GL1001

GL1001 is a potent and selective small molecule inhibitor of angiotensin-converting enzyme 2 (ACE2). Developed by Genzyme, it was primarily explored as a potential therapeutic for inflammatory bowel disease (IBD). ACE2 is an enzyme within the renin-angiotensin system (RAS) that is highly expressed in the gastrointestinal tract and plays a role in regulating inflammation. In preclinical studies using mouse models of dextran sodium sulfate (DSS)-induced colitis, subcutaneous administration of GL1001 significantly reduced intestinal inflammation and disease activity, showing efficacy comparable to the standard treatment sulfasalazine. Despite these promising preclinical results, the compound has not advanced into human clinical trials and remains a research tool.