Peptide Profile
Larazotide
Restore your intestinal barrier and protect against gluten damage
Dose Range
250 mcg-1000 mcgmcg
Frequency
Once daily
Route
Oral (capsule or tablet)
Cycle Length
Ongoing/indefinite
Onset
Moderate (1-2 weeks)
Evidence
Strong
Compound Profile
Scientific & Efficacy Data
C34H59N9O12
Molecular Formula
785.9 g/mol
Molecular Weight
Unknown - acts primarily as local intestinal barrier regulator rather than systemic drug
Half-Life
Orally administered; acts locally on intestinal epithelium with minimal systemic absorption
Bioavailability
206899-25-6
CAS #
44146842
PubChem ID ↗
Developed By · 2002
Hermitage Research Team
Hermitage Biotech (formerly Innovative Therapy Corporation)
Primary Benefits
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.
Clinical trials show larazotide significantly reduces gastrointestinal symptoms in celiac patients during gluten challenge, including reduced diarrhea, abdominal pain, and inflammation markers.
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.
Amino Acid Sequence
Eight amino acid synthetic peptide (exact sequence: proprietary, derived from Vibrio cholerae zonula occludens toxin)Dosing
How much
do I take?
Timing
Best time to take
Take Larazotide at the same time each day for consistent blood levels. Morning dosing with breakfast is often preferred, but follow your healthcare provider's specific instructions.
With food?
Larazotide can typically be taken with or without food. Taking it with a light meal may help reduce any GI discomfort. Avoid taking with grapefruit juice or high-fat meals unless specifically directed.
If stacking
Larazotide should be used as directed by your healthcare provider. If combining with other medications or supplements, discuss potential interactions with your provider. Avoid combining with compounds that have overlapping mechanisms unless specifically guided by a medical professional.
Adjusting Your Dose
Increase if
- +You've tolerated the current dose for the recommended period without significant side effects
- +Therapeutic goals haven't been met at the current dose level
- +Your healthcare provider recommends dose escalation based on your response
- +Lab work or clinical assessments support a higher dose
Decrease if
- -Side effects are bothersome or impacting daily life despite management strategies
- -You experience any signs of an adverse reaction
- -Lab results indicate the need for dose reduction
- -Your healthcare provider recommends a lower dose based on your response
Signs of right dose
- ✓Therapeutic goals being met with minimal side effects
- ✓Stable and consistent response to treatment
- ✓Lab values or clinical markers trending in the right direction
- ✓Good tolerance with manageable or absent side effects
Dosing Calculator
Calculate Your Exact Dose
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Suitability
Is this
right for me?
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
Who Should Avoid
Do not use if
- ×Known hypersensitivity to larazotide or any component
- ×Severe gastrointestinal obstruction
- ×Active untreated infections (may require monitoring)
- ×Pregnancy and breastfeeding (limited safety data)
Use with caution if
- !You are taking other medications—discuss potential interactions with your healthcare provider
- !You have a history of liver or kidney disease
- !You are elderly or have multiple medical conditions
- !You are planning surgery in the near future—inform your surgeon about Larazotide use
- !You have any chronic health conditions that require regular monitoring
Administration
How do I
use it?
Reconstitution
What you need
- •Larazotide in its prescribed form
- •Clean, dry storage container
- •Measuring device if applicable (oral syringe, measuring cup)
- •Calendar or reminder app for dosing schedule
Injection
Route
Larazotide is administered Oral (capsule or tablet)—no injection required
Best sites
- •Not applicable—this is not an injectable formulation
Technique
- 1.Follow the specific administration instructions for your Larazotide formulation
- 2.Take or apply as directed by your healthcare provider
- 3.Store properly between uses according to package instructions
Storage
Signs of degradation
Sample Daily Schedule
Safety
Is it
safe?
Safety Profile
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
- •Transient Diarrhea
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.
Interactions
With other peptides
- ✓Synergistic intestinal barrier repair - glutamine feeds enterocytes while larazotide regulates tight junctions
- ✓Supports healthy gut microbiome while larazotide restores barrier function for better probiotic colonization
- ✓Essential for tight junction protein synthesis and intestinal epithelial cell repair
With medications
- !High-dose NSAIDs - Can increase intestinal permeability and may counteract larazotide's barrier-protective effects
- !Excessive Alcohol - Alcohol damages tight junctions and can undermine larazotide's therapeutic benefits
- !Certain Antibiotics - May disrupt beneficial gut microbiota needed for barrier healing synergy
With supplements
- ✓Multivitamins - Generally safe to take alongside Larazotide. Space doses apart if taking oral formulations to ensure optimal absorption.
- ✓Electrolyte supplements - Helpful if experiencing any GI side effects that could lead to dehydration. Safe to combine.
Effectiveness
Does it
work?
Evidence Level
Strong human trials
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
"Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials"
Research investigators, 2022
Finding: Meta-analysis of four randomized trials showed larazotide significantly improved gastrointestinal symptoms when patients were exposed to gluten. The peptide maintained a favorable safety profile with few adverse events, supporting its potential as adjunct therapy.
View Study"Coeliac disease and the intestinal barrier: mechanisms of disruption and strategies for restoration"
Research investigators, 2025
Finding: Larazotide acetate acts as a zonulin antagonist to restore intestinal barrier integrity in celiac disease. The review highlighted larazotide and other barrier-restoring therapies as important complementary approaches to gluten avoidance.
View Study"Ameliorative Effects of Larazotide Acetate on Intestinal Permeability and Bacterial Translocation in Acute Pancreatitis Model in Rats"
Research investigators, 2024
Finding: Larazotide reduced intestinal damage scores and bacterial translocation frequency from 100% to 50% in acute pancreatitis models. The peptide's tight junction-regulating effects prevented harmful bacteria from crossing the intestinal barrier.
View Study"Celiac disease: Hope for new treatments beyond a gluten-free diet"
Research investigators, 2024
Finding: Larazotide represents a new pharmacological treatment option for celiac disease patients with persistent symptoms. The peptide offers potential to improve quality of life beyond traditional gluten-free dietary management.
View Study"Current pharmacological approaches and potential future therapies for Celiac disease"
Research investigators, 2021
Finding: Larazotide emerged as a leading tight junction regulator with robust clinical trial data. The peptide's mechanism of blocking zonulin receptors offers a novel therapeutic approach distinct from traditional gluten-degrading enzymes.
View StudyFrequently Asked Questions