bi 1021958

BI 1021958 is a novel antagonist of the chemoattractant-receptor-homologous molecule (CRTH2), developed for the oral treatment of asthma. It targets airway inflammation in asthma by inhibiting prostaglandin binding to CRTH2 receptors. The drug has been evaluated in phase 1 clinical trials for safety, tolerability, pharmacokinetics, and pharmacodynamics in both healthy subjects and patients with well-controlled asthma. Adverse events were infrequent and generally mild to moderate. Maximum plasma concentration was achieved within ≤2.5 hours after single doses and ≤2 hours after multiple doses; exposure increased proportionally with dose[1][3]. After ≥60 mg single doses or >40 mg multiple doses, >95% inhibition of eosinophil shape change was observed for ≥24 hours[1][3].