Review Article

The Molecular Biology of Soft-Tissue Sarcomas and Current Trends in Therapy

Table 6

Current clinical trials with tyrosine kinase inhibitors in sarcomas.

AgentHuman trialsClinical benefit rate (CR, PR, and SD)Targets: notes

ImatinibGIST85% (5% CR; 45% PR)KIT. FDA Approved
SunitinibGIST65% (7% PR)VEGFR-1, VEGFR-2, VEGFR-3, PDGFR a/β, KIT.
FDA Approved
SorafenibAngiosarcoma, GIST14%VEGFR-2, VEGFR-3, PDGFR, c-RAS, b-RAF, KIT
PazopanibPalette
STS
PFS = 20 versus 7 weeks ( )VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, KIT
BrivanibSTS
ASCO 2011
30% overall
3 PR in angiosarcomas
FGF and VEGF
(FGF-positive did better)
CediranibSTS
ASCO 2011
78% (43%, PR)
Alveolar soft part sarcoma
VEGFR-1, VEGFR-2, and VEGFR-3
TivantinibSTS
ASCO 2011
80% (5%, PR)
Clear cell sarcoma, ASPS
c-Met
AxitinibSTS, angiosarcomaN/AVEGFR-1, VEGFR-2, and VEGFR-3