Larazotide
Restore your intestinal barrier and protect against gluten damage
Written by Michael Carroll — Owner, Director of Research · Reviewed by the Peptide Initiative Research Team · Editorial standards
Suggested dose
0.5 mg
Compound profile
Scientific & efficacy data
Healing & Recovery
Peptide profile
Strong human trials
Larazotide
0.5 mg · Once daily
Molecular formula
C34H59N9O12
- Mol. weight
- 785.9 g/mol
- CAS number
- 206899-25-6
- PubChem
- 44146842
- Developed · 2002
- Hermitage Research Team
Hermitage Biotech (formerly Innovative Therapy Corporation)
Amino acid sequence
Eight amino acid synthetic peptide (exact sequence: proprietary, derived from Vibrio cholerae zonula occludens toxin)Intestinal Barrier Protection
Larazotide is specifically designed to strengthen and protect the intestinal barrier by blocking zonulin, the protein that opens tight junctions. This prevents undigested food particles and harmful substances from passing through intestinal walls.
Celiac Disease Management
Clinical trials show larazotide significantly reduces gastrointestinal symptoms in celiac patients during gluten challenge, including reduced diarrhea, abdominal pain, and inflammation markers.
Safety & Tolerability
Extensive clinical testing demonstrates excellent safety with few adverse events. It's well-tolerated across different populations and has a favorable side effect profile compared to many other therapeutic options.
Dosing
How much do I take?
0.5 mg · three times daily (before meals)
0.5 mg
Three times daily (before meals)
Covers timing · dose-adjustment guidance.
Suitability
Is this right for me?
Best for managing celiac disease symptoms despite strict gluten avoidance & reducing accidental gluten exposure damage
Best for
Managing celiac disease symptoms despite strict gluten avoidance
Larazotide is particularly well-suited for individuals focused on managing celiac disease symptoms despite strict gluten avoidance. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Reducing accidental gluten exposure damage
Larazotide is particularly well-suited for individuals focused on reducing accidental gluten exposure damage. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Restoring digestive comfort and nutrient absorption
Larazotide is particularly well-suited for individuals focused on restoring digestive comfort and nutrient absorption. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Supporting intestinal healing and barrier function
Larazotide is particularly well-suited for individuals focused on supporting intestinal healing and barrier function. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Consider alternatives if
Do not use if
Use with caution if
Not sure?
Compare Larazotide with similar peptides to find the best fit for your goals.
Administration
How do I use it?
Oral (capsule or tablet)
Route
Larazotide is administered Oral (capsule or tablet)—no injection required
Best sites
Covers reconstitution · step-by-step technique · storage · a sample daily schedule.
Safety
Is it safe?
4 common side effects · 2 serious
Larazotide (ALX-0061, AT-1001) is a synthetic tight-junction regulator that improved intestinal barrier function in Phase 2 celiac disease trials with favorable safety.
The mechanism—zonula occludens-1 modulation—is specific to epithelial tight junctions without broad immunosuppression. Gastrointestinal side effects (nausea, diarrhea, abdominal pain) occur in 10-20% of patients but are typically mild and resolve with dose adjustment or continued exposure.
FDA feedback on Phase 3 trials indicated efficacy trends but required additional manufacturing and clinical data before approval consideration.
Larazotide safety derives from two Phase 2b randomized controlled trials (n=316 and n=362 patients) published in Gut and Gastroenterology showing no serious adverse events attributable to larazotide and favorable tolerability compared to placebo. Serum enzyme elevation was minimal and reversible.
Phase 3 trial data remain unpublished as of 2025, but regulatory interactions with FDA suggest development is ongoing. The peptide demonstrates selective intestinal barrier modulation without systemic toxicity in evaluated cohorts.
Common side effects · experienced by some users
Headache
Occasional headaches reported in clinical trials, usually mild and transient. Often resolves within a few hours to days.
Management: Stay hydrated, rest in a quiet environment, and monitor frequency. If persistent, discuss with your healthcare provider about dose adjustment.
Nausea
Some patients experience mild nausea, particularly when taking the peptide on an empty stomach. This is typically mild and temporary.
Management: Take larazotide with food or a light meal to minimize nausea. Try ginger tea or small frequent meals throughout the day.
Abdominal Cramping
Occasional mild cramping or discomfort reported during the adjustment period. Usually diminishes after the first week of treatment.
Management: Use a heating pad, practice gentle stretching, and ensure adequate hydration. Contact your doctor if cramping is severe or persistent.
Fatigue
Rare reports of mild fatigue, possibly related to the body's healing response. Energy levels typically normalize quickly.
Management: Ensure adequate sleep, maintain good nutrition, and stay physically active. Supplement with B vitamins if deficient.
Less common
These typically resolve with continued use or dose adjustment.
Stop and seek help if
- Severe or worsening side effects that don't improve with dose adjustment or supportive care
- Signs of an allergic reaction—rash, hives, swelling, or difficulty breathing
- Your healthcare provider recommends discontinuation based on your clinical response
- Development of any new medical condition that may be contraindicated with Larazotide
- Pregnancy or planning to become pregnant (unless specifically approved for use during pregnancy)
- Abnormal lab results or clinical markers that suggest adverse effects
Larazotide should only be started, adjusted, or discontinued under medical supervision. This information is for educational purposes only and does not replace professional medical advice. Never stop a prescribed treatment without consulting your healthcare provider first, as abrupt discontinuation may have consequences.
With other peptides
- Safe:L-Glutamine — Synergistic intestinal barrier repair - glutamine feeds enterocytes while larazotide regulates tight junctions
- Safe:Probiotics — Supports healthy gut microbiome while larazotide restores barrier function for better probiotic colonization
- Safe:Zinc — Essential for tight junction protein synthesis and intestinal epithelial cell repair
With medications
- Caution:High-dose NSAIDs — Can increase intestinal permeability and may counteract larazotide's barrier-protective effects
- Caution:Excessive Alcohol — Alcohol damages tight junctions and can undermine larazotide's therapeutic benefits
- Caution:Certain Antibiotics — May disrupt beneficial gut microbiota needed for barrier healing synergy
With supplements
- Safe:Multivitamins — Generally safe to take alongside Larazotide. Space doses apart if taking oral formulations to ensure optimal absorption.
- Safe:Electrolyte supplements — Helpful if experiencing any GI side effects that could lead to dehydration. Safe to combine.
Effectiveness
How do I know it's working?
Strong human trials · first signs week 1-2: initial response (1-2 weeks)
Evidence level
Strong human trials
(Phase 3 or FDA approved)
Regulatory status
Not FDA approved
Onset of effects
Moderate
(1-2 weeks)
How it works
Larazotide is a peptide designed to tighten the intestinal barrier in celiac disease.
It binds to proteins that hold intestinal cells together, preventing harmful gluten from leaking through and triggering immune reactions.
The deeper mechanism
Larazotide (AT-1001) is a 9-amino acid peptide that modulates tight junction proteins, specifically claudins and ZO-1, preventing paracellular transport of dietary antigens in celiac disease.
What to expect
Week 1-2: Initial Response (1-2 weeks)
What you might notice
- Body begins adjusting to the peptide
- Tight junctions start receiving the barrier-protective signal
- Some patients notice subtle improvements in bloating
- Minor side effects like mild nausea may occur but typically resolve quickly
What's normal
- Initial response to Larazotide is beginning at the cellular level
- Different individuals experience Larazotide's onset at different rates
- Transient systemic effects from initial Larazotide exposure are common
What's next
- Maintain consistent Larazotide administration as prescribed
- Document subjective effects and physical markers daily
- Schedule a check-in with your provider about initial observations
Week 3-6: Barrier Strengthening (3-6 weeks)
What you might notice
- Intestinal barrier integrity improves noticeably
- Patients often report reduced abdominal pain, less frequent diarrhea, and improved energy levels
- The zonulin antagonist effect becomes more pronounced as tight junctions strengthen
What's normal
- Larazotide is now achieving steady-state pharmacokinetics
- Measurable changes aligned with Larazotide's mechanism may appear
- Initial adjustment effects typically resolve by this point
What's next
- Maintain Larazotide dosing exactly as established
- Track progress toward intended outcomes in detail
- Review lab work or biomarker changes with your healthcare team
Week 7-12: Established Benefit (7-12 weeks)
What you might notice
- Maximum therapeutic benefits typically achieved
- Significant reduction in gastrointestinal symptoms
- Improved tolerance to small amounts of gluten exposure (though strict gluten-free diet still recommended)
- Intestinal inflammation markers decrease
What's normal
- Larazotide has achieved stable, long-term homeostatic integration
- Sustained efficacy of Larazotide remains consistent
- Chronic Larazotide effects remain stable and predictable
What's next
- Maintain your established Larazotide protocol for sustained benefits
- Continue periodic monitoring to confirm Larazotide efficacy
- Review comprehensive Larazotide response with your provider
Month 4+: Maintenance Phase (Ongoing)
What you might notice
- Continued barrier protection and symptom improvement
- Benefits plateau at optimal level
- Maintenance dosing may reduce requirements
- Patient can assess impact on quality of life with reduced GI symptom burden and improved nutrient absorption
What's normal
- Full therapeutic effects of Larazotide are well-characterized at this point
- Maintenance of Larazotide's therapeutic effects is typical
- Tolerance patterns with Larazotide are generally stable over months
What's next
- Comprehensive assessment of Larazotide efficacy should be conducted
- Discuss long-term continuation, cycling, or protocol modifications
- Continue regular monitoring of relevant biomarkers or symptoms
Signs it's working
Treatment Response
- Improvement in the primary symptoms or condition being treated
- Positive changes in relevant lab values or clinical markers
- Consistent, stable response to Larazotide over time
- Reduction in symptom frequency or severity
General Well-being
- Improved energy levels and daily functioning
- Better quality of life related to the treated condition
- Manageable or absent side effects indicating good tolerance
- Positive feedback from healthcare provider during check-ups
Not seeing results? Common reasons
- Not at therapeutic dose yet—initial doses are for building tolerance, not maximum effect
- Insufficient time at target dose—most compounds need several weeks to show full benefits
- Inconsistent dosing schedule—regular, consistent use is crucial for optimal results
- Individual variation in response—genetics, metabolism, and other factors affect outcomes
- Underlying conditions or medications interfering with absorption or effectiveness
- Improper storage leading to degraded product—always verify proper storage conditions
Key research
Clinical trials
Tested in people
10 registered studies, none currently enrolling.
By phase
A trial spanning two phases is counted in both, so these can sum above the total. Observational studies carry no phase.
What kind of research
About 1,211 people took part in the studies that actually administered Larazotide. Observational studies analyse the records of people already taking it — nobody was given anything for the study, so they are counted separately and cannot show cause and effect.
Most recent
AT1001 for the Treatment of Long COVID
Massachusetts General Hospital
AT1001 for the Treatment of COVID-19 Related MIS-C
Massachusetts General Hospital
Study to Evaluate the Efficacy and Safety of Larazotide Acetate for the Relief of CeD Symptoms
9 Meters Biopharma, Inc.
Sources: ClinicalTrials.gov, the EU Clinical Trials Information System and ISRCTN, deduplicated so a study registered twice is counted once. A study is counted when Larazotide is named as an intervention; studies that only mention it in passing are not.
Questions
Frequently asked
Is larazotide a cure for celiac disease?
No, larazotide is not a cure for celiac disease. It's a therapeutic treatment that helps manage symptoms and protect the intestinal barrier. The gold standard treatment remains a strict gluten-free diet. However, larazotide may provide additional protection, especially for those exposed to small amounts of gluten accidentally or those struggling with persistent symptoms despite dietary compliance.
Can I eat gluten if I take larazotide?
No, you should not intentionally consume gluten even while taking larazotide. The medication provides additional barrier protection, but it's not designed to allow normal gluten consumption. In clinical trials, larazotide was used during controlled gluten challenges under medical supervision. Continue following a strict gluten-free diet as the foundation of celiac disease management.
How is larazotide different from other celiac treatments?
Larazotide is unique because it targets the fundamental mechanism of intestinal barrier dysfunction through zonulin antagonism. Rather than suppressing the immune system like some treatments, it restores normal intestinal barrier function. This mechanism-based approach offers potential advantages in safety and effectiveness for barrier restoration.
When will larazotide be FDA approved?
Larazotide is currently in Phase 3 clinical trials, which are the final stage before FDA review. If trials are successful and the FDA approves it, it could become available within the next few years. However, timelines for drug approval can vary. Check ClinicalTrials.gov for the most current trial status and estimated completion dates.
Who should not take larazotide?
Larazotide should not be used by people with known hypersensitivity to the peptide, severe gastrointestinal obstruction, or compromised kidney function. Pregnant and breastfeeding women should avoid it due to limited safety data. Always consult with a gastroenterologist before starting treatment to ensure it's appropriate for your specific situation.
Can larazotide be used for non-celiac gluten sensitivity?
Research is still ongoing regarding larazotide's effectiveness in non-celiac gluten sensitivity and other conditions involving intestinal permeability. While clinical trials have focused on celiac disease, the mechanism of action suggests potential benefits for other conditions characterized by compromised barrier function. Discuss with your healthcare provider about potential off-label uses.
How does larazotide compare to just following a gluten-free diet?
A gluten-free diet is the foundation of celiac disease management and must continue. Larazotide is designed to work alongside this diet. While a gluten-free diet prevents new gluten from damaging the barrier, larazotide actively helps restore and protect an already-damaged barrier. Together, they offer comprehensive barrier protection and symptom management.
Further reading
History & related research
History · since 2003
The peptide that seals the gut and treats celiac disease from the inside.
Larazotide is a short peptide made of eight amino acids. It stops intestinal walls from leaking by blocking zonulin, a protein that opens gaps between gut cells.
Read the full history of LarazotideStudied for
Ready for the protocol?
Every dosing tier, administration route, timing note, and dose-adjustment rule for Larazotide, on one page.