5-lipoxygenase activating protein (FLAP) is essential for the activity of 5-LO, the key first step in leukotriene biosynthesis. AZD5718 is a novel oral FLAP inhibitor aiming to reduce cardiovascular mortality and morbidity in coronary artery disease (CAD) patients by attenuation of proinflammatory and vasoactive leukotriene production.<br/>The recently concluded Phase 1 study demonstrates that AZD5718 is safe & tolerated, with a pharmacokinetics amenable for QD oral dosing. Paired with dose dependent & potent target engagement on both arms of the 5-LO pathway, the Phase 2a study started 2017.<br/>Herein we will disclose the medicinal chemistry discovery and development of AZD5718 which entirely originates from a novel chemical series

Discovery of AZD5718, a novel 5-lipoxygenase activating protein (FLAP) inhibitor

256th National Meeting (2018)

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