Latest research on Zafirlukast

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), which is usually taken just once daily. Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.

Latest findings

LTRAs (Montelukast, pranlukast, and Zafirlukast) mostly antagonize cysLT1 receptor only, but 5-LO inhibitor (Zileuton) can inhibit the production of all the leukotrienes including cysLT and LTB4 [62]. [source, 2016]
In the 4-week open-label ACCEPT (Accolate Clinical Experience and Pharmacoepidemiology) trial involving 3,700 asthma patients, the addition of zafirlukast provided clinical improvement in asthma patients as overall, but the clinical effect was less evident in the elderly, compared to younger patients [71]. [source, 2016]
Also in a retrospective pooled analysis of 5 RCTs comparing Zafirlukast to Fluticasone as monotherapy, the effects of Zafirlukast appeared to be lost in older adults (aged ≥50 years) [72]. [source, 2016]
LTRAs such as Montelukast or Zafirlukast have shown significant clinical efficacy in improving cough and/or capsaicin cough sensitivity among patients with cough variant asthma or non-asthmatic eosinophilic bronchitis [102–105]. [source, 2015]
In 1990, three new medicines produced, which are used in asthma treatment: Antagonists of leukotriene receptor Zafirlukast (8), Montelukast (9), and inhibitor of the leukotriene synthesis such Zileuton (10). [source, 2015]
Zafirlukast and Montelukast are selective competitive antagonists with high affinity for the receptor cys-LT1 (9). [source, 2015]
Maybe, it is worth to mention that Zafirlukast inhibits substantially also the manifestation of basophils and lymphocytes in airways after experimental exposure of asthmatic people to an Allergen (12). [source, 2015]
In clinical trials with Zafirlukast, all studies indicated some decrease in the number of asthma exacerbations, with average of reduction to 50% (13). [source, 2015]
When Zafirlukast (14) and Montelukast (15) compared with the low dose therapy of inhaled glucocorticoids, improvement in pulmonary function and in the need to reduce the administration of therapy with β2 adrenergic agonists was higher at patients treated with glucocorticoids. [source, 2015]
Zafirlukast and Montelukast, antagonists of leukotriene receptor, today are administered in treatment of bronchial asthma. [source, 2015]