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 …

Understanding and Overcoming Resistance to Selective FGFR Inhibitors across FGFR2-Driven Malignancies

F Facchinetti, Y Loriot, F Brayé, D Vasseur… - Clinical Cancer …, 2024 - aacrjournals.org
Purpose: Understanding resistance to selective FGFR inhibitors is crucial to improve the
clinical outcomes of patients with FGFR2-driven malignancies. Experimental Design: We …

Molecular Targeting of the Fibroblast Growth Factor Receptor Pathway across Various Cancers

KS Shan, S Dalal, NN Thaw Dar, O McLish… - International Journal of …, 2024 - mdpi.com
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases that are
involved in the regulation of cell proliferation, survival, and development. FGFR alterations …

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 …

[HTML][HTML] Pemigatinib for patients with previously treated, locally advanced or metastatic cholangiocarcinoma harboring FGFR2 fusions or rearrangements: A joint …

A Parisi, B Delaunay, G Pinterpe, A Hollebecque… - European Journal of …, 2024 - Elsevier
Background Pemigatinib is approved for patients with pretreated, locally advanced or
metastatic CCA harboring FGFR2 rearrangements or fusions. We aim to assess the …

FGFR inhibition blocks NF-ĸB-dependent glucose metabolism and confers metabolic vulnerabilities in cholangiocarcinoma

Y Zhen, K Liu, L Shi, S Shah, Q Xu, H Ellis… - Nature …, 2024 - nature.com
Genomic alterations that activate Fibroblast Growth Factor Receptor 2 (FGFR2) are common
in intrahepatic cholangiocarcinoma (ICC) and confer sensitivity to FGFR inhibition. However …

[HTML][HTML] Genomic correlates of response and resistance to the irreversible FGFR1-4 inhibitor futibatinib based on biopsy and circulating tumor DNA profiling

L Goyal, D DiToro, A Hollebecque, JA Bridgewater… - Annals of …, 2024 - Elsevier
Background Futibatinib is the only covalent inhibitor of FGFR1-4 to gain regulatory approval
in oncology. Here, we present genomic analyses of tissue biopsies and circulating tumor …

[HTML][HTML] A Model for Decoding Resistance in Precision Oncology: Acquired Resistance to FGFR inhibitors in Cholangiocarcinoma

L Goyal, D DiToro, F Facchinetti, EE Martin, P Peng… - Annals of …, 2024 - Elsevier
Background Fibroblast growth factor receptor (FGFR) inhibitors have significantly improved
outcomes for patients with FGFR-altered cholangiocarcinoma, leading to their regulatory …

Mitochondria targeted drug delivery system overcoming drug resistance in intrahepatic cholangiocarcinoma by reprogramming lipid metabolism

Y Duan, M Deng, B Liu, X Meng, J Liao, Y Qiu, Z Wu… - Biomaterials, 2024 - Elsevier
The challenge of drug resistance in intrahepatic cholangiocarcinoma (ICC) is intricately
linked with lipid metabolism reprogramming. The hepatic lipase (HL) and the membrane …

Cholangiocarcinoma Targeted Therapies: Mechanisms of Action and Resistance

H Ellis, C Braconi, JW Valle, N Bardeesy - The American Journal of …, 2024 - Elsevier
Cholangiocarcinoma (CCA) is an aggressive bile duct malignancy with heterogeneous
genomic features. While most patients receive standard-of-care chemo/immunotherapy …