Role of regorafenib as second-line therapy and landscape of investigational treatment options in advanced hepatocellular carcinoma

Figures & data

Figure 1 Chemical structure of sorafenib: 4-(4-[{(4-chloro-3-[trifluoromethyl] phenyl)carbamoyl}amino]-3-phenoxy)-N-methylpyridine-2-carboxamide.

Note: Regorafenib differs from sorafenib by addition of a fluorine atom in the central phenyl ring as indicated in red, resulting in different target inhibition.

Table 1 Landscape of systemic treatment in hepatocellular carcinoma

Agent	Class	Line of treatment	Status	Result
Sorafenib	TKI	First line	SOC	Median OS 10.7 months
Lenvatinib	TKI	First line	Phase III	Q4 2016
Nivolumab	anti-PD-1	First line	Phase III	Q2 2017
JX-594	Oncolytic virus	First line in combination with sorafenib	Phase III	Q12018
Regorafenib	TKI	Second line	Phase IIIa	Median OS 10.6 months
Tivantinib	anti-MET	Second line	Phase III	Q4 2016
Cabozantinib	anti-MET	Second line	Phase III	Q2-3 2017
Ramucirumab	anti-VEGR2	Second line	Phase III	Q2-3 2017
Pembrolizumab	anti-PD-1	Second line	Phase III	Q1 2018

Note:

a RESORCE trial with positive results, approval expected in 2017.

Abbreviations: OS, overall survival; TKI, tyrosine kinase inhibitor; SOC, standard of care; anti-PD-1, antiprogrammed cell death receptor 1 blocking antibody; anti-VEGFR2, anti-vascular endothelial growth factor receptor 2 blocking antibody.