Leukotrienes are powerful mediators of inflammation processes. Possibilities of their biosynthesis inhibition have been intensively studied during recent two decades aiming to develop new methods of therapy of various inflammatory diseases, particularly asthma. Biosynthesis of all leukotrienes is dependent on the production of the key intermediate LTA4. Transformation of arachidonic acid to LTA4 is catalyzed by the enzyme 5-lipoxygenase and facilitated by FLAP. The present paper discusses the results of recent development of new drugs in this area.