TAS-203

TAS-203 is a novel **benzimidazole derivative** that functions as a selective **phosphodiesterase 4 (PDE4) inhibitor**. It belongs to the dialkoxyphenyl (catechol) family of PDE4 inhibitors and represents a second-generation compound designed to separate therapeutic anti-inflammatory effects from emetogenic side effects. The drug demonstrates potent anti-inflammatory activities with significantly **reduced emetogenic potential** compared to other PDE4 inhibitors like cilomilast and rolipram. TAS-203 shows poor brain distribution after oral administration, which contributes to its lower central nervous system-related side effects. The compound has been developed for the treatment of **airway inflammatory diseases** such as asthma and chronic obstructive pulmonary disease (COPD), with particular effectiveness against airway inflammation, mucus hypersecretion, and airway hyperresponsiveness.

Other names

2-[3-(cyclopropylmethoxy)-4-methoxyphenyl]-5-(1H-1,2,4-triazol-1-yl)-1H-benzimidazole