AMG487

AMG487 is a potent and selective small molecule antagonist of the chemokine (C-X-C motif) receptor 3 (CXCR3). It is an orally bioavailable 8-azaquinazolinone derivative that prevents chemokines CXCL9, CXCL10, and CXCL11 (notably CXCL10/IP-10 and CXCL11/ITAC) from binding to CXCR3 and thereby inhibits chemotaxis of immune cells to sites of inflammation. AMG487 has demonstrated extensive selectivity for CXCR3 over other chemokine receptors, modulates inflammatory processes, and has shown efficacy in preclinical models of autoimmune and inflammatory diseases, including rheumatoid arthritis, experimental autoimmune uveitis, and models of graft-versus-host disease. It was developed primarily for autoimmune/inflammatory diseases such as psoriasis and rheumatoid arthritis, where it reached Phase II clinical trials but was discontinued due to lack of clinical efficacy. Research continues in other indications, particularly autoimmune and transplantation-related disorders, primarily in preclinical or translational settings[1][5][8][9][2][3][4][7].

Other names

AMG487AMG-487AMG 487T487T-487T 487