Acquired resistance to LY2874455 in FGFR2-amplified gastric cancer through an emergence of novel FGFR2-ACSL5 fusion

Oncotarget. 2017 Feb 28;8(9):15014-15022. doi: 10.18632/oncotarget.14788.

Abstract

Background: Fibroblast growth factor 2 (FGFR2) amplification, occurring in ~2-9% of gastric cancers (GC), is associated with poor overall survival.

Results: RNA sequencing identified a novel FGFR2-ACSL5 fusion in the resistant tumor that was absent from the matched pre-treatment tumor. The FGFR2-amplified PDC line was sensitive to FGFR inhibitors whereas the PDC line with concomitant FGFR2 amplification and FGFR2-ACSL5 fusion exhibited resistance. Additionally, the FGFR2-amplified GC PDC line, which was initially sensitive to FGFR2 inhibitors, subsequently also developed resistance.

Materials and methods: We identified an FGFR2-amplified patient with GC, who demonstrated a dramatic and long-term response to LY2874455, a pan-FGFR inhibitor, but eventually developed an acquired LY2874455 resistance. Following resistance development, an endoscopic biopsy was performed for transcriptome sequencing and patient-derived tumor cell line (PDC) establishment to elucidate the underlying molecular alterations.

Conclusions: FGFR inhibitors may function against FGFR2-amplified GC, and a novel FGFR2-ACSL5 fusion identified by transcriptomic characterization may underlie clinically acquired resistance.

Implications for practice: Poor treatment response represents a substantial concern in patients with gastric cancer carrying multiple FGFR2 gene copies. Here, we show the utility of a general FGFR inhibitor for initial response prior to treatment resistance and report the first characterization of a potential resistance mechanism involving an FGFR2-ACSL5 fusion protein.

Keywords: FGFR2 amplification; gastric cancer; targeted therapy.

Publication types

  • Case Reports

MeSH terms

  • Adult
  • Coenzyme A Ligases / genetics*
  • Drug Resistance, Neoplasm / genetics*
  • Female
  • Gene Amplification*
  • Humans
  • Indazoles / pharmacology*
  • Oncogene Proteins, Fusion / genetics*
  • Prognosis
  • Receptor, Fibroblast Growth Factor, Type 2 / genetics*
  • Stomach Neoplasms / drug therapy
  • Stomach Neoplasms / genetics*
  • Stomach Neoplasms / pathology

Substances

  • 2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3yl)vinyl)-1H-pyrazol-1-yl)ethanol
  • Indazoles
  • Oncogene Proteins, Fusion
  • FGFR2 protein, human
  • Receptor, Fibroblast Growth Factor, Type 2
  • Coenzyme A Ligases
  • ACSL5 protein, human