Thursday, October 11, 2012
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Fibroblast growth factor receptor 1 (FGFR1;
growth factor 19 (FGF19)
amplification may help predict sensitivity to FGFR
inhibitors in cancer
FGFR1, FGFR2 and FGF19 amplification may
help predict sensitivity to FGFR inhibitors. In breast, lung and osteosarcoma
cell lines and primary human osteosarcoma samples, FGFR1 amplification
was associated with sensitivity to the pan-FGFR inhibitor NVP-BGJ398.
In breast, gastric and esophageal cancer cells and in gastric cancer
xenografts in rats, FGFR2 amplification was associated with
sensitivity to the compound. In liver cancer cell lines, FGF19
amplification was associated with NVP-BGJ398 sensitivity when klotho-b (KLB)
was expressed. Ongoing work includes clinical trials with NVP-BGJ398 to treat
patients with cancer bearing genetic alterations in FGFRs. NVP-BGJ398 is
currently in Phase I trials to treat cancer.
At least seven different companies have FGFR inhibitors in development,
ranging from preclinical to Phase III trials, to treat various cancers.
Published online Oct. 11, 2012
Patent application filed
for compound; unlicensed
Guagnano, V. et al.
Cancer Discov.; published online Sept. 20, 2012;
Contact: Diana Graus Porta, Novartis Institutes for
BioMedical Research, Basel, Switzerland
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