lirimilast

Lirimilast (BAY 19-8004) is a selective, orally active phosphodiesterase-4 (PDE4) inhibitor developed by Bayer for the treatment of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). PDE4 is the predominant enzyme responsible for the hydrolysis of cyclic adenosine monophosphate (cAMP) in inflammatory cells; by inhibiting this enzyme, lirimilast increases intracellular cAMP levels, which leads to the suppression of inflammatory mediator release and potential bronchodilation. Clinical evaluation of lirimilast showed that while it could reduce certain inflammatory markers in the sputum of COPD patients, it did not significantly improve lung function (FEV1) or reduce total sputum cell counts in short-term trials. Development was eventually discontinued, a common outcome for early-generation PDE4 inhibitors due to limited clinical efficacy and dose-limiting side effects like nausea.

Other names

lirimilastBAY 19-8004BAY19-8004BAY-19-8004