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. 2021 Oct 6;22(19):10774. doi: 10.3390/ijms221910774

Table 1.

Tyrosine kinase inhibitors under phase II/III clinical studies for HCC treatment [4].

Drug Targets Descriptions Reference
Cediranib
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VEGFR Shows high toxicity and is ineffective for patients with unresectable or metastatic HCC [30]
Dovitinib
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c-KIT, Flt-3, FGFR,
VEGFR
Significantly prolongs survival and inhibits primary tumour growth and lung metastasis in HCC xenograft models [31,32]
Erlotinib
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EGFR Shows modest prolonged progression-free survival and overall survival in patients with unresectable HCC [33,34]
Gefitinib
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EGFR Inhibits the tumor growth of HCC xenografts in a mouse model [35]
Selumetinib
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MEK1 Suppresses tumour growth of HCC xenografts in mouse model
Shows inadequate antitumour activity with short progression-free survival in patients with locally advanced or metastatic HCC
[36,37]
Brivanib
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FGFR, VEGFR Increases apoptosis, reduces microvessel density, and decreases VEGFR phosphorylation
Shows promising antitumour activity in patients with advanced HCC
[28,29]
Linifanib
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PDGFR, VEGFR Inhibits tumour growth of HCC xenografts in the mouse model Shows similar overall survival to sorafenib in patients with advanced HCC [38,39,40]
Sunitinib
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c-Kit, Flt-3, PDGFP,
VEGFR
Increases apoptosis and reduces microvessel density of HCC xenografts
Displays poor overall survival in patients with advanced HCC and has severe toxicity
[41]
Orantinib
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FGFR, PDGFR, VEGFR Suppresses the tumour growth of subcutaneously co-injected HCC cell line xenografts
Shows no improvement in overall survival in patients with unresectable HCC
[42,43]
Bevacizumab VEGF Inhibits tumour growth of HCC cell lines or patient-derived HCC xenografts [44,45]
Cetuximab EGFR Shows no obvious response in patients with advanced HCC [46]

VEGF: Vascular endothelial growth factor; VEGFR: Vascular endothelial growth factor receptor; FGFR: Fibroblast growth factor receptor; EGFR: Epidermal growth factor receptor; MEK1: Mitogen-activated protein kinase (MAPK) kinase; PDGFR: Platelet-derived growth factor receptor; Flt-3: FMS-like tyrosine kinase-3.