Leukotrienes (LTs) belong to pro-inflammatory mediators that are biosynthesized from arachidonic acid (AA), inter alia, by 5-lipoxygenase (5-LOX) enzyme in association with 5-LOX-activating protein (FLAP). An activation of LTs synthesis pathway occurs during the development and maintenance of numerous diseases such as asthma, anaphylactic shock, allergic rhinitis, psoriasis, rheumatoid arthritis, osteoporosis, as well as cardiovascular diseases, neurodegenerative diseases and certain types of cancer. The main goal of this review was to present recent advances on the new compounds influencing the LOX pathway, which are under-going clinical studies. The mechanisms of action and possible implementations of these molecules in a treatment of asthma, cancer and cardiovascular diseases are discussed.