Ensifentrine (E1566-GRP)

Ensifentrine (RPL-554) is a first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50 values of 0.4 nM and 1479 nM, respectively. Ensifentrine also inhibits lipopolysaccharide-induced tumor necrosis factor alpha release from human monocytes in a concentration-dependent manner. Ensifentrine demonstrates bronchoprotective and anti-inflammatory activities and can be used for chronic obstructive pulmonary disease (COPD) research.