Nerandomilast

Nerandomilast is an inhibitor of phosphodiesterase 4B (PDE4B. IC50 = 0. µM). It is selective for PDE4B over PDE4A, PDE4C, and PDE4D (IC50s = 0. 8. and 0. µM, respectively), PDE7A, PDE3A, PDE1C, and PDE9A (IC50s = 14, 120, 46, and >100 µM, respectively), and does not inhibit PDE2A, PDE5, or PDE6. Nerandomilast inhibits LPS-induced TNF-alpha release and phytohemagglutinin P-induced IL-2 release in isolated human peripheral blood mononuclear cells (PBMCs. IC50s = 0. and 0. µM, respectively). It exhibits a lower emetic potential than roflumilast (Cay-15141) in Asian house shrews. Nerandomilast (12. mg/kg) reduces decreases in forced vital capacity and static lung volume in a mouse model of pulmonary fibrosis bleomycin-induced. Formulations containing nerandomilast have been used in the treatment of idiopathic pulmonary fibrosis.