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We evaluated safety, tolerability, pharmacokinetics, and pharmacodynamics of AZD5718, a novel 5‐lipooxygenase activating protein (FLAP) inhibitor, in a randomized, single‐blind, placebo‐controlled, first‐in‐human (FIH) study consisting of single and multiple ascending dosing (SAD and MAD) for 10 days in healthy subjects. Target engagement was measured by  ex vivo  calcium ionophore stimulated leukotriene B (LTB 4 ) production in whole blood and endogenous leukotriene E (LTE 4 ) in urine. No clinically relevant safety and tolerability findings were observed. The AZD5718 was rapidly absorbed and plasma concentrations declined biphasically with a mean terminal half‐life of 10–12 h. Steady‐state levels were achieved after ∼3 days. After both SADs and MADs, a dose/concentration‐effect relationship between both LTB 4  and LTE 4  vs. AZD5718 exposure was observed with concentration of half inhibition (IC 50 ) values in the lower nM range. Based on obtained result, AZD5718 is considered as a suitable drug candidate for future evaluation in patients with coronary artery disease (CAD).

Initial Clinical Experience with AZD5718, a Novel Once Daily Oral 5‐Lipoxygenase Activating Protein Inhibitor