Background: The involvement of intercellular tight junctions and, in particular, the modulation of their
competency by the zonulin pathway with a subsequent increase in epithelial and endothelial permeability, has been
described in several chronic and acute inflammatory diseases. In this scenario, Larazotide, a zonulin antagonist, could be
employed as a viable therapeutic strategy.
Objective: The present review aims to describe recent research and current observations about zonulin involvement in
several diseases and the use of its inhibitor Larazotide for their treatment.
Methods: A systematic search was conducted on PubMed and Google Scholar, resulting in 209 publications obtained with
the following search query: “Larazotide,” “Larazotide acetate,” “AT-1001,” “FZI/0” and “INN-202.” After careful
examination, some publications were removed from consideration because they were either not in English or were not
directly related to Larazotide.
Results: The obtained publications were subdivided according to Larazotide’s mechanism of action and different diseases:
celiac disease, type 1 diabetes, other autoimmune diseases, inflammatory bowel disease, Kawasaki disease, respiratory
(infective and/or non-infective) diseases, and other.
Conclusions: A substantial role of zonulin in many chronic and acute inflammatory diseases has been demonstrated in both
in vivo and in vitro, indicating the possible efficacy of a Larazotide treatment. Moreover, new possible molecular targets for
this molecule have also been demonstrated.