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Among the 4 FGFRs, the expression of FGFR1 was upregulated in RO82W-1 cells compared with that in normal thyroid cells, whereas FGFR2 and FGFR3 protein expression was downregulated.
Given that any strategy that inhibits activation of p38 should theoretically induce synthetic lethality when combined with paclitaxel in p53-null cells, we next explored the use of triple angiokinase inhibitor BIBF1120, which not only inhibits VEGFR, PDGFR, and FGFR2, but also has antiangiogenic activity in the vascular endothelium.
Katoh, "FGFR2 abnormalities underlie a spectrum of bone, skin, and cancer pathologies," Journal of Investigative Dermatology, vol.
The distributions of the rare genotypes (AG and GG) of the FGFR2 gene polymorphism (2451A/G SNP at the 3'UTR) were highest in group A (ratio of homozygous mutants 18.84%, rare allele frequency [MAF] = 0.4638) and lowest in group B (ratio of homozygous rare alleles 8.82%, MAF = 0.3676, Fisher exact probability test P = 0.1227, Odds ratio 1.
tropicalis, FGFR3 is expressed in the developing lens, FGFR2 is prominently expressed in corneal epithelium, and FGFR1 and FGFR4 are expressed in "cells surrounding the lens" in early tadpoles (Lea et al., 2009).
Incyte is planning to submit an NDA seeking approval for pemigatinib as a second-line treatment for patients with FGFR2 translocated cholangiocarcinoma in the second half of 2019.
In a phase 1/2 study in patients with iCCA harboring FGFR2 gene fusions, treatment with derazantinib resulted in an objective response rate of 21%, nearly 3 times higher than standard-of-care chemotherapy.
The product is now indicated in the United States for the treatment of adult patients having locally advanced or metastatic bladder cancer that has a type of susceptible genetic alteration called FGFR3 or FGFR2, and whose condition had progressed during or after being previously treated with platinum-containing chemotherapy.
BALVERSA ,which is now approved for locally advanced or metastatic urothelial carcinoma (mUC), which has susceptible fibroblast growth factor receptor (FGFR) or FGFR2 genetic alterations and who have progressed during or following at least one line of prior platinum-containing chemotherapy, including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy, follows the US FDA's breakthrough therapy designation and priority review designation, added the company.
Following testing, laboratories reported the variants detected in each specimen by selecting from a master variant list containing 90 variants in 15 genes (AKT1, ALK, BRAF, EGFR, ERBB2, FBXW7, FGFR2, GNAS, IDH1, KIT, KRAS, MET, NRAS, PIK3CA, and STK11).
Discovered and developed in house by Eisai, LENVIMA is an orally administered kinase inhibitor with a novel binding mode that selectively inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors (VEGFR1, VEGFR2 and VEGFR3) and fibroblast growth factor (FGF) receptors (FGFR1, FGFR2, FGFR3 and FGFR4) in addition to other pathway-related RTKs (including the platelet-derived growth factor (PDGF) receptor PDGFRalpha; KIT; and RET) involved in tumor angiogenesis, tumor progression and modification of tumor immunity.
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- FGFR signalling adaptor
- FGFR substrate 2
- FGFR-signalling adaptor SNT