BI 665915 is a highly potent, selective, orally active 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 1.7 nM.
BI 665915 displays no activity against other enzymes and receptors in the leukotriene pathway such as 5-LO, COX-1 and -2, phospholipase A2, LTA4 hydrolase, BLT1, and BLT2 (IC50s>10 uM).
BI 665915 shows functional inhibition of LTB4 production in human whole blood (IC50=45 nM).
BI 665915 demonstrates a dose-dependent DMPK relationship and inhibition of LTB4 production in vivo.
