Zileuton is an inhibitor of 5-lipoxygenase that exhibits anti-inflammatory, anti-asthma, anti-allergic, neuroprotective, cognition enhancing, anti-metastatic, and anticancer chemotherapeutic activities. In vitro and in vivo, zileuton inhibits release of arachidonic acid, inhibiting production of inflammatory mediators such as prostaglandins. Zileuton inhibits hyperplasia, hypertrophy, and remodeling of the extracellular matrix in animal models of chronic asthma and is thought to act through a PI3K/Akt-mediated pathway. In an animal model of cerebral ischemia/reperfusion using middle cerebral artery occlusion, zileuton inhibited increases in caspases 1 and 3, preventing neuronal apoptosis. Zileuton also displays some benefit in animal models of Alzheimer’s disease, decreasing amyloid-β (Aβ) levels and deposition, downregulating signaling by γ-secretase and phosphorylation of tau protein, and improving memory deficits.