IBD3540

IBD3540 is a novel, gut-restricted, small molecule inhibitor of glutamate carboxypeptidase II (GCPII) designed for the oral treatment of inflammatory bowel disease (IBD). GCPII is significantly overexpressed in the inflamed intestinal mucosa of patients with Crohn’s disease and ulcerative colitis. IBD3540 is a conjugate of the GCPII inhibitor 2-PMPA and the secondary bile acid deoxycholic acid, a design intended to limit systemic absorption and focus activity within the gastrointestinal tract. In preclinical studies, it has demonstrated potent anti-inflammatory activity in both acute (DSS-induced) and chronic (IL10-/-) mouse colitis models, reducing pro-inflammatory cytokines such as TNF-alpha, IL-12p40, and IL-17. It has shown superior efficacy compared to standard-of-care agents like sulfasalazine and tofacitinib in head-to-head mouse model comparisons.

Other names

deoxycholic acid 2-PMPA conjugate