Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease.