gemilukast

Gemilukast (ONO-6950) is an orally active small molecule drug developed as a dual antagonist of the cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2). It exhibits potent inhibitory activity with IC50 values of 1.7 nM for human CysLT1 and 25 nM for human CysLT2. Gemilukast was designed to block both receptor subtypes involved in bronchoconstriction and airway inflammation, mechanisms implicated in asthma pathophysiology. Preclinical studies demonstrated its efficacy in reducing bronchoconstriction induced by leukotrienes in animal models, as well as antigen-induced constriction of isolated human bronchi. The drug was evaluated up to phase II clinical trials for the treatment of asthma but development was discontinued after phase II[1][2][3][5][7].

Brand names

Gemilukast

Other names

gemilukast1232861-58-3UNII-42I6GGX6D6UNII42I6GGX6D6UNII 42I6GGX6D6