Zileuton

Zileuton (trade name ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. Zileuton inhibits antigen-induced contraction of tracheal strips in vitro (IC50 = 6 μM) and exhibits antiasthmatic activity in vivo. Zileuton also weakly inhibits CYP1A2 (Ki = 66 - 98 μM). Zileuton is used for the maintenance treatment of asthma. Research on mice suggests that Zileuton used alone or in combination with imatinib may inhibit chronic myeloid leukemia (CML).