Roflumilast

Roflumilast

Clinical data
Trade names	Daxas,Daliresp
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a611034
License data	EU EMA: Daxas US FDA: Roflumilast
Pregnancy category	AU: B3 US: C (Risk not ruled out)
Routes of administration	Oral
ATC code	R03DX07 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	79%
Protein binding	99%
Metabolism	Hepatic via CYP1A2 & CYP3A4
Biological half-life	17 hours (30 hours [active metabolite])
Excretion	Urine (70%)
Identifiers
IUPAC name 3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
CAS Number	162401-32-3 N
PubChem CID	449193
IUPHAR/BPS	6962
ChemSpider	395793 N
UNII	0P6C6ZOP5U
ChEBI	CHEBI:47657 N
ChEMBL	CHEMBL193240 N
ECHA InfoCard	100.210.960
Chemical and physical data
Formula	C17H14Cl2F2N2O3
Molar mass	403.207 g/mol
3D model (Jmol)	Interactive image
SMILES C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
InChI InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24) N Key:MNDBXUUTURYVHR-UHFFFAOYSA-N N
NY (what is this?)

Roflumilast (trade names Daxas, Daliresp) is a drug that acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). It has anti-inflammatory effects and is used as an orally administered drug for the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease (COPD).

In June 2010, Daxas was approved in the EU for severe COPD associated with chronic bronchitis. In March 2011, Daliresp gained FDA approval in the US for reducing COPD exacerbations.

Its primary clinical use is in the prevention of exacerbations (lung attacks) in severe COPD.

Common (1–10% incidence) adverse effects include: