FGFR-targeted therapeutics: clinical activity, mechanisms of resistance and new directions

M Katoh, Y Loriot, G Brandi, S Tavolari… - Nature Reviews …, 2024 - nature.com
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 …

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 …

Futibatinib for FGFR2-Rearranged Intrahepatic Cholangiocarcinoma

L Goyal, F Meric-Bernstam… - … England Journal of …, 2023 - Mass Medical Soc
Background Alterations in fibroblast growth factor receptor 2 (FGFR2) have emerged as
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 …

Charting co-mutation patterns associated with actionable drivers in intrahepatic cholangiocarcinoma

G Kendre, K Murugesan, T Brummer, O Segatto… - Journal of …, 2023 - Elsevier
Background & Aims In recent years, intrahepatic cholangiocarcinoma (iCCA) has evolved as
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

JE Berchuck, F Facchinetti, DF DiToro, I Baiev… - Annals of …, 2022 - Elsevier
Background Targeted therapies have transformed clinical management of advanced biliary
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 …

EGFR inhibition potentiates FGFR inhibitor therapy and overcomes resistance in FGFR2 fusion–positive cholangiocarcinoma

Q Wu, Y Zhen, L Shi, P Vu, P Greninger, R Adil… - Cancer …, 2022 - aacrjournals.org
FGFR inhibitors are approved for the treatment of advanced cholangiocarcinoma harboring
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 …

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 …