PF-07054894

PF-07054894 is an orally active, potent, and selective small molecule antagonist of the C-C chemokine receptor type 6 (CCR6), a G protein-coupled receptor involved in the migration of pathogenic lymphocytes and dendritic cells to sites of inflammation. It acts as an insurmountable antagonist at CCR6, blocking CCR6-mediated chemotaxis with high potency (IC50 = 5.7 nM in vitro) and functional selectivity over related receptors such as CCR7 and CXCR2[1][2][5][6]. Developed by Pfizer, PF-07054894 is being investigated primarily for the treatment of inflammatory bowel disease, particularly ulcerative colitis. The drug has completed Phase 1 studies in healthy volunteers and is currently in Phase 1 clinical trials for ulcerative colitis[2][4][8]. Its mechanism involves inhibiting T cell migration mediated by CCL20/CCR6 signaling both in vitro and in vivo[5][6].