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BIIL-260 is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with the Ki value of 1.7 nM[1].

BIIL260 is a selective and potent leukotriene B4 (BLT1) receptor antagonist with a Ki value of 1.8 nM in human U937 cells. BIIL260 was used found to act as an inverse agoniststabilizing the inactive state of BLT1.

[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