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FGFR-targeted therapeutics: clinical activity, mechanisms of resistance and new directions
Fibroblast growth factor (FGF) signalling via FGF receptors (FGFR1–4) orchestrates fetal
development and contributes to tissue and whole-body homeostasis, but can also promote …
development and contributes to tissue and whole-body homeostasis, but can also promote …
Futibatinib: first approval
YY Syed - Drugs, 2022 - Springer
Futibatinib (Lytgobi®) is an oral, covalently binding, irreversible inhibitor of fibroblast growth
factor receptor (FGFR) 1–4 that is being developed by Taiho Oncology and Taiho …
factor receptor (FGFR) 1–4 that is being developed by Taiho Oncology and Taiho …
Futibatinib for FGFR2-Rearranged Intrahepatic Cholangiocarcinoma
Background Alterations in fibroblast growth factor receptor 2 (FGFR2) have emerged as
promising drug targets for intrahepatic cholangiocarcinoma, a rare cancer with a poor …
promising drug targets for intrahepatic cholangiocarcinoma, a rare cancer with a poor …
Pemigatinib in previously treated solid tumors with activating FGFR1–FGFR3 alterations: phase 2 FIGHT-207 basket trial
J Rodón, S Damian, M Furqan, J García-Donas… - Nature medicine, 2024 - nature.com
Fibroblast growth factor receptor (FGFR) alterations drive oncogenesis in multiple tumor
types. Here we studied pemigatinib, a selective, potent, oral FGFR1–FGFR3 inhibitor, in the …
types. Here we studied pemigatinib, a selective, potent, oral FGFR1–FGFR3 inhibitor, in the …
Charting co-mutation patterns associated with actionable drivers in intrahepatic cholangiocarcinoma
Background & Aims In recent years, intrahepatic cholangiocarcinoma (iCCA) has evolved as
a “role model” for precision oncology in gastrointestinal cancers. However, its rarity, paired …
a “role model” for precision oncology in gastrointestinal cancers. However, its rarity, paired …
The clinical landscape of cell-free DNA alterations in 1671 patients with advanced biliary tract cancer
Background Targeted therapies have transformed clinical management of advanced biliary
tract cancer (BTC). Cell-free DNA (cfDNA) analysis is an attractive approach for cancer …
tract cancer (BTC). Cell-free DNA (cfDNA) analysis is an attractive approach for cancer …
Landscape of clinical resistance mechanisms to FGFR inhibitors in FGFR2-altered cholangiocarcinoma
Q Wu, H Ellis, G Siravegna, AG Michel… - Clinical Cancer …, 2024 - aacrjournals.org
Purpose: FGFR inhibitors are effective in FGFR2-altered cholangiocarcinoma, leading to
approval of reversible FGFR inhibitors, pemigatinib and infigratinib, and an irreversible …
approval of reversible FGFR inhibitors, pemigatinib and infigratinib, and an irreversible …
EGFR inhibition potentiates FGFR inhibitor therapy and overcomes resistance in FGFR2 fusion–positive cholangiocarcinoma
FGFR inhibitors are approved for the treatment of advanced cholangiocarcinoma harboring
FGFR2 fusions. However, the response rate is moderate, and resistance emerges rapidly …
FGFR2 fusions. However, the response rate is moderate, and resistance emerges rapidly …
Secondary IDH1 resistance mutations and oncogenic IDH2 mutations cause acquired resistance to ivosidenib in cholangiocarcinoma
JM Cleary, B Rouaisnel, A Daina, S Raghavan… - NPJ precision …, 2022 - nature.com
The mutant IDH1 inhibitor ivosidenib improves outcomes for patients with IDH1-mutated
cholangiocarcinoma, but resistance inevitably develops. Mechanisms of resistance and …
cholangiocarcinoma, but resistance inevitably develops. Mechanisms of resistance and …
Geospatial immune heterogeneity reflects the diverse tumor–immune interactions in intrahepatic cholangiocarcinoma
Y Lin, L Peng, L Dong, D Liu, J Ma, J Lin, X Chen… - Cancer …, 2022 - aacrjournals.org
Intrahepatic cholangiocarcinoma (iCCA) exhibits extensive intratumoral heterogeneity and
an extremely high mortality rate. Here, we performed whole-exome sequencing, RNA …
an extremely high mortality rate. Here, we performed whole-exome sequencing, RNA …