1
Table 1. Marketed and late clinical development small-molecule inhibitors of VEGF signaling.*
Drug name
Originator
Highest
Diseases
Cellular target
development
phase
Brain, breast, colorectal, lung,
Sorafenib
Bayer
Launched-2005
endocrine, ovarian, liver, female
reproductive system cancers
Launched Sunitinib
Breast, colorectal, endocrine, gastric,
Flt3, C-KIT, PDGFR, Raf
kinase, VEGFR-2/3
c-FMS, Flt3, C-KIT, PDGF,
liver, non-small cell lung, prostate and
Pfizer, Sugen
2006
renal cancers, myeloid leukemia
VEGFR-1/2/3
Breast, colorectal, pancreatic, lung,
Vatalanib
Novartis
Phase III
prostate cancers, glioblastoma, Kaposi's
C-KIT, PDGF, VEGFR-
sarcoma, multiple myeloma, myeloid
1/2/3
leukemia, solid tumors
Vandetanib
AstraZeneca
Brain, breast, endocrine cancers,
EGFR, FGFR, RET,
NSCLC, solid tumors
VEGFR-1/2/3
Phase III
AZD-2171
AstraZeneca
Phase II/III
Colorectal cancer and NSCLC
VEGFR-1/2/3
SU-6668
Sugen
Phase II
Breast and liver cancers, solid tumors
FGFR, PDGFR, VEGFR-2
CP-547632
OSI, Pfizer
Phase II
NSCLC and ovarian cancer
EGFR, PDGFR, VEGFR-2
Psoriasis, multiple myeloma, ovarian
GlaxoSmithKli
Pazopanib
Phase II
ne
and renal cancers, sarcoma
VEGFR-2
AMG-706
Amgen
Phase II
Gastrointestinal cancer and NSCLC
PDGFR, VEGFR-1/2/3
AEE-788
Novartis
Phase I/II
Glioblastoma
EGFR, HER2, VEGFR-2
E-7080
Eisai
Phase I
Solid tumors
VEGFR-2
Multiple myeloma, myeloid leukemia
FGFR3, PDGFR, VEGFR-
CHIR-258
Chiron
Phase I
and solid tumors
1/2
OSI-930
OSI
Phase I
Tumors
C-KIT, PDGFR, VEGFR-2
Bayer
Phase I
Tumors
PDGFR, VEGFR-2
Abbott
Phase I
Tumors
BAY579352
CSF1R, ERK, Flt3,
ABT-869
PDGFR, VEGFR-2
BMS-
Bristol-Myers
582664
Squibb
KRN-951
Kirin Brewery
Phase I
Digestive/gastrointestinal cancer
FGFR1, VEGFR-2
Phase I
Tumors and AMD
VEGFR-2
2
*data as of June 2006.