Megan Pane1, Curtis Johnston1∗, Rena Eudy-Byrne1, Tyler Dunlap1, Nikolas Onufrak2∗, Sonja Hartmann2∗, Steve Choy21Metrum Research Group, Boston, MA, U.S.A.,2Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT, U.S.A.
∗Affiliation during time of analysis
Mechanism of Action
• Nerandomilast (JASCAYD®) is an orally administered, preferential inhibitor of the
phosphodiesterase-4B (PDE4B) isoenzyme
• PDE4B hydrolyzes and inactivates cyclic adenosine monophosphate
Therapeutic Indication
• Approved by the U.S. FDA and China’s CDE for the treatment of idiopathic pul-
monary fibrosis (IPF) and progressive pulmonary fibrosis (PPF)
• IPF is a specific type of interstitial lung disease (ILD) and PPF is associated with a
subset of ILDs distinct from IPF
• Both IPF and PPF lead to lung scarring that progresses over time, with a median
survival time of 3-5 years
Chemical and Metabolic Properties
• Nerandomilast (R-enantiomer) contains a chiral sulfoxide group and undergoes a
minor level of metabolic chiral inversion following oral administration
• The resulting S-enantiomer is pharmacologically inactive
• Both nerandomilast and the S-enantiomer were characterized in this analysis