Nerandomilast | PDE4B inhibitor

Nerandomilast chemical structure

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Nerandomilast (1423719-30-5) is a potent and selective inhibitor of phosphodiesterase 4B (IC50’s: PDE4A = 248 nM, PDE4B = 10 nM, PDE4C = 8,700 nM, PDE4D = 91 nM, PDE7A = 14 µM, PDE3A = 120 µM, PDE1C = 46 µM).1 It inhibited TNFα release (IC50 = 35 nM) and IL-2 release (IC50 = 9 nM) in human PBMCs. Nerandomilast has potent anti-inflammatory activity and displayed efficacy in mouse models of lung fibrosis.1,2 Approved for the treatment of idiopathic pulmonary fibrosis.

References/Citations:

  1. Herrmann et al. (2022)BI 1015550 is a PDE4B Inhibitor and a Clinical Drug Candidate for the Oral Treatment of Idiopathic Pulmonary Fibrosis, Front. Pharmacol., 13 838449
  2. Reininger et al. (2024)PDE4B inhibition by nerandomilast: Effects on lung fibrosis and transcriptome in fibrotic rats and on biomarkers in human lung epithelial cells, Br. J. Pharmacol., 181 4766
1423719-30-5, BI 1015550, BI1015550, nerandomilast, Nerandomilast supplier, PDE4B inhibitor, selective PDE4B inhibitor
Alternate Name:
BI 1015550

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Nerandomilast (1423719-30-5) is a potent and selective inhibitor of phosphodiesterase 4B (IC50’s: PDE4A = 248 nM, PDE4B = 10 nM, PDE4C = 8,700 nM, PDE4D = 91 nM, PDE7A = 14 µM, PDE3A = 120 µM, PDE1C = 46 µM).1 It inhibited TNFα release (IC50 = 35 nM) and IL-2 release (IC50 = 9 nM) in human PBMCs. Nerandomilast has potent anti-inflammatory activity and displayed efficacy in mouse models of lung fibrosis.1,2 Approved for the treatment of idiopathic pulmonary fibrosis.

References/Citations:

  1. Herrmann et al. (2022)BI 1015550 is a PDE4B Inhibitor and a Clinical Drug Candidate for the Oral Treatment of Idiopathic Pulmonary Fibrosis, Front. Pharmacol., 13 838449
  2. Reininger et al. (2024)PDE4B inhibition by nerandomilast: Effects on lung fibrosis and transcriptome in fibrotic rats and on biomarkers in human lung epithelial cells, Br. J. Pharmacol., 181 4766