e-Drug3D

1527

AXITINIB


INN
AXITINIB

cas 319460-85-0
CLASS

ANTINEOPLASTIC AGENT
PROTEIN KINASE INHIBITOR
RENAL CELL CARCINOMA

ROUTE (list)

ORAL

ATC code

L01EK01

PK parameters

F 58 PERCENT (5 MILLIGRAM)
VD 160 LITER (5 MILLIGRAM TWICE DAILY)
Cl 38 LITER / HOUR
PPB 99 PERCENT
t1/2 4.3 HOUR (5 MILLIGRAM TWICE DAILY)

Solubility

IN AQUEOUS MEDIA OVER THE RANGE PH 1.1 TO PH 7.8 IS IN EXCESS OF 0.2 MICROGRAM / MILLILITER


Target

TARGET RECEPTOR TYROSINE KINASES
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTORS
VEGFR-1
VEGFR-2
VEGFR-3

PDB
4WA9 (THE CRYSTAL STRUCTURE OF HUMAN ABL1 WILD TYPE KINASE DOMAIN IN COMPLEX WITH AXITINIB)

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

Download experimental 3D coordinates of AXI with added hydrogens

DrugCentral

Vascular endothelial growth factor receptor 1 UNIPROT P17948 FLT1

Vascular endothelial growth factor receptor 2 UNIPROT P35968 KDR

Download SDF file N-methyl-2-[3-((E)2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide

Formula:
C22H18N4OS

Calculated chemical properties:

MW 386.47
NB_atoms 28
XLogP 4.64
PSA 62.253
NB_HD 2
NB_HA 5
fsp3 0.05
Lipinski(0=no;1=yes) 1

FDA
NDA 202324 (label) INN (AXITINIB) INLYTA (PF PRISM CV) APPROVAL= AP YEAR= 2012 NEWMOLECULARENTITY
NDA 210234 (pdf not found) INN (AXITINIB) AXITINIB (TEVA PHARMS) APPROVAL= TA YEAR= 2018
NDA 211650 (pdf not found) INN (AXITINIB) AXITINIB (APOTEX INC) APPROVAL= TA YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL