TA-270

TA-270 is an orally active quinolinone small-molecule anti-inflammatory agent with dual 5-lipoxygenase inhibitory and antioxidant, peroxynitrite-scavenging activity, developed primarily for chronic obstructive pulmonary disease (COPD) and neutrophilic asthma. It was rationally designed by combining structural features of ascorbic acid and aspirin and incorporating sinapinic acid, a component of the traditional medicine Saibokuto, to enhance free radical scavenging and leukotriene-modulating properties.[1][3] Preclinical studies show TA-270 potently inhibits 5-lipoxygenase–mediated leukotriene production in mast cells, neutrophils, and eosinophils while sparing cyclooxygenase pathways, and it reduces airway hyperresponsiveness and biphasic asthmatic and allergic rhinitis responses in guinea pig models, largely via suppression of peroxynitrite-induced oxidative stress and inflammatory cell recruitment.[1][5][9] Clinically, TA-270 has been evaluated in multiple Phase 1 and Phase 2 trials (over 700 subjects) as an oral tablet for COPD and neutrophilic asthma, with exploratory work in cystic fibrosis and allergic airway disease, and has shown a safety profile favorable compared with other oral anti-inflammatory drugs.[1][3][7]

Other names

4-hydroxy-1-methyl-3-octyloxy-7-sinapinoylamino-2(1H)-quinolinone