Ligand id: 6962

Name: roflumilast

IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: roflumilast

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 1
Rotatable bonds 8
Topological polar surface area 60.45
Molecular weight 402.03
XLogP 3.52
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Roflumilast is used to treat asthma and chronic obstructive pulmonary disease (COPD) [1]. The drug reduces and prevents worsening of the lung inflammation that causes COPD.
Phase 1 proof-of-concept trials of topical roflumilast in patients with atopic dermatitis and psoriasis were withdrawn (apparently due to business decisions) before any participants were treated.
Mechanism Of Action and Pharmacodynamic Effects
Upon inhibition of phosphodiesterase-4, cAMP levels in lung cells increase in turn activating protein kinase A. This leads to inactivation of transcription factors involved in the inflammation underlying COPD.
External links