peptideNot FDA-approvedNot FDA-approved; larazotide has been studied as an investigational drug in celiac disease and, more recently, pediatric post-COVID inflammatory syndromeNot sold as a dietary supplement in the cited trials
LarazotideBenefits, Dosage & Interactions
Also known as: AT-1001
Larazotide, also known by its development code AT-1001, is an orally administered peptide compound. " Larazotide is designed to block the functional activity of zonulin, a human protein that modulates intestinal tight junctions. Research on Larazotide focuses on tissue recovery.
How much Larazotide do people take?
Celiac disease trials used oral larazotide acetate doses ranging from 0.5 mg to 8 mg per dose, with 0.5 mg or 0.25 mg three times daily most consistently associated with symptom benefit. Route reported: Oral capsule, taken before meals. Frequency reported: Three times daily before meals in the celiac disease RCTs. These are amounts documented in the cited studies and labels for Larazotide — they are reported for reference, not a recommendation. Regulatory status differs by country, including between the US (FDA) and Canada (Health Canada). Confirm any amount with a licensed clinician before you take it.
See the full reported protocol and its sourcesResearched by DoseRoutine Research TeamReviewed for accuracy by Nicholas Alexander, RSE, SO, PMPLast updated Educational reference only — not medical advice. Always confirm dosing and safety decisions with a licensed clinician.
Evidence: Strong — 4 human randomized trials published.
Evidence strengthStrong · 4/4
PreclinicalStrong human evidence
4 human randomized trials published.
Can larazotide replace a gluten-free diet?
No. Larazotide was investigated as an adjunct for celiac disease, not as permission to eat gluten. The cited phase 3 program was discontinued after an interim analysis; earlier signals should not be presented as established treatment success.
Source: Celiac Disease Foundation trial update
Browse compound evidence cardsPlasma half-life
Minimal systemic absorption reported; larazotide acts locally in the gut lumen rather than being measured with a conventional plasma half-life
Typical timing
with a meal
Food rule
with food
Default unit
mg
What published protocols report
Ranges documented in the literature, shown for reference. DoseRoutine does not recommend an amount — your prescriber or the product label sets the dose.
- Reported amounts
- Celiac disease trials used oral larazotide acetate doses ranging from 0.5 mg to 8 mg per dose, with 0.5 mg or 0.25 mg three times daily most consistently associated with symptom benefit[1][2][3]
- Cycle length
- Trial durations of 8 to 12 weeks in the celiac disease studies; the pediatric MIS-C trial used a short inpatient course[1][2][3]
Reported for Larazotide in the cited sources. Published ranges are not dosing advice.
Mixing Larazotide: bacteriostatic water and syringe units
The vial arrives as dry powder. How much water you add sets the strength, and the strength sets the mark you draw to on the syringe. The table assumes a 5 mg vial and a 250 mcg example draw on a U-100 insulin syringe, where 100 units is one millilitre. If your vial is a different size, scale it — the arithmetic is the same.
| Bacteriostatic water added | Resulting strength | 250 mcg draws to |
|---|---|---|
| 1 mL | 5 mg/mL | 5 units |
| 2 mL | 2.5 mg/mL | 10 units |
| 3 mL | 1.67 mg/mL | 15 units |
Units, not millilitres. Insulin syringes are marked in units, and mixing up mcg and mg on a peptide label is the single most common error people report. Check the label twice. Run your own vial through the calculator.
Storage and stability
- Before mixing
- Sealed and still as a dry powder, Larazotide vials are normally kept in the fridge at 2–8 °C, out of light. Short spells at room temperature during shipping are the norm for lyophilized peptides and are not, on their own, a sign the vial is spoiled.
- After mixing
- Once bacteriostatic water goes in, the vial belongs in the fridge and is generally treated as good for about 28 days — that is how long the benzyl alcohol in bacteriostatic water is relied on to hold back bacterial growth. Plain sterile water has no preservative, so a vial mixed with it is a single-session vial. Never freeze a reconstituted vial.
- When to throw it out
- A properly mixed vial is clear. Cloudiness, floating strands, a color change or powder that will not go into solution after gentle swirling all mean the vial should be discarded rather than used. Shaking a peptide vial hard is the usual cause — swirl it, or run the water down the inside wall of the vial instead of onto the powder.
Handling and shelf-life figures describe general practice for lyophilized peptides. They are not a dose and not medical advice — your prescriber or the product label sets the amount.
References & evidence
Documents the Larazotide entry is written from. Each number matches an inline marker above.
- [1]Larazotide Acetate for Persistent Symptoms of Celiac Disease Despite a Gluten-Free Diet: A Randomized Controlled TrialLeffler DA, Kelly CP, Green PH, Fedorak RN, DiMarino A, Perrow W, et al. · Gastroenterology · 2015 · Peer-reviewed · PMID 25683116
- [2]A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challengeLeffler DA, Kelly CP, Abdallah HZ, Colatrella AM, Harris LA, Leon F, et al. · The American Journal of Gastroenterology · 2012 · Peer-reviewed · PMID 22825365
- [3]Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotideYonker LM, Kane AS, Swank Z, Papadakis L, Kenyon V, Han S, et al. · Science Translational Medicine · 2025 · Peer-reviewed · PMID 40737433
References & Evidence
Sources on this page that document Larazotide dosing, timing and safety.
- [1]National Center for Biotechnology Information View source
Educational information only — not medical advice. Dose ranges vary by person, indication and prescriber.
What is Larazotide studied for?
What is Larazotide?Sources for this section: Jumps to this entry in the sources and references list at the end of the page.
Larazotide, also known by its development code AT-1001, is an orally administered peptide compound. It is being investigated for its potential role in managing conditions characterized by increased intestinal permeability, often referred to as "leaky gut." Larazotide is designed to block the functional activity of zonulin, a human protein that modulates intestinal tight junctions. By doing so, it aims to reduce the passage of undigested food particles, toxins, and microbes from the gut lumen into the bloodstream. Currently, larazotide is an investigational compound and is not approved for clinical use by regulatory bodies such as the FDA or EMA. Its development has primarily focused on celiac disease, where increased intestinal permeability is a prominent feature.
What does the research say about Larazotide?
Tap a section to expand.
Larazotide's primary mechanism of action involves interacting with zonulin, a protein that reversibly regulates the permeability of intestinal tight junctions. Tight junctions are structures between epithelial cells that control the paracellular pathway, meaning the passage of substances between cells. When zonulin is released in the gut, it binds to specific receptors on intestinal epithelial cells, initiating a cascade that leads to the disassembly of tight junction proteins. This disassembly increases the permeability of the intestinal lining.
Larazotide acts as a zonulin antagonist. It is a synthetic octapeptide that is thought to block the binding of zonulin to its receptor, thereby preventing the zonulin-mediated increase in intestinal permeability. By inhibiting this pathway, larazotide aims to maintain the integrity of the intestinal barrier and reduce the translocation of potentially harmful substances from the gut lumen into the systemic circulation. This mechanism suggests a potential therapeutic benefit in conditions where increased intestinal permeability is implicated, such as celiac disease or other inflammatory bowel conditions (Source: DrugBank, PubChem).
Source for this section: Sources for How does Larazotide work?: Jumps to this entry in the sources and references list at the end of the page.
As an investigational compound, larazotide's potential benefits are still under evaluation through clinical trials. The primary anticipated benefit of larazotide is its ability to reduce increased intestinal permeability. In conditions like celiac disease, increased intestinal permeability is considered a key factor in the disease's pathogenesis, allowing immunogenic peptides from gluten to cross the intestinal barrier and trigger an immune response.
Clinical trials, particularly in the context of celiac disease, have explored larazotide's potential to:
* **Reduce symptoms of celiac disease:** By restoring gut barrier function, it is hypothesized that larazotide could mitigate gastrointestinal symptoms (e.g., abdominal pain, bloating, diarrhea) and potentially systemic symptoms in celiac patients who consume gluten, even inadvertently. (Source: NIH ODS)
* **Improve intestinal histology:** Some studies have looked into whether larazotide can help in the healing of intestinal villi, which are often damaged in celiac disease.
* **Reduce inflammation:** By limiting the exposure to triggers from the gut lumen, it may contribute to reduced local and systemic inflammation.
It is important to emphasize that these are potential benefits under investigation, and larazotide is not currently approved for any medical use.
The evidence for larazotide's effects primarily comes from preclinical studies and clinical trials, particularly in individuals with celiac disease. Its development has progressed through various phases of clinical research.
* **Celiac Disease:** Numerous clinical trials have investigated larazotide as an adjunct therapy for celiac disease, especially for patients who experience persistent symptoms despite adhering to a strict gluten-free diet, or for incidental gluten exposure. A review published in the *Cochrane Database of Systematic Reviews* assesses the evidence of various therapies for celiac disease, including larazotide, noting the need for further robust trials to establish efficacy and long-term safety. While some studies have shown promise in reducing symptoms and improving quality of life in challenged celiac patients, conflicting results across trials highlight the complexity of the condition and the investigational nature of the compound (Source: Cochrane).
* **Mechanism Confirmation:** Preclinical and early-phase studies have provided evidence supporting larazotide's mechanism of action in modulating tight junctions and reducing zonulin-mediated permeability (Source: PubChem, DrugBank).
Ongoing research continues to clarify larazotide's therapeutic potential, optimal dosing, and long-term safety profile across different patient populations and conditions. It is crucial to monitor findings from ongoing and future clinical trials to fully understand its efficacy and role in clinical practice.
Clinical trials of larazotide have reported various side effects, although these are typically mild to moderate in severity. Given that larazotide is an investigational drug, the full spectrum and frequency of potential side effects are still being characterized.
Commonly reported side effects have included:
* Gastrointestinal disturbances: Nausea, abdominal pain, diarrhea, constipation.
* Headache
* Fatigue
* Dizziness
* Upper respiratory tract infections
These side effects are generally considered transient. The development of larazotide is ongoing, and further studies are needed to provide a complete safety profile. This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
As an investigational compound, specific warnings for larazotide are still under evaluation. However, based on its mechanism of action and the nature of clinical trials, general considerations apply:
* **Pregnancy and Breastfeeding:** There is insufficient data on the use of larazotide during pregnancy or breastfeeding. Therefore, it is generally advised to avoid use in these populations until more safety data is available. (Source: NIH ODS)
* **Pediatric Use:** Safety and efficacy in pediatric populations have not been fully established, and use should be approached with caution or avoided.
* **Underlying Medical Conditions:** Individuals with severe gastrointestinal conditions other than those being studied (e.g., inflammatory bowel disease, severe liver or kidney impairment) should exercise caution, as the effects of larazotide in these contexts are not well-understood.
* **Hypersensitivity:** As with any peptide compound, there is a theoretical risk of hypersensitivity reactions, though these have not been predominantly reported in trials. If signs of allergic reaction appear, discontinue use immediately.
* **Duration of Use:** Long-term safety data for larazotide are still being gathered. The implications of prolonged use on overall gut health and systemic function are not fully known.
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Given that larazotide is an investigational drug and not approved for clinical use, a comprehensive list of contraindications established by regulatory bodies does not exist. However, based on available research and general pharmacological principles, potential contraindications or situations where extreme caution is warranted may include:
* **Known Hypersensitivity:** Individuals with a known allergy or severe hypersensitivity reaction to larazotide or any of its excipients should avoid its use.
* **Severe Gastrointestinal Obstruction:** In conditions involving severe mechanical obstruction of the gastrointestinal tract, the use of oral compounds like larazotide might not be appropriate.
* **Acute Gastrointestinal Bleeding:** In situations of active and significant gastrointestinal bleeding, the administration of any oral compound should be carefully considered by a clinician.
As more research becomes available and if larazotide were to gain approval, a definitive list of contraindications would be provided by regulatory agencies (e.g., FDA, EMA). This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
As an investigational compound, comprehensive drug-drug interaction studies for larazotide are limited. Therefore, specific compounds that absolutely "do not mix" with larazotide are not fully elucidated. However, general considerations for any investigational compound apply:
* **Other Agents Affecting Gut Permeability:** Concomitant use with other drugs or supplements that are known to either increase or decrease intestinal permeability could theoretically alter larazotide's effects or lead to unforeseen interactions. Data on such interactions are currently lacking.
* **Immunosuppressants:** In conditions like celiac disease, some patients may be on immunosuppressive therapy if they have refractory disease. The interaction between larazotide and immunosuppressants has not been thoroughly studied.
* **Highly Protein-Bound Drugs:** While larazotide is a peptide, if it were to interact with plasma proteins, it could theoretically displace or be displaced by highly protein-bound drugs, altering free drug concentrations. However, this is largely speculative without specific pharmacokinetic studies.
* **Agents Affecting Gut Motility:** Drugs that significantly alter gut motility could theoretically affect the absorption or transit time of larazotide, potentially impacting its efficacy.
Until more data are available, caution should be exercised when considering combining larazotide with any other prescription medications, over-the-counter drugs, or dietary supplements. This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Larazotide is typically administered orally. In clinical trials, the timing of administration commonly suggested is "with a meal," especially with meals containing gluten when evaluated in celiac disease studies. The rationale for this timing is often linked to its proposed mechanism of action: by being present in the gut when potential zonulin-releasing triggers (like gluten) are consumed, it can ideally block the increase in intestinal permeability proactively. The specific dose and exact timing (e.g., immediately before, during, or after a meal) would be determined by the licensed clinician managing the treatment. The typical half-life of larazotide in the body is approximately 1 hour, suggesting that maintaining its presence in the gut lining might require specific dosing regimens.
Source for this section: Sources for When should you take Larazotide?: Jumps to this entry in the sources and references list at the end of the page.
Put it into practice
Reading about Larazotide is the first step — DoseRoutine helps you act on it. These free tools turn what you just learned into a routine.
What interacts with Larazotide?
| Interacts with | Severity | Type | What happens | What to do |
|---|---|---|---|---|
| Any peptide + hormone | Note | Category ruleConfidence: theoretical | Injectable peptides plus hormones can have overlapping or compounding effects that aren't always well characterized.Source pending | Track bloodwork with a provider; don't assume combinations are neutral. |
Frequently asked questions about Larazotide
Larazotide is an investigational peptide primarily studied for its potential to manage increased intestinal permeability in conditions like celiac disease. It is not currently approved for any medical use.
Larazotide works by blocking the activity of zonulin, a protein that regulates the 'tightness' of the junctions between cells in the intestinal lining. By inhibiting zonulin, it aims to reduce intestinal permeability, sometimes referred to as 'leaky gut'.
No, Larazotide is an investigational compound and is not currently approved by the FDA or any other major regulatory agency for clinical use. It is still undergoing clinical trials.
Clinical trials have reported generally mild to moderate side effects such as nausea, abdominal pain, diarrhea, constipation, headache, fatigue, and dizziness. The full safety profile is still being determined.
There is currently insufficient data regarding the use of Larazotide during pregnancy or breastfeeding. It is generally advised to avoid its use in these populations until more safety information is available. Always consult a healthcare professional.
Interaction risk for Larazotide comes from the rest of the stack: other peptides, prescription medicines, hormone therapy and peptides. Because Larazotide is usually taken with a meal, most avoidable conflicts come from what else lands in that same window. Risk depends on dose, timing and what else is taken the same day, so each pairing has to be checked rather than assumed safe. The free checker at https://doseroutine.com/interaction-checker covers Larazotide with no sign-up.
Larazotide is typically taken with a meal. Published protocols usually have it taken with food. Published ranges differ between studies and formulations — the dose to use is the one on your label or from your clinician.
There is no single answer for Larazotide plus TRT. What matters is the specific protocol you are on and what your most recent hormone panel shows. No general contraindication applies across every TRT protocol, so confirm the combination with the prescribing clinician. See the free TRT interaction reference: https://doseroutine.com/trt-supplement-interactions
Pairing Larazotide with peptides has to be assessed one peptide at a time, because GLP-1 agonists, secretagogues, healing peptides and melanocortins do not share an interaction profile. Check the combination peptide by peptide rather than as one group, and review it with a clinician familiar with peptide protocols.
Published frequency for Larazotide varies by protocol and formulation, so the label or prescription is what sets it. It is typically taken with a meal. Most protocols have it taken with food. Frequency is a clinical decision, not a fixed rule — confirm it with the prescriber or product label. Comparison of apps that keep a schedule like this: https://doseroutine.com/best-dose-tracking-apps
The effect of a missed dose of Larazotide depends on the protocol and formulation you are on. Doubling up to "catch up" is generally not appropriate unless the label or prescriber says so. Follow the missed-dose instructions on your label or from your clinician, and log the miss so the pattern is visible later rather than forgotten.
For Larazotide the useful record is the dose, the time it was actually taken, and what else was taken in the same window. A written log or spreadsheet works for planning but does not remind you or flag conflicts — see the honest comparison at https://doseroutine.com/vs/spreadsheet and the wider roundup at https://doseroutine.com/best-dose-tracking-apps — DoseRoutine tracks the schedule, the remaining supply and interactions with the rest of your routine in one place.
No. Larazotide was investigated as an adjunct for celiac disease, not as permission to eat gluten. The cited phase 3 program was discontinued after an interim analysis; earlier signals should not be presented as established treatment success.
Small or earlier studies can produce encouraging results that do not hold up in a larger program. The discontinued trial limits confidence in clinical benefit; it does not justify a self-treatment protocol or replacing established celiac care.
Celiac disease trials used oral larazotide acetate doses ranging from 0.5 mg to 8 mg per dose, with 0.5 mg or 0.25 mg three times daily most consistently associated with symptom benefit. Route reported: Oral capsule, taken before meals. Frequency reported: Three times daily before meals in the celiac disease RCTs. These are amounts documented in the cited studies and labels for Larazotide — they are reported for reference, not a recommendation. Regulatory status differs by country, including between the US (FDA) and Canada (Health Canada). Confirm any amount with a licensed clinician before you take it.
Which studies looked at Larazotide?
Peer-reviewed research indexed in PubMed. Each entry links to the original record.
- 1.Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials(opens PubMed in a new tab)Clin Res Hepatol Gastroenterol · 2022 · PMID 34339872 · https://pubmed.ncbi.nlm.nih.gov/34339872/
- 2.The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases(opens PubMed in a new tab)Curr Med Chem · 2021 · PMID 33397225 · https://pubmed.ncbi.nlm.nih.gov/33397225/
Sources cited on this page
Specific documents referenced by the numbered markers above. Each number matches the marker in the text.
- PubChem CID 9810532(opens in a new tab)National Center for Biotechnology Information · pubchem.ncbi.nlm.nih.gov/compound/9810532
Verify at
Publisher search links for Larazotide. These are places to check the information — they are not citations, so they are not numbered.
- DrugBank(publisher search, opens in a new tab)DrugBank Online · publisher search
- NIH Office of Dietary Supplements(publisher search, opens in a new tab)National Institutes of Health · publisher search
- Cochrane Library(publisher search, opens in a new tab)Cochrane · publisher search
- ClinicalTrials.gov(publisher search, opens in a new tab)U.S. National Library of Medicine · publisher search
- PubMed literature search(publisher search, opens in a new tab)National Library of Medicine · publisher search
- DailyMed labeling archive(publisher search, opens in a new tab)U.S. National Library of Medicine · publisher search
- Wikipedia entry(publisher search, opens in a new tab)Wikipedia · publisher search
DoseRoutine compiles summaries from publicly available scientific and regulatory references. Always verify important decisions with a licensed clinician. How we source and review this information.
What is the short answer on Larazotide?
Plain-text summary, safe to quote verbatim:
Larazotide, also known by its development code AT-1001, is an orally administered peptide compound. " Larazotide is designed to block the functional activity of zonulin, a human protein that modulates intestinal tight junctions. Research on Larazotide focuses on tissue recovery.
Source: DoseRoutine — https://doseroutine.com/library/larazotide
Larazotide cheat sheet
DoseRoutine cheat sheet · Peptide
Larazotide
Larazotide, also known by its development code AT-1001, is an orally administered peptide compound. " Larazotide is designed to block the functional activity of zonulin, a human protein that modulates intestinal tight junctions.
Evidence
Strong
4 human randomized trials published.
Studied range
Celiac disease trials used oral larazotide acetate doses ranging from 0.5 mg to 8 mg per dose, with 0.5 mg or 0.25 mg three times daily most consistently associated with symptom benefit
Route
Oral capsule, taken before meals
Frequency studied
Three times daily before meals in the celiac disease RCTs
Half-life
Minimal systemic absorption reported; larazotide acts locally in the gut lumen rather than being measured with a conventional plasma half-life
Timing
with a meal
With food
with food
Storage
Room temperature, sealed, as used in the cited trials
Not FDA-approvedNot FDA-approved; larazotide has been studied as an investigational drug in celiac disease and, more recently, pediatric post-COVID inflammatory syndromeNot sold as a dietary supplement in the cited trialsRecovery
Key references
- Larazotide Acetate for Persistent Symptoms of Celiac Disease Despite a Gluten-Free Diet: A Randomized Controlled Trial (2015)
- A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge (2012)
- Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide (2025)
Studied ranges, not dosing advice. Not medical advice — talk to a clinician. doseroutine.com/library/larazotide
Cite this page
Using this in an article, AI answer, or research note? Please attribute:
DoseRoutine. (2026). Larazotide — Overview, Benefits & Side Effects. Retrieved from https://doseroutine.com/library/larazotide
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