Table 1.

Examples of TKI in clinical development

TKIMain target(s)Development stage
AfatinibEGFR/HER2FDA approved
AlectinibALKPhase III
ApatinibVEGFR2Phase II
AxitinibVEGFR1/2/3FDA approved
BafetinibBcr-AblPhase II
BosutinibBcr-AblFDA approved
BrivanibFGFR, VEGFRPhase II
CanertinibPan-ErbBNo longer in development
CediranibVEGFR1/2/3Phase III
CeritinibALKFDA approved
CrizotinibALKFDA approved
DasatinibSRC, Bcr-AblFDA approved
DovitinibFGFR, VEGFRPhase III
ErlotinibEGFRFDA approved
FedratinibJAK2Discontinued
GefitinibEGFRFDA approved
IbrutinibBTKFDA approved
ImatinibBcr-AblFDA approved
LapatinibEGFR, HER2FDA approved
LestaurtinibFLT3No longer in development
LevantinibFGFR, VEGFRFDA approved
LucitanibFGFR1/2, VEGFR1/2/3, PGFRα/βPhase II
MotesanibVEGFR, PDGFR, SCFRPhase II/III
NeratinibEGFR, HER2, HER4Phase III
NilotinibBcr-AblFDA approved
NintedanibPDGFRα/β, FGFR1/3, VEGFR1/2/3Phase II
PazopanibVEGFRFDA approved
PonatinibBcr-AblFDA approved
QuizartinibFLT3Phase II/IIb
RegorafenibVEGFRFDA approved
RuxolitinibJAK2FDA approved
SemaxanibVEGFRNo longer in development
SorafenibVEGFR, BRAFFDA approved
SunitinibVEGFRFDA approved
TivozanibVEGFR1/2/3Phase III
ToceranibKIT, VEGFR2, PDGFRFDA approved in canines
VandetanibVEGFR, EGFR, RETFDA approved