Published : 2022-08-17

Anti-leukotriene drugs in the therapy of inflammatory diseases

Bartłomiej Pyrak

Karolina Rogacka

Dariusz Maciej Pisklak


A key part of many chronic diseases is inflammation controlled by inflammatory mediators. Regulation of their function allows to mute the inflammatory response, which is a desired effect in the treatment of inflammatory diseases. The source of mediators is arachidonic acid, converted to pro-inflammatory mediators by cyclooxygenases (COX) or lipooxygenases (LOX). The 5-LOX pathway is full of target points for regulation of biosynthesis of cysteinyl leukotrienes (CysLT) – one of the major classes of inflammatory mediators. These compounds exert their activity through specific leukotriene receptors – first (CysLT1R) and second (CysLT2R). Drugs that inhibit CysLT synthesis as well as leukotriene receptors antagonists (LTRA) form group of drugs known as anti-leukotriene drugs. Currently, only a few representatives of this group are available in the pharmacies around the world: the 5-LOX inhibitor – zileuton – and three CysLT1R antagonists – montelukast, pranlukast, zafirlukast. LTRAs due to their wide range of anti-inflammatory effects, are a group of drugs with a high potential in the treatment of inflammatory diseases. The study of new applications of known LTRAs and the search for new members of the LTRA group are the main directions of development in this field of pharmacy. This work summarizes the benefits of using anti-leukotriene drugs in the treatment od chronic diseases and presents new directions of using LTRAs.


cysteinyl leukotrienes, antagonism, anti-leukotriene drugs, COVID-19, mutations

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Pyrak, B., Rogacka, K., & Pisklak, D. M. (2022). Anti-leukotriene drugs in the therapy of inflammatory diseases. Prospects in Pharmaceutical Sciences, 20(2), 1–23.

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