(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) with an IC50 of 1.7 nM for FLAP binding.

FLAP:1.7 nM , FLAP functional (human whole blood):45 nM

(S)-BI 665915 demonstrates significantly weaker activity in a mouse whole blood (mWB) assay compared to a human whole blood assay (mWB IC50 of 4800 nM; hWB IC50 of 45 nM). It exhibits modest human hepatocyte clearance (41% of hepatic blood flow) and high plasma protein binding (unbound fraction of 4.7%).

(S)-BI 665915 (single oral dose; 1-100 mg/kg;2 h) demonstrates dose-dependent LTB4 production inhibition in mouse whole blood . (S)-BI 665915 (iv of 1 mg/kg or po of 10 mg/kg) shows low iv plasma clearance in all three species, with clearance values of 7 % Qh in rat, 2.8 % Qh in dog, and 3.6 % Qh in cynomolgus monkey, respectively. The volume of distribution (Vss) across species tested is in a range of 0.5 to 1.2 L/kg, and the bioavailability was good (45 to 63 %) in all species tested.