.Pharmacolibrary.Drugs.R_RespiratorySystem.R03D_OtherSystemicDrugsForObstructiveAirwayDiseases.R03DX07_Roflumilast.Roflumilast

Information

Roflumilast is a selective phosphodiesterase-4 (PDE4) inhibitor used as an anti-inflammatory drug primarily in the treatment of severe chronic obstructive pulmonary disease (COPD) with a history of exacerbations. It is approved as an oral therapy to reduce the risk of COPD exacerbations.

Pharmacokinetics

Pharmacokinetic parameters in healthy adult volunteers after a single oral dose.

References

1. Li, Q, et al., & Ding, L (2017). Pharmacokinetics of Roflumilast and Its Active Metabolite Roflumilast N-Oxide in Healthy Chinese Subjects After Single and Multiple Oral Doses. European journal of drug metabolism and pharmacokinetics 42(3) 371–381. DOI:10.1007/s13318-016-0343-4 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27306372

2. Han, M, et al., & Li, JT (2023). A Single-center, Open-label, Parallel Control Study Comparing the Pharmacokinetics and Safety of a Single Oral Dose of Roflumilast and Its Active Metabolite Roflumilast N-oxide in Healthy Chinese and Caucasian Volunteers. Clinical pharmacology in drug development 12(3) 314–323. DOI:10.1002/cpdd.1209 PUBMED:https://pubmed.ncbi.nlm.nih.gov/36484261

3. Lahu, G, et al., & Facius, A (2010). Population pharmacokinetic modelling of roflumilast and roflumilast N-oxide by total phosphodiesterase-4 inhibitory activity and development of a population pharmacodynamic-adverse event model. Clinical pharmacokinetics 49(9) 589–606. DOI:10.2165/11536600-000000000-00000 PUBMED:https://pubmed.ncbi.nlm.nih.gov/20690782

Revisions

• 06/2025 initial generated model