Pulmonary

In vitro and cell culture studies identified a dual-acting PDE-4 inhibitor/ADRB2 agonist that could help treat COPD. In in vitro activity assays, a quinolone analog conjugated to a PDE-4 inhibitor tool compound inhibited human PDE-4B activity with an IC₅₀ of 1.38 nM. In human lung endothelial cell-based activity assays, the compound agonized ADRB2 with an EC₅₀ of 39 pM. In a human lung endothelial cell line, the compound increased expression of anti-inflammatory genes compared with vehicle, and produced a comparable gene expression profile to that produced by combination of another PDE-4 inhibitor tool compound and the ADRB2 agonist Arcapta indacaterol. Next steps could include testing the dual-acting compound in animal models of COPD.

Novartis AG markets Arcapta Neohaler to treat COPD...