israpafant

Israpafant (Y-24180) is a potent, selective, and long-acting antagonist of the platelet-activating factor receptor (PAFR). It was originally developed for the treatment of asthma. Israpafant belongs to the thienotriazolodiazepine chemical class and is structurally related to benzodiazepines such as etizolam but exhibits much higher affinity for PAFR and only weak binding to benzodiazepine receptors. Its mechanism involves inhibition of PAF-induced human platelet aggregation with an IC50 of 0.84 nM, suppression of eosinophil activation, reduction in interleukin 5 (IL-5) and IL-4 production by Th2 cells, and modulation of calcium transport in certain cell types. Preclinical studies demonstrated its efficacy in suppressing immediate asthmatic responses in animal models, while clinical trials showed improvement in bronchial hyperresponsiveness among asthma patients[1][2][3][4][5][7][8].

Other names

Y 24180Y24180Y-24180