e-Drug3D

1585

REGORAFENIB

INN
REGORAFENIB

cas 755037-03-7

CLASS

ANTINEOPLASTIC
METASTATIC COLORECTAL CANCER
KINASES INHIBITOR

ROUTE (list)

ORAL

ATC code

L01EX05

PK parameters

F 76 PERCENT
Tmax 4 HOUR
PPB 99.5 PERCENT
t1/2 28 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER

Target

TARGET RET
VEGFR1
VEGFR2
VEGFR3
KIT
PDGFR-ALPHA
PDGFR-BETA
FGFR1
FGFR2
TIE2
DDR2
TRKA
RAF-1
BRAF
BRAF(V600E)
SAPK2
PTK5
ABL

DrugCentral

Serine,threonine-protein kinase B-raf UNIPROT P15056 BRAF

Vascular endothelial growth factor receptor 2 UNIPROT P35968 KDR

Download SDF file

2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-

Formula:
C21H15ClF4N4O3

Calculated chemical properties:

MW 482.82
NB_atoms 33
XLogP 5.69
PSA 86.385
NB_HD 3
NB_HA 7
fsp3 0.10
Lipinski(0=no;1=yes) 0

FDA
NDA 203085 (label) INN (REGORAFENIB) STIVARGA (BAYER HLTHCARE) APPROVAL= AP YEAR= 2012
NDA 204369 (label) INN (REGORAFENIB) STIVARGA (BAYER HEALTHCARE PHARMS) APPROVAL= AP YEAR= 2013 NEWAPPLICATION
NDA 209728 (pdf not found) INN (REGORAFENIB) REGORAFENIB (ACTAVIS LABS FL) APPROVAL= AP YEAR= 2025 DISCONTINUED