e-Drug3D
1510
cas 162401-32-3
CLASS
RESPIRATORY
CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
PHOSPHODIESTERASE PDE4 INHIBITORS
ROFLUMILAST IS THREE TIMES MORE POTENT THAN ROFLUMILAST N-OXIDE AT INHIBITION OF THE PDE4 ENZYME IN VITRO THE PLASMA AUC OF ROFLUMILAST N-OXIDE ON AVERAGE IS ABOUT 10-FOLD GREATER THAN THE PLASMA AUC OF ROFLUMILAST
ROUTE (list)
ORAL TOPICAL
PK parameters
F 80 PERCENT
VD 188 LITER (65 KILOGRAM)
Cl 9.6 LITER / HOUR
PPB 99 PERCENT
t1/2 17 HOUR
Solubility
PRACTICALLY INSOLUBLE IN WATER
TARGET PDE4
PHOSPHODIESTERASE 4
PHOSPHODIESTERASE 4
PDB
1XMU (CATALYTIC DOMAIN OF HUMAN PHOSPHODIESTERASE 4B IN COMPLEX WITH ROFLUMILAST)
Ligand code = ROF (link to the list of PDB complexes)
Download experimental 3D coordinates of ROF with added hydrogens
Phosphodiesterase 4 UNIPROT P27815 PDE4A
Formula:
C17H14Cl2F2N2O3
Calculated chemical properties:
MW 403.20
NB_atoms 26
XLogP 5.03
PSA 58.075
NB_HD 1
NB_HA 5
fsp3 0.29
Lipinski(0=no;1=yes) 0
NB_atoms 26
XLogP 5.03
PSA 58.075
NB_HD 1
NB_HA 5
fsp3 0.29
Lipinski(0=no;1=yes) 0
FDA
NDA 022522 (pdf not found) INN (ROFLUMILAST) DALIRESP (ASTRAZENECA) APPROVAL= AP YEAR= 2011
NDA 208257 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (PHARMOBEDIENT) APPROVAL= AP YEAR= 2018
NDA 208213 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (HETERO LABS LTD III) APPROVAL= AP YEAR= 2018
NDA 208236 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (SENORES PHARMS) APPROVAL= AP YEAR= 2018 DISCONTINUED
NDA 208272 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (TORRENT) APPROVAL= AP YEAR= 2018
NDA 208180 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (MICRO LABS) APPROVAL= AP YEAR= 2019
NDA 208247 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (STRIDES PHARMA) APPROVAL= AP YEAR= 2020
NDA 208256 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (MSN) APPROVAL= AP YEAR= 2022
NDA 208299 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (PRINSTON INC) APPROVAL= AP YEAR= 2022
NDA 208303 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (ZYDUS PHARMS) APPROVAL= AP YEAR= 2022
NDA 215985 (pdf not found) INN (ROFLUMILAST) ZORYVE (ARCUTIS) APPROVAL= AP YEAR= 2022
NDA 212490 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (ALKEM LABS LTD) APPROVAL= AP YEAR= 2023
NDA 213298 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2023
NDA 217242 (pdf not found) INN (ROFLUMILAST) ZORYVE (ARCUTIS) APPROVAL= AP YEAR= 2023
NDA 022522 (pdf not found) INN (ROFLUMILAST) DALIRESP (ASTRAZENECA) APPROVAL= AP YEAR= 2011
NDA 208257 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (PHARMOBEDIENT) APPROVAL= AP YEAR= 2018
NDA 208213 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (HETERO LABS LTD III) APPROVAL= AP YEAR= 2018
NDA 208236 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (SENORES PHARMS) APPROVAL= AP YEAR= 2018 DISCONTINUED
NDA 208272 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (TORRENT) APPROVAL= AP YEAR= 2018
NDA 208180 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (MICRO LABS) APPROVAL= AP YEAR= 2019
NDA 208247 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (STRIDES PHARMA) APPROVAL= AP YEAR= 2020
NDA 208256 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (MSN) APPROVAL= AP YEAR= 2022
NDA 208299 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (PRINSTON INC) APPROVAL= AP YEAR= 2022
NDA 208303 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (ZYDUS PHARMS) APPROVAL= AP YEAR= 2022
NDA 215985 (pdf not found) INN (ROFLUMILAST) ZORYVE (ARCUTIS) APPROVAL= AP YEAR= 2022
NDA 212490 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (ALKEM LABS LTD) APPROVAL= AP YEAR= 2023
NDA 213298 (pdf not found) INN (ROFLUMILAST) ROFLUMILAST (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2023
NDA 217242 (pdf not found) INN (ROFLUMILAST) ZORYVE (ARCUTIS) APPROVAL= AP YEAR= 2023