VEGF A
VEGF C & D
VEGF B
Bevacizumab
VEGFR1

SUNI
AXI
VEGFR2

SUNI
AXI
SORA
BRIV
VEGFR3

SUNI
AXI
SORA
lymphatics
PDGF
SCF
RET

PDGFR

SUNI
AXI
SORA
c Kit

SUNI
AXI
SORA
RETR

SUNI
RAS
RAP
C.RAF
B.RAF
SORA
MEK
ERK
Endothelial cells
Cancer cell
Sorafenib and Sunitinib have been approved by the FDA respectively in December 2005 for RCC, and in January 2006 for RCC and GIST.
The aim of this drawing is not to show  differences in chemical structure,
efficacy or safety, but to pinpoint differences in biological mechanisms of action.
Although there are many similar targets (VEGFR2, VEGFR3, PDGFR, c Kit), Sunitinib is also active on VEGFR1, and on the RET receptor (which is becoming an exciting target for other cancers, such as thyroid, where trials are ongoing with a few molecules).
Sorafenib is active on intra-cellular kinases, such as those active on CRAF and BRAF, hence blocking the MEK/ERK pathway, which is a strategic target for many cancers.
SUNITINIB,SORAFENIB, AXITINIB, REGORAFENIB :
some differences, & competition
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- RAF-265, XL 281 & ECO 4601
are RAF kinase inhibitors
- ARRY 886 is a MEK inhibitor
- RAF-265
- XL 281
- ECO 4601
The MEK/ERK pathway plays
a key role in experimental
(HepG2) liver cancer
Abbreviations :
Bric brivanib, ERK: extracellular regulated kinase, FGF fibroblast growth receptor, MAPK: mitogen activated protein kinase, MEK: MAP-ERK kinase, Raf: rat fibrosarcoma, RET: rearranged during transcription, RAP: receptor associated protein, Ras: rat sarcoma
ARRY 886/AZD 6244
FGFR1
BRIV
Silibilin is an inhibitor of the MEK/ERK pathway, which could be a key quantitative and/or qualitative difference between sunitinib & sorafenib
VEMURAFENIB
- VEMURAFENIB is only active if BRAF bears a specific mutation, which occurs in 40 to 60% of melanomas. FDA approved AUG 2011.
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Regorafenib__Abstract_fron_ASCO_GI_January_2012.pdf
Regorafenib__Abstract_fron_ASCO_GI_January_2012.pdf