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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
LUMACAFTOR

LUMACAFTOR


ATC R07AX30

RESPIRATORY SYSTEM
CYSTIC FIBROSIS
POTENTIATOR
IMPROVES THE CONFORMATIONAL STABILITY OF F508DEL-CFTR RESULTING IN INCREASED PROCESSING AND TRAFFICKING OF MATURE PROTEIN TO THE CELL SURFACE

ORAL

Cmax 55.3 MICROMOLAR

Tmax 4 HOUR

VD 86 LITER

PPB 99 PERCENT

Cl 2.38 LITER / HOUR

HT 25.2 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN WATER

CFTR CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

PDB 7SVD (THE COMPLEX OF PHOSPHORYLATED HUMAN CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) WITH ATP, MG AND LUMACAFTOR (VX-809))

LIGAND CODE = VX8 (link to the list of PDB complexes)

Download experimental 3D coordinates of VX8 with added hydrogens

Cystic fibrosis transmembrane conductance regulator UNIPROT P13569 CFTR

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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