|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
1.H3B-6527 is an orally available covalent small molecule inhibitor of FGFR4 undergoing evaluation in adults with hepatocellular carcinoma.
|
31305210 |
2020 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Fisogatinib (BLU-554) is a highly selective and potent oral fibroblast growth factor receptor 4 (FGFR4) inhibitor currently in Phase I clinical trials for treatment of hepatocellular carcinoma (HCC).
|
31759109 |
2020 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Frequent overexpression of FGF19/FGFR4-related biomarkers was detected in resectable HCC.
|
30698907 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Fisogatinib (BLU-554) is a potent and selective inhibitor of FGFR4 and demonstrates clinical benefit and tumor regression in patients with HCC with aberrant FGF19 expression.
|
31575540 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
FGFR4 is therefore a promising target for the treatment of HCC harboring aberrant FGF19-FGFR4 signaling, and several FGFR4 inhibitors have advanced to clinical trial.
|
30403487 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Currently, the safety and preliminary efficacy of several small molecule inhibitors targeting FGFR4 are under early phase clinical assessment, mainly in hepatocellular carcinoma patients.
|
31146605 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
CONCLUSION: We defined a FGF19-SOX18-FGFR4 positive feedback loop that played a pivotal role in HCC metastasis, and targeting this pathway may be a promising therapeutic option for the clinical management of HCC.
|
31529503 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
These results validate the oncogenic driver role of the FGFR4 pathway in HCC and the use of FGF19 as a biomarker for patient selection.<i>See related commentary by Subbiah and Pal, p. 1646</i>.<i>This article is highlighted in the In This Issue feature, p. 1631</i>.
|
31575541 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
FGF401 is the first FGFR4 inhibitor to enter clinical trials, and a phase I/II study is currently ongoing in HCC and other solid malignancies.
|
31409633 |
2019 |
|
Liver carcinoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Aberrant expression of fibroblast growth factor 19-fibroblast growth factor receptor 4 (<i>FGF19-FGFR4</i>) is reported to be an oncogenic-driver pathway for HCC patients.
|
31167419 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Aberration in FGFR4 signaling drives carcinogenesis and progression in a subset of hepatocellular carcinoma (HCC) patients, thereby making FGFR4 an attractive molecular target for this disease.
|
31413803 |
2019 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Previous studies have demonstrated that FGF15 and FGF19 induce the activation of its receptor, FGF receptor 4 (FGFR4), which can promote hepatocellular carcinoma progression and regulate liver lipid metabolism.
|
29468415 |
2018 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
FGF401 is a highly selective FGFR4 kinase inhibitor being developed for hepatocellular carcinoma, currently in phase I/II clinical studies.
|
29432567 |
2018 |
|
Liver carcinoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
After constructing the best silencing FGFR4 expression vector, migration and invasiveness of TGF-β1 in HCC was studied in vitro and in vivo.
|
29490293 |
2018 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
FGFR4 activation in HCC cells was inhibited by BLU9931.
|
28983785 |
2018 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
The fibroblast growth factor receptor 4 (FGFR4) pathway is an essential regulatory component of bile acid synthesis, and its relationship with hepatocellular carcinoma (HCC) has been reported.
|
28445152 |
2017 |
|
Liver carcinoma
|
0.100 |
GeneticVariation
|
disease |
BEFREE |
Pharmacological interference with FGF15/19-FGFR4 signaling inhibits experimental hepatocarcinogenesis, and specific FGFR4 inhibitors are currently being tested in selected HCC patients with tumoral FGF19-FGFR4/KLB expression.
|
28249259 |
2017 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
|
29247039 |
2017 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
FGFR4-MAPK signaling plays an important role in driving proliferation of a molecular subclass of HCC.
|
26481559 |
2016 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
As FGF19 and its specific receptor FGFR4 are frequently amplified in HCC cells, selective targeting this signaling node may lend insights into a potential effective therapeutic approach for blocking metastasis of HCC.
|
26498355 |
2016 |
|
Liver carcinoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
FGF19 is overexpressed in a significant proportion of human hepatocellular carcinomas (HCC), and activation of its receptor FGFR4 promotes HCC cell growth.
|
25346390 |
2015 |
|
Liver carcinoma
|
0.100 |
GeneticVariation
|
disease |
BEFREE |
In addition, this is the first study that evaluated the risk factors associated with FGFR4 polymorphism variants in Taiwanese patients with HCC.
|
25860955 |
2015 |
|
Liver carcinoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
FGFR4 overexpression in non-tumourigenic hepatocarcinoma cells significantly reduced cell-matrix adhesion, enabled cells to grow anchorage-independently in soft agar, to disintegrate the lymph-/blood-endothelial barrier for intra-/extravasation of tumour cells and to form tumours in SCID mice.
|
25031272 |
2014 |
|
Liver carcinoma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
In mice, ectopic overexpression of FGF19 drives HCC development in a process that requires FGFR4.
|
24728076 |
2014 |
|
Liver carcinoma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Elevated KLB expression in HCC tissues provides further credence to the oncogenic role of increased FGFR4 signaling in HCC progression and represents a novel biomarker to identify additional patients amenable to anti-FGFR4 therapy.
|
22439738 |
2012 |