Independent · non-commercial · publishes on a quarterly cycle|Current cycle 2026 Q3
Compound Evidence InstituteEvidence synthesis · established 2023Graded assessments of compounds, trials, methods and supply
Document set current to 30 July 2026
Compound monograph · Repair and regeneration

Larazotide acetate — compound monograph

Octapeptide tight-junction regulator (zonulin antagonist). Discontinued. The Institute assesses 1 outcome for this compound and grades the strongest at moderate certainty.

Document identifier
CEI-MN-035
Series
Compound monograph
Version
4.3
Published
07 May 2026
Last reviewed
07 May 2026
Next review
07 May 2028
Identifier
10.71829/cei.mono.35
Certainty
Moderate
Cycle
2026 Q2

§1Identification and status

§1.1Nomenclature

Preferred name
Larazotide acetate
Compound class
Octapeptide tight-junction regulator (zonulin antagonist)
Assessment series
Repair and regeneration
Synonyms and codes
AT-1001 · INN-202 · larazotide (INN)
Route as evaluated
Oral, before meals

§1.2Chemistry

Chemical identifiers are reproduced where they are public. Where a structure has not been published the monograph records not disclosed rather than constructing one.[1]

CAS registry number
258818-34-7
Molecular formula
C33H55N7O11
Average mass
725.83
Monoisotopic mass
725.40
ATC classification
not assigned

§1.3Sequence and structural notes

H-Gly-Gly-Val-Leu-Val-Gln-Pro-Gly-OH

An octapeptide derived from the Vibrio cholerae zonula occludens toxin. It acts locally in the intestinal lumen and is not intended to be systemically absorbed, which makes it pharmacologically unusual and analytically straightforward.

§1.4Assessment status

The Institute assesses Larazotide acetate across 1 indication and grades the strongest of them at moderate certainty. Clinical development was terminated. The Institute treats a discontinued programme as evidence.

Distribution of certainty ratingsShare of assessed outcomes at each certainty level.1assessed outcomes
HighModerateLowVery low
Figure 1. Distribution of certainty ratings across the 1 outcome the Institute assesses for Larazotide acetate. A rating attaches to a specific population, comparator and outcome and does not transfer between them.

Table 1. Assessed outcomes for Larazotide acetate, ordered by certainty. Each row links to the per-indication evidence extract.

IndicationEffect as recordedCertaintyTrials
Inflammatory bowel disease and mucosal barrier disordersA phase 2b trial met its primary endpoint on symptom scores at the 0.5 mg dose; the subsequent phase 3 trial was discontinued for futility at interim…Moderate2
Effects are reproduced as the contributing trials reported them. Where a confidence interval is held it appears on the per-indication extract rather than in this summary table.

References cited on this page

References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.

  1. International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use. ICH Q6B Specifications: Test Procedures and Acceptance Criteria for Biotechnological/Biological Products. ICH Harmonised Tripartite Guideline 1999;Step 4 version. identifier not held by the Institute

Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.

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