Larazotide acetate
Tissue Repair and Healing
ABOUT
Larazotide is an oral tight-junction regulator developed for coeliac disease. Its phase 3 trial was stopped at interim analysis in 2022, so no confirmatory efficacy evidence exists.
EVIDENCE OVERVIEW
Too little published work to judge either way
WHAT THIS MEANS
Insufficient evidence. Review the research and limitations before relying on this record.
IDENTITY
HALF-LIFE
HOW IT IS THOUGHT TO WORK
An eight-amino-acid peptide developed from work on zonulin, a human protein homologous to Vibrio cholerae zonula occludens toxin that regulates intestinal tight junctions. In coeliac disease, gluten exposure triggers zonulin release, opening paracellular tight junctions and allowing immunogenic gluten peptides across the epithelium. Larazotide is thought to act as a zonulin antagonist, and has been linked to inhibition of myosin light chain kinase, which reduces tension on actin filaments and facilitates tight-junction closure.
PHARMACOKINETICS
Acts locally in the intestinal lumen and is minimally absorbed systemically. Given orally in an enteric-coated capsule designed to release in the small intestine, so systemic pharmacokinetic parameters are largely inapplicable by design.
REVIEW
PUBLISHED PAIR RECORDS
with Teduglutide
Increased absorption of an orally dosed compoundTeduglutide labelling states that, because it enlarges intestinal absorptive capacity, there is a potential for increased absorption of concomitant oral medicines, and directs prescribers to monitor any oral drug that is titrated or has a narrow therapeutic index because it may need a dose reduction. Larazotide acetate is taken orally, so it falls inside that statement. Larazotide is the sharpest case in this catalogue: it is an enteric-coated oral peptide whose whole design assumes release at a particular point in the small intestine and minimal systemic absorption, and it acts on the same intestinal barrier teduglutide remodels. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Semaglutide
Delayed gastric emptying may alter delivery of an enteric-coated oralSemaglutide labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Liraglutide
Delayed gastric emptying may alter delivery of an enteric-coated oralLiraglutide labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Exenatide
Delayed gastric emptying may alter delivery of an enteric-coated oralExenatide labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Dulaglutide
Delayed gastric emptying may alter delivery of an enteric-coated oralDulaglutide labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Tirzepatide
Delayed gastric emptying may alter delivery of an enteric-coated oralTirzepatide labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Pramlintide
Delayed gastric emptying may alter delivery of an enteric-coated oralPramlintide labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines, and pramlintide labelling adds that it is not recommended for patients taking other drugs that alter gastrointestinal motility. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with PT-141
Delayed gastric emptying may alter delivery of an enteric-coated oralPT-141 labelling states that it delays gastric emptying and may affect the rate and extent of absorption of concomitantly administered oral medicines. Larazotide acetate is given as an enteric-coated oral capsule designed to release in the small intestine, acts locally on tight junctions there, and is minimally absorbed systemically - so what matters for it is where and when the capsule arrives, not a plasma concentration. Changing gastric emptying changes that delivery. Larazotide's own confirmatory phase 3 trial was stopped at interim analysis for futility, so there is no established effect size for it to lose in the first place; the interaction concern is about delivery, not about diminishing a proven benefit. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 21 Aug 2026with Kyinsu
Inherited from a component of this blendKyinsu contains Semaglutide, and the catalogue holds a curated pair record between that component and Larazotide acetate: Semaglutide (delayed gastric emptying may alter delivery of an enteric-coated oral). Taking the blend therefore carries the same consideration as taking that component on its own, with the difference that a fixed-ratio vial cannot be adjusted independently of the rest of its contents. The evidence and citations here are the component record's; nothing has been studied about the blend itself. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 25 Aug 2026with CagriSema
Inherited from a component of this blendCagriSema contains Semaglutide, and the catalogue holds a curated pair record between that component and Larazotide acetate: Semaglutide (delayed gastric emptying may alter delivery of an enteric-coated oral). Taking the blend therefore carries the same consideration as taking that component on its own, with the difference that a fixed-ratio vial cannot be adjusted independently of the rest of its contents. The evidence and citations here are the component record's; nothing has been studied about the blend itself. Peppy reports curated pharmacology, not a safety verdict. A prescriber or pharmacist should review any intended combination.
Reviewed 25 Aug 2026HUMAN EVIDENCE
This is a clean example of a positive phase 2 not surviving phase 3. A multicentre randomised double-blind placebo-controlled phase 2 trial in 342 adults on a gluten-free diet met its primary endpoint at the 0.5 mg three-times-daily dose only (p=0.022 by ANCOVA, p=0.005 by MMRM), with the higher 1 mg and 2 mg doses failing. The confirmatory phase 3 CeDLara trial at over 100 sites was discontinued in June 2022 after an interim analysis concluded that the sample size needed to detect a difference against placebo was too large to justify continuing. No positive phase 3 result exists, and the outcome has prompted reassessment of how central zonulin-mediated tight-junction dysfunction is to coeliac disease.
REPORTED EFFECTS
Tolerability in the trials was acceptable, consistent with minimal systemic absorption. The compound is not approved for any indication, and the failure of the phase 3 trial was one of futility rather than of safety.
RESEARCH LIMITATIONS
This is a source-backed summary, not a recommendation. Read the mechanism, pharmacokinetic, human-evidence and reported-effect fields separately: a mechanism is not an outcome. Availability, legal status and product quality differ by jurisdiction; consult a qualified clinician.
CURATED SOURCES · 2