M ROFLUMILAST (is an active metabolite) | ROFLUMILAST | ATC D05AX06 ATC R03DX07
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 | - | PPB 97 PERCENT HT 30 HOUR | PDE4 PHOSPHODIESTERASE 4 | Phosphodiesterase 4 UNIPROT P27815 PDE4A more at DrugCentral | EMA ANSM (in French) Inxight Drugs Dailymed Drugs.com SIDER side effects Chemical Probes Portal ChEMBL BindingDB DrugBank |
ROFLUMILAST (has an active metabolite) | ROFLUMILAST | ATC D05AX06 ATC R03DX07
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 | ORAL TOPICAL | F 80 PERCENT VD 188 LITER (65 KILOGRAM) PPB 99 PERCENT Cl 9.6 LITER / HOUR HT 17 HOUR SOLUBILITY PRACTICALLY INSOLUBLE IN WATER | PDE4 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 more at DrugCentral | EMA ANSM (in French) Inxight Drugs Dailymed Drugs.com SIDER side effects Chemical Probes Portal ChEMBL BindingDB DrugBank |