Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, possessing anti-inflammatory activities.

In cells treated with anti-CD3, IL-2 levels decrease over time both in the presence and absence of Zileuton sodium (A 64077 sodium). Zileuton sodium may reduce IL-2 concentrations by inhibiting 5-lipoxygenase, thereby decreasing leukotriene B4 production, which is known to induce IL-2 [2].

In rats undergoing ischemia/reperfusion (I/R), treatment with Zileuton sodium (A 64077 sodium) (5 mg/kg, p.o.) does not significantly alter NF-κB expression levels in the presence of COX inhibitors, yet it notably decreases NF-κB staining. This same dosage of Zileuton significantly lowers the apoptotic index in I/R rats, though it doesn't affect raised serum TNF-α levels [1]. Additionally, at a dosage of 1200 mg/kg, Zileuton sodium effectively inhibits polyp formation in the APC Δ468 mutation of the colon and small intestine. It reduces proliferation rates of non-epithelial cells in polyps while elevating apoptosis rates, leading to a significant increase in apoptotic cell numbers in both sites. This reduction in cell proliferation contributes substantially to the decreased polyposis in the small intestine and colon of Zileuton-fed APC Δ468 mice [3].