Reference Detail

Contact

Missing content? – Request curation!

Request curation for specific Genes, Variants, or PubMed publications.

Have questions, comments, or suggestions? - Let us know!

Email us at : ckbsupport@jax.org

Ref Type Journal Article
PMID (37980453)
Authors Saridogan T, Akcakanat A, Zhao M, Evans KW, Yuca E, Scott S, Kirby BP, Zheng X, Ha MJ, Chen H, Ng PKS, DiPeri TP, Mills GB, Rodon Ahnert J, Damodaran S, Meric-Bernstam F
Title Efficacy of futibatinib, an irreversible fibroblast growth factor receptor inhibitor, in FGFR-altered breast cancer.
URL
Abstract Text Several alterations in fibroblast growth factor receptor (FGFR) genes have been found in breast cancer; however, they have not been well characterized as therapeutic targets. Futibatinib (TAS-120; Taiho) is a novel, selective, pan-FGFR inhibitor that inhibits FGFR1-4 at nanomolar concentrations. We sought to determine futibatinib's efficacy in breast cancer models. Nine breast cancer patient-derived xenografts (PDXs) with various FGFR1-4 alterations and expression levels were treated with futibatinib. Antitumor efficacy was evaluated by change in tumor volume and time to tumor doubling. Alterations indicating sensitization to futibatinib in vivo were further characterized in vitro. FGFR gene expression between patient tumors and matching PDXs was significantly correlated; however, overall PDXs had higher FGFR3-4 expression. Futibatinib inhibited tumor growth in 3 of 9 PDXs, with tumor stabilization in an FGFR2-amplified model and prolonged regression (> 110 days) in an FGFR2 Y375C mutant/amplified model. FGFR2 overexpression and, to a greater extent, FGFR2 Y375C expression in MCF10A cells enhanced cell growth and sensitivity to futibatinib. Per institutional and public databases, FGFR2 mutations and amplifications had a population frequency of 1.1%-2.6% and 1.5%-2.5%, respectively, in breast cancer patients. FGFR2 alterations in breast cancer may represent infrequent but highly promising targets for futibatinib.

Filtering

  • Case insensitive filtering will display rows if any text in any cell matches the filter term
  • Use simple literal full or partial string matches
  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

Sorting

  • Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.

Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 Y375C FGFR2 amp triple-receptor negative breast cancer sensitive Futibatinib Preclinical - Pdx Actionable In a preclinical study, Lytgobi (furibatinib) inhibited viability of cells derived from a patient-derived xenograft (PDX) model of FGFR2-amplified triple-negative breast cancer harboring FGFR2 Y375C in culture and induced tumor regression and improved survival in the patient-derived xenograft (PDX) model (PMID: 37980453). 37980453
FGFR2 Y375C cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of a cholangiocyte cell line harboring FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 Y375C FGFR2 amp triple-receptor negative breast cancer sensitive Pemigatinib Preclinical - Patient cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells derived from a patient-derived xenograft (PDX) model of FGFR2-amplified triple-negative breast cancer harboring FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 Y375C breast cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited viability of breast epithelial cells expressing FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 amp breast cancer sensitive Futibatinib Preclinical - Pdx Actionable In a preclinical study, Lytgoi (futibatinib) inhibited tumor growth and improved survival in a patient-derived xenograft (PDX) model of FGFR2-amplified breast cancer (PMID: 37980453). 37980453
FGFR2 Y375C breast cancer sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of breast epithelial cells expressing FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 Y375C breast cancer sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of breast epithelial cells expressing FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 Y375C breast cancer sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited viability of breast epithelial cells expressing FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 Y375C breast cancer sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited Fgfr2 signaling and viability in breast epithelial cells expressing FGFR2 Y375C in culture (PMID: 37980453). 37980453