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Fibroblast growth factor receptor 1 (FGFR1; CD331), FGFR2 and fibroblast 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.

SciBX 5(40); doi:10.1038/scibx.2012.1067
Published online Oct. 11, 2012

Patent application filed for compound; unlicensed

Guagnano, V. et al. Cancer Discov.; published online Sept. 20, 2012;
doi:10.1158/2159-8290.CD-12-0210
Contact: Diana Graus Porta, Novartis Institutes for BioMedical Research, Basel, Switzerland
e-mail:
diana.graus_porta@novartis.com