Roflumilast (BY217; B 9302107; BYK-20869; Daxas; Daliresp)

Description: Roflumilast (BY-217; APTA-2217; B 9302-107; BYK20869; Daxas; Daliresp) is a novel, highly potent, selective, and long-acting inhibitor of phosphodiesterase 4/PDE4 with potential anti-inflammatory activity. It inhibits PDE4 with IC50s of 0.2-4.3 nM in a cell-free assay. It has anti-inflammatory effects and is under development as an orally administered drug for the treatment of inflammatory conditions of the lungs such as asthma, and chronic obstructive pulmonary disease (COPD). In vitro studies show that roflumilast inhibits the production of inflammatory mediators in a variety of human immune cells, suggesting a role for reducing COPD-related inflammation.

References: Pulm Pharmacol Ther. 2010 Aug; 23(4):235-56; J Pharmacol Exp Ther. 2001 Apr; 297(1):267-79.

Related CAS: 292135-78-5 (Roflumilast N-oxide); 1391052-76-8 (Roflumilast Impurity E)