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Anti-Tumour Activity of Lenvatinib in HCC Pre-Clinical Models
Cell
FGF19 gene
amplification
IC
50
(nmol/L)
Lenvatinib Sorafenib
HEP 3B2. 1-7
+
230
[86]
a
2,300
[620]
a
HuH-7
+
420
[160]
a
2,200
[590]
a
PLC/PRF/5
-
>10,000
5,300
[1,400]
a
1. Matsuki M
et al
. Poster presented at 107th Annual Meeting of the AACR, Washington, DC, USA. Apr 1–5, 2017.
a = Values in bracket are IC
50
as protein-unbound form (62.5% for lenvatinib, 73.2% [reported] for sorafenib in culture medium with 10% FBS)
Cell growth inhibition
(%)
Concentration (mol/L)
120
100
80
60
40
20
0
-20
10
-3
10
-4
10
-5
FBS = foetal bovine serum; FGF = fibroblast growth factor; HCC = hepatocellular carcinoma; IC
50
= 50% inhibitory concentration.
Lenvatinib inhibited in vitro proliferation of HCC cell lines harbouring FGF19 gene amplification