Zileuton is an orally active inhibitor of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Zileuton has the chemical name (±)-1(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea and the following chemical structure:

Zileuton has the molecular formula C₁₁H₁₂N₂O₂S and a molecular weight of 236.29. It is a racemic mixture (50:50) of R(+) and S(-) enantiomers. Zileuton is a practically odorless, white, crystalline powder that is soluble in methanol and ethanol, slightly soluble in acetonitrile, and practically insoluble in water and hexane. The melting point ranges from 144.2°C to 145.2°C. ZYFLO tablets for oral administration are supplied in one dosage strength containing 600 mg of zileuton.

Inactive Ingredients: crospovidone, hydroxypropyl cellulose, hypromellose, magnesium stearate, microcrystalline cellulose, pregelatinized starch, propylene glycol, sodium starch glycolate, talc, and titanium dioxide.

Last reviewed on RxList: 6/29/2012
This monograph has been modified to include the generic and brand name in many instances.