Amelubant (BIIL 284) is a potent, oral and long acting LTB4 receptor antagonist, negligibly binds to LTB4 receptor, with Kis of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a proagent of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity[1].
LTB4: 221 nM (Ki, in vital human granulocytes); LTB4: 230 nM (Ki, in cell membranes)
[1] Birke FW, et al. In vitro and in vivo pharmacological characterization of BIIL 284, a novel and potent leukotriene B(4) receptor antagonist. J Pharmacol Exp Ther. 2001 Apr;297(1):458-66. PMID:11259574
