BMS-587101

BMS-587101 is a potent and orally active small molecule antagonist of leukocyte function-associated antigen 1 (LFA-1), also known as integrin alpha-L/beta2 (ITGAL/ITGB2). It was developed by Bristol Myers Squibb for its anti-inflammatory properties and has demonstrated efficacy in preclinical models of autoimmune and inflammatory diseases such as rheumatoid arthritis. The drug works by selectively blocking the binding of LFA-1 to its ligand ICAM-1 on endothelial cells. This inhibition reduces T cell adhesion to endothelium, T cell proliferation in response to antigen stimulation (MLR), and Th1 cytokine production. In animal models of antibody-induced and collagen-induced arthritis, oral administration of BMS-587101 significantly reduced inflammation and joint destruction compared to controls[2][5][7]. Despite promising preclinical results for immune-mediated diseases like rheumatoid arthritis and psoriasis[3], development was discontinued after reaching phase 2 clinical trials.

Other names

5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl]methyl]-3-thiophenecarboxylic acid