zotemtegrast

Zotemtegrast (LY3534651) is an investigational, oral small molecule antagonist of the α4β7 integrin, currently under development by Eli Lilly for the treatment of inflammatory bowel diseases (IBD), including ulcerative colitis and Crohn's disease. By selectively inhibiting the α4β7 integrin, zotemtegrast blocks its interaction with mucosal addressin cell adhesion molecule-1 (MAdCAM-1), which is primarily expressed on the vascular endothelium of the gastrointestinal tract. This mechanism prevents the migration of pro-inflammatory T-lymphocytes into the gut mucosa, thereby reducing intestinal inflammation. As an oral therapy, zotemtegrast aims to provide a more convenient alternative to existing injectable α4β7 inhibitors, such as vedolizumab, and is being studied both as a monotherapy and in combination with other biologics like mirikizumab.

Other names

(s)-3-((s)-2-(5-(2-(dimethylamino)ethyl)-2-oxo-4-(trifluoromethyl)pyridin-1(2h)-yl)-4-methylpentanamido)-3-(4-fluoro-2',4',5,6'-tetramethyl-[1,1'-biphenyl]-3-yl)propanoic acid