac patients experiencing inadvertent gluten exposure
Lactulose/Mannitol Ratio Improvement
Moderate EvidenceNormalizes intestinal permeability as measured by lactulose/mannitol excretion ratios, indicating restored tight junction function
Villous Architecture Preservation
PreliminaryHelps maintain small intestinal villous height and crypt depth ratios by preventing gluten-induced inflammatory damage to the intestinal mucosa
Inflammatory Marker Reduction
PreliminaryDecreases pro-inflammatory cytokine production including TNF-α, IL-15, and interferon-γ in response to gluten peptide exposure
Quality of Life Enhancement
PreliminaryImproves patient-reported outcomes and reduces anxiety around inadvertent gluten exposure in individuals with celiac disease
Research Dosing Protocols
Research Purposes Only: All content is for informational and research purposes only. This site does not provide medical advice, diagnosis, or treatment. Consult a qualified healthcare professional before using any peptide or supplement.
| Research Protocol | Dose Range | Route |
|---|---|---|
| Celiac disease management | 1–4 mg | oral |
| Intestinal permeability studies | 0.25–2 mg | oral |
| Gluten challenge protocols | 2–8 mg | oral |
Frequency
Three times daily with meals
Timing
Administer 30-60 minutes before meals to maximize protective effect
Cycle Length
Continuous use during study periods (typically 12-24 weeks)
Research Notes
- 1Most effective when taken before anticipated gluten exposure
- 2Requires consistent dosing schedule for optimal barrier protection
- 3Should be taken with adequate water to ensure proper dissolution
- 4Research protocols often include gluten challenge testing
Reconstitution Guide
Standard Reconstitution
Vial Size
0 mg
Bacteriostatic Water
0 mL
Concentration
NaN mcg
per 0.1 mL (10 units)
Step-by-Step Guide
Gather Materials
Larazotide vial, bacteriostatic water, alcohol swabs, insulin syringes.
Equilibrate Temperature
Remove the vial from storage and allow it to reach room temperature (5-10 minutes).
Sanitize
Swab the rubber stopper of both the peptide vial and bacteriostatic water vial with alcohol.
Draw Water
Draw 0 mL of bacteriostatic water into a syringe.
Add Water to Vial
Insert the needle into the peptide vial and direct the water stream against the glass wall — not directly onto the powder.
Mix Gently
Swirl the vial gently until the powder is fully dissolved. Never shake. The solution should be clear and colorless.
Store Properly
Refrigerate at Room temperature (stable in solid form). 24 months when stored properly.
Storage Temperature
Room temperature (stable in solid form)
Shelf Life
24 months when stored properly
Important Notes
- •Available as oral capsules - no reconstitution required
- •Store in dry conditions away from moisture
- •Protect from excessive heat and light exposure
Larazotide Dosing Calculator
Calculate daily intake, cycle totals, and vials needed with pre-filled protocols →
Larazotide Reconstitution Calculator
Calculate concentration, syringe units, and doses per vial with auto-filled values →
Safety & Side Effects
Reported Side Effects
- !Mild gastrointestinal discomfort
- !Nausea (typically transient)
- !Headache
- !Dizziness
- !Fatigue
- !Abdominal cramping
- !Changes in bowel movements
- !Possible allergic reactions in sensitive individuals
- !Transient increase in intestinal gas production
Potential Interactions
- ⚡May affect absorption of other oral medications when taken concurrently
- ⚡Potential interactions with other tight junction modulators
- ⚡Could theoretically interfere with medications requiring intestinal permeability for absorption
- ⚡May interact with probiotics or other gut microbiome modulators
Important: Side effects and interactions listed here are compiled from published research and community reports. This is not a complete list. No formal drug interaction studies have been conducted for most research peptides. Always consult a qualified healthcare provider.
Research Studies
The following studies are referenced in this profile. PubMed IDs are provided where available for independent verification.
Safety and efficacy of larazotide acetate in patients with coeliac disease: a randomised, placebo-controlled study
Phase IIb trial showing larazotide acetate 0.5mg three times daily reduced symptoms in celiac patients during gluten challenge, with good safety profile
Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial
Demonstrated symptom improvement in celiac patients with persistent symptoms despite gluten-free diet, particularly for abdominal pain and stool consistency
Zonulin, a newly discovered modulator of intestinal permeability, and its expression in coeliac disease
Foundational research identifying zonulin pathway and its role in celiac disease pathophysiology, providing mechanistic basis for larazotide development
Note: This is not an exhaustive list of all published research. Studies are selected for relevance and quality. Click PubMed IDs to verify sources independently. Inclusion does not imply endorsement of the peptide for any clinical use.
Frequently Asked Questions
Larazotide is primarily researched for treating celiac disease by preventing gluten-induced intestinal permeability. It blocks the zonulin pathway that causes tight junction disruption when celiac patients are exposed to gluten.
Larazotide blocks CXCR3 receptors that zonulin normally binds to, preventing the cascade that opens tight junctions between intestinal cells. This maintains the intestinal barrier and reduces symptoms when gluten exposure occurs.
Larazotide has not received FDA approval for commercial use. It remains in clinical development, though it has shown promise in Phase II trials for celiac disease treatment.
The most common side effects include mild gastrointestinal discomfort, nausea, headache, and dizziness. Most adverse effects are transient and resolve with continued use.
No, larazotide is not intended to replace a gluten-free diet. Research focuses on its use as an adjunctive therapy for celiac patients who experience symptoms despite dietary adherence.
Larazotide is taken orally as capsules, typically three times daily before meals. The timing before meals is important for optimal protective effect against gluten exposure.
Larazotide provides protection primarily when taken before gluten exposure. Its effects on intestinal permeability can be measured within hours, but symptom improvement may take several days to weeks of consistent use.
Research studies have used doses ranging from 0.25mg to 8mg taken three times daily, with 0.5-2mg three times daily being the most commonly studied range for celiac disease applications.
Research & Educational Use Only
All content is for informational and research purposes only. This site does not provide medical advice, diagnosis, or treatment. Consult a qualified healthcare professional before using any peptide or supplement.
The information presented here is compiled from published research studies and is intended for informational purposes only. Individual results may vary. Always consult with a licensed healthcare provider.