sibofimloc

Sibofimloc is a first-in-class, orally administered, gut-restricted small molecule FimH-blocker developed for the treatment of Crohn’s disease. It selectively binds to and aggregates FimH-expressing pathogenic bacteria (notably certain Enterobacteriaceae such as adherent-invasive Escherichia coli) in the gut. By blocking the adhesion of these bacteria to the intestinal wall and inhibiting their interaction with human TLR4 receptors on epithelial cells, sibofimloc reduces pro-inflammatory cytokine production (including TNF alpha) and suppresses intestinal inflammation without disrupting the overall composition of the gut microbiota. Sibofimloc is being developed under a global licensing and co-development partnership between Enterome and Takeda. It has demonstrated good tolerability in Phase 1 studies with minimal systemic absorption and is currently in Phase 2 clinical trials for prevention of postoperative recurrence in Crohn’s disease[3][5][6][7][8][9].

Other names

1616113-45-1sibofimloc [INN]