e-Drug3D

1929

ERDAFITINIB


INN
ERDAFITINIB

cas 1346242-81-6
CLASS

ANTINEOPLASTIC
FGFR1, FGFR2, FGFR3 AND FGFR4 KINASE INHIBITOR
TREATMENT OF ADVANCED OR METASTATIC UROTHELIAL CARCINOMA
ALSO BINDS TO RET, CSF1R, PDGFRA, PDGFRB, FLT4, KIT AND VEGFR2

ROUTE (list)

ORAL

ATC code

L01EN01

PK parameters

Tmax 2.5 HOUR
VD 29 LITER
Cl 0.362 LITER / HOUR
PPB 99.8 PERCENT
t1/2 59 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER


Target

TARGET FGFR1
FGFR2
FGFR3
FGFR4

PDB
5EW8 (FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693)

Ligand code = 5SF (link to the list of PDB complexes)

Download experimental 3D coordinates of 5SF with added hydrogens

DrugCentral

Vascular endothelial growth factor receptor 2 UNIPROT P35968 KDR

Fibroblast growth factor receptor 3 UNIPROT P22607 FGFR3

Download SDF file 1,2-Ethanediamine, N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-

Formula:
C25H30N6O2

Calculated chemical properties:

MW 446.55
NB_atoms 33
XLogP 4.18
PSA 75.676
NB_HD 1
NB_HA 8
fsp3 0.32
Lipinski(0=no;1=yes) 1

FDA
NDA 212018 (pdf not found) INN (ERDAFITINIB) BALVERSA (JANSSEN BIOTECH) APPROVAL= AP YEAR= 2019 NEWMOLECULARENTITY

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL