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Updated: Oct 19, 2025

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
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Futibatinib, an Irreversible FGFR1-4 Inhibitor, in Patients with Advanced Solid Tumors Harboring FGF/FGFR

Funda Meric-Bernstam1, Rastislav Bahleda2, Cinta Hierro3

  • 1Department of Investigational Cancer Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, Texas. fmeric@mdanderson.org.

Cancer Discovery
|September 23, 2021
PubMed

Insights

Futibatinib, an irreversible FGFR inhibitor, showed clinical activity in advanced solid tumors with FGFR alterations. The drug demonstrated promise in cholangiocarcinoma and other cancers, supporting further trials.

Area of Science:

  • Oncology
  • Pharmacology
  • Genetics

Background:

  • Fibroblast growth factor receptor (FGFR) aberrations are implicated in various advanced solid tumors.
  • Targeted therapies inhibiting FGFR signaling represent a promising treatment strategy.
  • Understanding the efficacy and safety of novel FGFR inhibitors in diverse histologies is crucial.

Purpose of the Study:

  • To evaluate the safety and efficacy of futibatinib, a selective FGFR1-4 inhibitor, in a phase I dose-expansion trial.
  • To identify tumor types and specific FGFR alterations that respond to futibatinib treatment.
  • To assess futibatinib's activity in patients with acquired resistance to prior FGFR inhibitors.

Main Methods:

  • A large, multihistology phase I dose-expansion trial enrolled 197 patients with advanced solid tumors.
  • Patients received futibatinib, and objective response rate (ORR) was assessed.
  • Tumor samples were analyzed for FGFR aberrations, including known and novel alterations.

Main Results:

  • Futibatinib demonstrated an overall ORR of 13.7% across a broad spectrum of tumors.
  • Highest activity was observed in FGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma (ORR, 25.4%).
  • Responses were noted in patients with acquired resistance to prior FGFR inhibitors; safety profile was manageable.

Conclusions:

  • Futibatinib exhibits clinical activity and a manageable safety profile in patients with FGFR-aberrant advanced solid tumors.
  • Genomically selected early-phase trials can effectively identify patient subsets benefiting from targeted therapies like futibatinib.
  • Results support ongoing phase II/III trials of futibatinib in cholangiocarcinoma and other selected populations.

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