Gene Detail

Gene Symbol FGFR1
Synonyms bFGF-R-1 | BFGFR | CD331 | CEK | ECCL | FGFBR | FGFR-1 | FLG | FLT-2 | FLT2 | HBGFR | HH2 | HRTFDS | KAL2 | N-SAM | OGD
Gene Description FGFR1 is a receptor tyrosine kinase activated upon binding of the FGF ligand, which activates RAS-MAPK and PI3K-AKT pathways (PMID: 22508544). Altered function of Ffgr1 may lead to increased cell proliferation and decreased apoptosis (PMID: 22508544) and overexpression has been identified in colorectal cancer (PMID: 30181810) and gastric cancer (PMID: 29976636) and amplification has been identified in breast cancer (PMID: 30119151).
Entrez Id 2260
Chromosome 8
Map Location 8p11.23
Canonical Transcript NM_023110

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "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.

Variant Impact Protein Effect Variant Description Associated with drug Resistance
dec exp none no effect FGFR1 dec exp indicates decreased expression of the Fgfr1 protein and/or mRNA. However, the mechanism causing the decreased expression is unspecified.
Y374C missense gain of function - predicted FGFR1 Y374C lies within the extracellular domain of the Fgfr1 protein (UniProt.org). Y374C is predicted to confer a gain of function to Fgfr1, as the corresponding variant in an alternate isoform (Y372C) results in increased activity in cell culture (PMID: 15625620).
A268S missense no effect - predicted FGFR1 A268S lies within the Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). A268S has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
P252S missense gain of function - predicted FGFR1 P252S lies within the extracellular domain of the Fgfr1 protein (PMID: 18056464). P252S is predicted to confer a gain of function to the Fgfr1 protein, as demonstrated by altered ligand specificity and increased ligand affinity (PMID: 18056464).
K655I missense unknown FGFR1 K655I lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). K655I has been identified in sequencing studies (PMID: 26920151, PMID: 23817572; PMID: 28069802), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
K656M missense unknown FGFR1 K656M lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). K656M has been identified in sequencing studies (PMID: 23817572, PMID: 24185512), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
P772S missense no effect - predicted FGFR1 P772S lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). P772S has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
W684G missense unknown FGFR1 W684G lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). W684G has not been characterized in the scientific literature and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
L122F missense no effect - predicted FGFR1 L122F lies within the extracellular domain of the Fgfr1 protein (UniProt.org). L122F has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
R209H missense no effect - predicted FGFR1 R209H lies within the extracellular domain of the Fgfr1 protein (UniProt.org). R209H has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
P123S missense no effect - predicted FGFR1 P123S lies within the extracellular domain of the Fgfr1 protein (UniProt.org). P123S has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
T658P missense unknown FGFR1 T658P lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). T658P has been identified in the scientific literature (PMID: 27608415, PMID: 23817572), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
M456I missense unknown FGFR1 M456I lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). M456I has been identified in sequencing studies (PMID: 27127140), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
mutant unknown unknown FGFR1 mutant indicates an unspecified mutation in the FGFR1 gene.
D166del deletion unknown FGFR1 D166del (corresponds to D133 in the canonical isoform) results in the deletion of one amino acid in the Ig-like C2-type domain 2 of the Fgfr1 protein at amino acid 166 (UniProt.org). D166del has not been characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
V561M missense gain of function - predicted FGFR1 V561M lies within the protein kinase domain of the Fgfr1 protein (UniProt.org), V561M is predicted to confer a gain of function to the Fgfr1 protein, as demonstrated by increased Fgfr1 autophosphorylation in cell culture, and has also been demonstrated to confer resistance to tyrosine kinase inhibitors (PMID: 25686244, PMID: 15157880). Y
P150S missense unknown FGFR1 P150S lies within the extracellular domain of the Fgfr1 protein (UniProt.org). P150S has been identified in sequencing studies (PMID: 30275180, PMID: 25042771), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
E334Q missense unknown FGFR1 E334Q lies within the Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). E334Q has been identified in sequencing studies (PMID: 25056374), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
E360K missense no effect - predicted FGFR1 E360K lies within the extracellular domain of the Fgfr1 protein (UniProt.org). E360K has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
G70R missense unknown FGFR1 G70R lies within the Ig-like C2-type domain 1 of the Fgfr1 protein (UniProt.org). G70R has been identified in sequencing studies (PMID: 18948947), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
R250Q missense loss of function - predicted FGFR1 R250Q lies within the linker D2-D3 region of the Fgfr1 protein (PMID: 23276709). R250Q is predicted to confer a loss of function to the Fgfr1, as demonstrated by disrupted ligand binding (PMID: 23276709).
K656E missense gain of function FGFR1 K656E lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). K656E confers a gain of function to the Fgfr1 protein resulting in constitutive activation of MAPK signaling, and is transforming in cultured cells (PMID: 23817572).
D165_D166del deletion unknown FGFR1 D165_D166del (corresponds to D132 in the canonical isoform) results in the deletion of two amino acids in the Ig-like C2 type domain 2 of the Fgfr1 protein from amino acids 165 to 166 (UniProt.org). D165_D166del has not been characterized in the scientific literature and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
S430F missense unknown FGFR1 S430F lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). S430F has been identified in sequencing studies (PMID: 22810696), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
rearrange unknown unknown FGFR1 rearrangement indicates an unspecified rearrangement of the FGFR1 gene.
wild-type none no effect Wild-type FGFR1 indicates that no mutation has been detected within the FGFR1 gene.
S125L missense unknown FGFR1 S125L lies within the extracellular domain of the Fgfr1 protein (UniProt.org). S125L has been identified in the scientific literature (PMID: 15908952, PMID: 25677745), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
R250W missense unknown FGFR1 R250W lies within the linker D2-D3 region of the Fgfr1 protein (PMID: 23276709). R250W is predicted to confer a loss of function to the Fgfr1 protein by disrupting ligand binding (PMID: 23276709), however, R250W results in similar cell proliferation and viability levels as wild-type Fgfr1, in two different cell lines (PMID: 29533785).
R78H missense unknown FGFR1 R78H lies within the Ig-like C2-type domain 1 of the Fgfr1 protein (UniProt.org). R78H has been identified in the scientific literature (PMID: 18056464), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
N330I missense unknown FGFR1 N330I lies within the Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). N330I has been identified in sequencing studies (PMID: 30385747, PMID: 15625620), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
D133E missense unknown FGFR1 D133E lies within the extracellular domain of the Fgfr1 protein (UniProt.org). D133E has not been characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
E138* nonsense unknown FGFR1 E138* results in the premature truncation of the Fgfr1 protein at amino acid 138 of 822 (UniProt.org). Due to the loss of all known functional domains, E138* is predicted to lead to a loss of function, however, E138* has not been biochemically characterized and results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785).
G610D missense unknown FGFR1 G610D lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). G610D has been identified in sequencing studies (PMID: 22810696), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
D90V missense no effect - predicted FGFR1 D90V lies within the Ig-like C2-type domain 1 of the Fgfr1 protein (UniProt.org). D90V has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
Q309* nonsense loss of function - predicted FGFR1 Q309* results in a premature truncation of the Fgfr1 protein at amino acid 309 of 822 (UniProt.org). Due to the loss of the protein kinase domain (UniProt.org), Q309* is predicted to lead to a loss of Fgfr1 protein function.
K656D missense unknown FGFR1 K656D lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). K656D has been identified in the scientific literature (PMID: 26920151, PMID: 24750136, PMID: 23817572), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Dec 2018).
R507H missense unknown FGFR1 R507H lies within the protein kinase domain of the Fgfr1 protein and also refers to R505H and R497H in other Fgfr1 isoforms (UniProt.org). R507H has not been characterized in the scientific literature and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
amp none no effect FGFR1 amplification indicates an increased number of copies of the FGFR1 gene. However, the mechanism causing the increase is unspecified.
T141R missense unknown FGFR1 T141R lies within the extracellular domain of the Fgfr1 protein (UniProt.org). T141R has been identified in sequencing studies (PMID: 23887298, PMID: 25567908), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
A431S missense unknown FGFR1 A431S lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). A431S has been identified in sequencing studies (PMID: 12738854, PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Dec 2018).
C381Y missense no effect - predicted FGFR1 C381Y lies within the transmembrane domain of the Fgfr1 protein (UniProt.org). C381Y has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
G687V missense unknown FGFR1 G687V lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). G687V has not been characterized in the scientific literature and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
S135F missense unknown FGFR1 S135F lies within the extracellular domain of the Fgfr1 protein (UniProt.org). S135F has not been characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
N546K missense gain of function FGFR1 N546K lies within the protein kinase domain of the Fgfr1 protein (UniProt.org, PMID: 26179511). N546K increases Fgfr1 protein kinase activity and is transforming in cultured cells (PMID: 26179511, PMID: 23817572, PMID: 29533785).
R189H missense unknown FGFR1 R189H lies within the Ig-like C2-type domain 2 of the Fgfr1 protein (UniProt.org). R189H has not been characterizedand therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
V102I missense unknown FGFR1 V102I lies within the Ig-like C2-type domain 1 of the Fgfr1 protein (UniProt.org). V102I has been identified in the scientific literature (PMID: 16764984), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
V273M missense no effect - predicted FGFR1 V273M lies within the extracellular domain of the Fgfr1 protein (UniProt.org). V273M has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
V460A missense no effect - predicted FGFR1 V460A lies within the extracellular domain of the Fgfr1 protein (UniProt.org). V460A has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
positive unknown unknown FGFR1 positive indicates the presence of the FGFR1 gene, mRNA, and/or protein.
Y307N missense no effect - predicted FGFR1 Y307N lies within the Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). Y307N has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
P252T missense gain of function - predicted FGFR1 P252T lies within the extracellular domain of the Fgfr1 protein (PMID: 18056464). P252T is predicted to confer a gain of function to the Fgfr1 protein, as demonstrated by altered ligand specificity and increased ligand affinity (PMID: 18056464).
over exp none no effect FGFR1 over exp indicates an over expression of the FGFR1 protein. However, the mechanism causing the over expression is unspecified.
act mut unknown gain of function FGFR1 act mut indicates that this variant results in a gain of function in the FGFR1 protein. However, the specific amino acid change has not been identified.
D128Y missense unknown FGFR1 D128Y does not lie within any known functional domains of the Fgfr1 protein (UniProt.org). D128Y has not been characterized in the scientific literature and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
P252R missense unknown FGFR1 P252R does not lie within any known functional domains of the Fgfr1 protein (UniProt.org). P252R has been identified in sequencing studies (PMID: 23348274), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
P772L missense no effect - predicted FGFR1 P772L lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). P772L has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
R424C missense no effect - predicted FGFR1 R424C lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). R424C has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
FGFR1 - TACC1 fusion gain of function FGFR1-TACC1 results from the fusion of FGFR1 and TACC1, demonstrating transforming ability in culture, tumor growth in xenografts, and increased errors in chromosomal segregation (PMID: 22837387).
T370A missense no effect - predicted FGFR1 T370A lies within the extracellular domain of the Fgfr1 protein (UniProt.org). T370A has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
inact mut unknown loss of function FGFR1 inact mut indicates that this variant results in a loss of function of the Fgfr1 protein. However, the specific amino acid change has not been identified.
V664L missense unknown FGFR1 V664L lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). V664L has been identified in sequencing studies (PMID: 16140923, PMID: 17344846), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
K291E missense no effect - predicted FGFR1 K291E lies within the Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). K291E has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
R576W missense unknown FGFR1 R576W lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). R576W has been identified in sequencing studies (PMID: 16186508), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
E670G missense unknown FGFR1 E670G lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). E670G has not been characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
R646L missense unknown FGFR1 R646L lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). R646L has not been characterized in the scientific literature and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Jan 2018).
R822C missense no effect - predicted FGFR1 R822C lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). R822C has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr1 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr1 protein function.
K656N missense unknown FGFR1 K656N lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). K656N has been identified in sequencing studies (PMID: 30143858, PMID: 24750136, PMID: 23817572), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
C381R missense gain of function - predicted FGFR1 C381R lies within the transmembrane domain of the Fgfr1 protein (UniProt.org). C381R is associated with increased phospho-ERK1/2 staining in a patient tumor sample (PMID: 30385747), and the corresponding variant in an alternate isoform (C379R) demonstrates constitutive Fgfr1 activity in a luciferase assay and increased ERK1/2 phosphorylation in cell culture (PMID: 26272615), and therefore, is predicted to result in gain of Fgfr1 function.
fusion fusion unknown FGFR1 fusion indicates a fusion of the FGFR1 gene, but the fusion partner is unknown.
T695A missense gain of function - predicted FGFR1 T695A lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). T695A has not been biochemically characterized, is predicted to confer a gain of function on the Fgfr1 protein as demonstrated by increased transformation ability in one of two different cell lines as compared to wild-type Fgfr1 (PMID: 29533785).
A263V missense no effect FGFR1 A263V lies within the Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). A263V demonstrates phosphorylation levels similar to wild-type Fgfr1 and is not transforming in culture (PMID: 26826182) and therefore, has no effect on Fgfr1 protein function.
K598N missense unknown FGFR1 K598N lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). K598N has been identified in sequencing studies (PMID: 23525077), but has not been biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown (PubMed, Nov 2018).
Molecular Profile Protein Effect Treatment Approaches
FGFR1 dec exp no effect
FGFR1 dec exp KRAS mut
FGFR1 dec exp KRAS wild-type
FGFR1 Y374C gain of function - predicted
FGFR1 A268S no effect - predicted
FGFR1 P252S gain of function - predicted FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 K655I unknown
FGFR1 K656M unknown
FGFR1 P772S no effect - predicted
FGFR1 W684G unknown
FGFR1 L122F no effect - predicted
FGFR1 R209H no effect - predicted
FGFR1 P123S no effect - predicted
FGFR1 T658P unknown
FGFR1 M456I unknown
FGFR1 mutant unknown
FGFR1 D166del unknown
FGFR1 V561M gain of function - predicted FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 P150S unknown
FGFR1 E334Q unknown
FGFR1 E360K no effect - predicted
FGFR1 G70R unknown
FGFR1 R250Q loss of function - predicted
FGFR1 K656E gain of function FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 D165_D166del unknown
FGFR1 S430F unknown
FGFR1 rearrange unknown
EGFR mutant FGFR1 wild-type
FGFR1 wild-type no effect
FGFR1 S125L unknown
FGFR1 R250W unknown
FGFR1 R78H unknown
FGFR1 N330I unknown
FGFR1 D133E unknown
FGFR1 E138* unknown
FGFR1 G610D unknown
FGFR1 D90V no effect - predicted
FGFR1 Q309* loss of function - predicted
FGFR1 K656D unknown
FGFR1 R507H unknown
FGFR1 amp no effect FGFR Inhibitor (Pan) FGFR1 Inhibitor GSK3052230
EGFR amp FGFR1 amp KRAS G13C
FGFR1 amp MET amp
EGFR amp FGFR1 amp
FGFR1 amp FGFR2 amp
FGFR1 amp KRAS G12V
FGFR1 amp MET dec exp
FGFR1 amp MET pos
FGFR1 amp NRAS amp
EML4-ALK FGFR1 amp
AKT1 S266L FGFR1 amp
FGFR1 amp PIK3CA mutant
FGFR1 amp KRAS amp
EGFR over exp FGFR1 amp
FGFR1 amp MET over exp
FGFR1 amp NRAS over exp
EML4-ALK CDKN2A del FGFR1 T141R SMAD4 Q83*
FGFR1 T141R unknown
FGFR1 A431S unknown
FGFR1 C381Y no effect - predicted
FGFR1 G687V unknown
FGFR1 S135F unknown
FGFR1 N546K gain of function FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 R189H unknown
FGFR1 V102I unknown
FGFR1 V273M no effect - predicted
FGFR1 V460A no effect - predicted
FGFR1 pos FGFR2 pos
FGFR1 positive unknown
FGFR1 Y307N no effect - predicted
FGFR1 P252T gain of function - predicted FGFR Inhibitor (Pan) FGFR1 Inhibitor
EGFR over exp FGFR1 over exp
FGFR1 over exp no effect FGFR Inhibitor (Pan) FGFR1 Inhibitor GSK3052230
FGFR1 over exp PIK3CA mut
EGFR neg FGFR1 over exp
FGFR1 act mut gain of function FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 D128Y unknown
FGFR1 P252R unknown
FGFR1 P772L no effect - predicted
FGFR1 R424C no effect - predicted
FGFR1-TACC1 gain of function FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 T370A no effect - predicted
FGFR1 inact mut loss of function
FGFR1 V664L unknown
FGFR1 K291E no effect - predicted
FGFR1 R576W unknown
FGFR1 E670G unknown
FGFR1 R646L unknown
FGFR1 R822C no effect - predicted
FGFR1 K656N unknown
FGFR1 C381R gain of function - predicted
FGFR1 fusion unknown
FGFR1 T695A gain of function - predicted FGFR Inhibitor (Pan) FGFR1 Inhibitor
FGFR1 A263V no effect
FGFR1 K598N unknown
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR1 dec exp KRAS mut colorectal cancer no benefit Trametinib Preclinical - Cell culture Actionable In a preclinical study, knocking down of Fgfr1 through shRNA did not sensitize KRAS mutant colorectal cancer cells to Mekinist (trametinib) induced growth inhibition in culture (PMID: 27338794). 27338794
FGFR1 dec exp KRAS mut lung cancer sensitive Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, Mekinist (trametinib) treatment demonstrated enhanced growth inhibition in KRAS mutant lung cancer cells with decreased Fgfr1 expression through shRNA knockdown in culture, and tumor regression in xenograft models (PMID: 27338794). 27338794
FGFR1 dec exp KRAS mut pancreatic cancer sensitive Trametinib Preclinical - Cell culture Actionable In a preclinical study, Mekinist (trametinib) treatment demonstrated enhanced growth inhibition of KRAS mutant pancreatic cancer cells with decreased Fgfr1 expression through shRNA knockdown in culture (PMID: 27338794). 27338794
FGFR1 dec exp KRAS wild-type lung cancer no benefit Trametinib Preclinical Actionable In a preclinical study, knocking down of Fgfr1 through shRNA did not sensitize KRAS wild-type lung cancer cells to Mekinist (trametinib) induced growth inhibition in culture (PMID: 27338794). 27338794
FGFR1 mutant transitional cell carcinoma predicted - sensitive Erdafitinib Phase II Actionable In a Phase II trial, Erdafitinib (JNJ-42756493) treatment resulted in an objective response rate of 42% (40/96, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations (J Clin Oncol 36, 2018 (suppl; abstr 4503); NCT02365597). detail...
FGFR1 mutant Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 40% (6/16) of patients with advanced solid tumors harboring FGFR single nucleotide variants, with a 6-month progression-free survival rate of 8% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 mutant Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell line xenograft Actionable In a preclinical study, a variety of cancer cell lines harboring mutations in FGFR1, FGFR2, and/or FGFR3 demonstrated sensitivity to INCB054828 in culture and in cell line xenograft models, resulting in inhibition of tumor growth (Cancer Res 2015;75(15 Suppl):Abstract nr 771). detail...
FGFR1 V561M Advanced Solid Tumor sensitive FIIN-01 Preclinical Actionable In a preclinical study, FIIN-01 inhibited Fgfr1 autophosphorylation in a human transformed embryonic kidney cell line harboring FGFR1 V561M mutation in culture (PMID: 20338520). 20338520
FGFR1 V561M Advanced Solid Tumor sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR1 V561M in culture (PMID: 28978721). 28978721
FGFR1 rearrange lung small cell carcinoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of small cell lung cancer cells harboring FGFR1 translocation in culture (PMID: 27550940). 27550940
FGFR1 rearrange myeloproliferative neoplasm sensitive Dovitinib Preclinical Actionable In a preclinical study, primary cells from 8p11 myeloproliferative syndrome patients harboring FGFR1 rearrangement were sensitive to Dovitinib (TKI258)-induced growth inhibition in culture (PMID: 17698633). 17698633
FGFR1 rearrange leukemia sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of leukemia cells harboring FGFR1 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
EGFR mutant FGFR1 wild-type non-small cell lung carcinoma resistant Ponatinib Preclinical Actionable In a preclinical study, non-small cell lung cancer cells harboring mutant EGFR and wild-type FGFR1 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR1 wild-type lung cancer decreased response AZD4547 Preclinical Actionable In a preclinical study, FGFR1 non-amplified lung cancer cell lines demonstrated reduced sensitivity to AZD4547 induced growth inhibition in culture and in xenograft models (PMID: 23082000). 23082000
FGFR1 wild-type breast cancer resistant Ponatinib Preclinical Actionable In a preclinical study, ER-positive breast cancer cells with wild-type FGFR1 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR1 amp non-small cell lung carcinoma sensitive AZD4547 Preclinical - Pdx Actionable In a preclinical study, AZD4547 inhibited FGFR1 signaling and resulted in tumor regression in patient-derived xenograft models of non-small cell lung carcinoma harboring FGFR1 amplification, wild-type for EGFR, K-Ras and negative for EML4-ALK fusion (PMID: 23082000). 23082000
FGFR1 amp lung squamous cell carcinoma sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of squamous cell lung cancer cell lines harboring FGFR1 amplification (PMID: 22238366). 22238366
FGFR1 amp estrogen-receptor positive breast cancer sensitive Lucitanib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification demonstrated sensitivity to treatment with Lucitanib (E-3810) in culture (PMID: 27126994). 27126994
FGFR1 amp lung squamous cell carcinoma sensitive BGJ398 Phase I Actionable In a Phase I trial, patients with lung squamous cell carcinoma harboring an FGFR1 amplification demonstrated a disease control rate of 50% (18/36) when treated with BGJ398, resulting in 14 patients with stable disease and 4 patients with a partial response (PMID: 27870574). 27870574
FGFR1 amp lung small cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment inhibited growth of FGFR1 amplified lung small cell carcinoma cell lines in culture and in cell line xenograft models (PMID: 23536011). 23536011
FGFR1 amp lung squamous cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp adrenocortical carcinoma sensitive Derazantinib Phase I Actionable In a Phase I trial, ARQ 087 treatment resulted in stable disease with a tumor reduction of 20% in an adrenocortical carcinoma patient harboring FGFR1 amplification, who remained on study for 3.5 years (PMID: 28972963; NCT01752920). 28972963
FGFR1 amp lung cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification were sensitive to PD173074 treatment in culture, demonstrating inhibition of cell growth (PMID: 30140389). 30140389
FGFR1 amp non-small cell lung carcinoma sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a non-small cell lung cancer cell line, harboring FGFR1 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp lung squamous cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a squamous cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151). 28108151
FGFR1 amp lung cancer sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of lung cancer cell lines harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR1 amp Her2-receptor positive breast cancer sensitive Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) promoted 6-month stable disease in Erbb2 (Her2)-positive breast cancer patients with FGFR1 amplification (PMID: 23658459). 23658459
FGFR1 amp lung small cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a small cell lung cancer cell line harboring FGFR1 amplification in culture (PMID: 23082000). 23082000
FGFR1 amp non-small cell lung carcinoma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215). 28630215
FGFR1 amp estrogen-receptor positive breast cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring an FGFR1 amplification demonstrated resistance to Alpelisib (BYL719) in culture (PMID: 27126994). 27126994
FGFR1 amp lung squamous cell carcinoma no benefit AZD4547 Phase I Actionable In a Phase Ib trial, AZD4547 demonstrated limited efficacy in patients with squamous cell lung cancer with FGFR1 amplification, resulting in an overall response rate of 8% (1/15) and a median overall survival of 4.9 months (PMID: 28615371; NCT00979134). 28615371
FGFR1 amp breast cancer sensitive BGJ398 Phase I Actionable In a Phase I trial, 28% (9/32) of breast cancer patients harboring FGFR1 amplification demonstrated stable disease when treated with BGJ398 (PMID: 27870574). 27870574
FGFR1 amp non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215). 28630215
FGFR1 amp lung cancer sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment resulted in greater tumor growth inhibition (56% vs 22%) in cell line xenograft models of FGFR1 amplified lung cancer compared to FGFR1 non-amplified models (PMID: 23536011). 23536011
FGFR1 amp Ewing sarcoma predicted - sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of Ewing’s sarcoma cell lines with FGFR1 copy number gain in culture (PMID: 26179511). 26179511
FGFR1 amp lung carcinoma sensitive Lucitanib Preclinical - Cell line xenograft Actionable in a preclinical study, Lucitanib (E-3810) preferentially inhibited growth of FGFR1-amplified lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 27988457). 27988457
FGFR1 amp synovial sarcoma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 amp lung squamous cell carcinoma no benefit Dovitinib Phase II Actionable In a Phase II clinical trial, dovitinib treatment resulted in a objective response rate of 11.5% (3/26, all partial responses) and disease control rate of 50% (13/26), and a median progression-free survival of 2.9 months in lung squamous cell carcinoma patients with FGFR1 amplification, and FGFR1 amplification was not determined to be a predictive biomarker for sensitivity (PMID: 27315356). 27315356
FGFR1 amp lung adenocarcinoma sensitive PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 64.6% tumor growth inhibition in patient-derived xenograft models of FGFR1-amplified lung adenocarcinoma (PMID: 28978721). 28978721
FGFR1 amp non-small cell lung carcinoma sensitive PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 96.1% tumor growth inhibition in patient-derived xenograft models of FGFR1-amplified non-small cell lung cancer (PMID: 28978721). 28978721
FGFR1 amp non-small cell lung carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma sensitive Cisplatin + Etoposide + GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, addition of GSK3052230 (FP-1039) to Platinol (cisplatin) and Vepesid (etoposide) resulted in improved tumor growth inhibition in cell line xenograft models of FGFR1 amplified lung small cell carcinoma (PMID: 23536011). 23536011
FGFR1 amp lung squamous cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp estrogen-receptor positive breast cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of estrogen receptor (ER)-positive breast cancer cells with FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp synovial sarcoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 amp estrogen-receptor positive breast cancer sensitive Nintedanib Preclinical Actionable In a preclinical study, Ofev (nintedanib) inhibited the growth of ER-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp lung small cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp estrogen-receptor positive breast cancer sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification (PMID: 7506125) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 7506125 27535969
FGFR1 amp breast cancer sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in ER-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp non-small cell lung carcinoma sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment inhibited growth of FGFR1 amplified non-small cell lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 23536011). 23536011
FGFR1 amp synovial sarcoma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 amp breast cancer no benefit AZD4547 Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a response rate of 12.5% (1/8) in patients with FGFR1-amplified breast cancer, and did not meet the predetermined criteria for efficacy (PMID: 27179038). 27179038
FGFR1 amp lung small cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a small cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151). 28108151
FGFR1 amp estrogen-receptor positive breast cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of estrogen receptor (ER)-positive breast cancer cells with FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp lung cancer predicted - sensitive Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Erdafitinib (JNJ-42756493) inhibited FGFR downstream signaling and proliferation of several lung cancer cell lines with FGFR1 amplification in culture, and inhibited tumor growth in an FGFR1-amplified lung cancer cell line xenograft model (PMID: 28341788). 28341788
FGFR1 amp lung cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of lung cancer cells with FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 59% (10/17) of patients with advanced solid tumors harboring FGFR amplification, with a 6-month progression-free survival rate of 15% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 amp estrogen-receptor positive breast cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in estrogen receptor (ER)-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp Her2-receptor negative breast cancer sensitive Pazopanib Clinical Study Actionable In a clinical case study, a patient with ERBB2 (HER2)-receptor negative breast cancer harboring FGFR1 amplification demonstrated antitumor activity when treated with Votrient (pazopanib), including a near complete loss of brain lesions and improved function of the liver (PMID: 29223982). 29223982
FGFR1 amp lung small cell carcinoma sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, a small cell lung cancer cell line harboring FGFR1 amplification demonstrated sensitivity to E7090, resulting in decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp non-small cell lung carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp non-small cell lung carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp lung squamous cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma sensitive FF-284 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of small cell lung cancer cell lines harboring FGFR1 amplification in culture (PMID: 25169980). 25169980
FGFR1 amp lung large cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a large cell lung cancer cell line harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR1 amp non-small cell lung carcinoma predicted - sensitive NGI-1 Preclinical - Cell culture Actionable In a preclinical study, NGI-1 inhibited FGFR1 phosphorylation and proliferation of a FGFR1-amplified cell line dependent on FGFR1 signaling in culture, however, did not inhibit proliferation of an FGFR1-amplified cell line not dependent on FGFR1 signaling (PMID: 27694802). 27694802
FGFR1 amp non-small cell lung carcinoma sensitive FF-284 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of non-small cell lung cancer cell lines harboring FGFR1 amplification in culture (PMID: 25169980). 25169980
FGFR1 amp transitional cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) worked synergistically to induce apoptosis and inhibit growth of a urothelial cell carcinoma cell line with FGFR1 amplification in culture, with increased efficacy over either agent alone (PMID: 28108151). 28108151
EGFR amp FGFR1 amp KRAS G13C lung cancer resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, a lung cancer cell line with co-amplification of FGFR1 and EGFR and harboring KRAS G13C demonstrated insensitivity to Erdafitinib (JNJ-42756493) in culture (PMID: 28341788). 28341788
FGFR1 amp MET amp lung squamous cell carcinoma predicted - resistant BGJ398 Phase I Actionable In a Phase I trial, MET amplification was detected in a squamous cell lung cancer patient harboring FGFR1 amplification whose disease relapsed after 17 months of BGJ398 treatment, supporting a role of MET amplification in drug resistance in FGFR1-amplified lung cancer (PMID: 28630215). 28630215
FGFR1 amp MET amp lung cancer sensitive AZD4547 + Crizotinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Xalkori (crizotinib) synergistically inhibited proliferation of FGFR1 amplified lung cancer cells that acquired resistance to AZD4547 through MET amplification in culture (PMID: 27429073). 27429073
FGFR1 amp MET amp lung cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, MET amplification was identified as the mechanism mediating acquired AZD4547 resistance in a FGFR1 amplified lung cancer cell line in culture (PMID: 27429073). 27429073
EGFR amp FGFR1 amp lung cancer resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, lung cancer cell lines with co-amplification of FGFR1 and EGFR demonstrated insensitivity to Erdafitinib (JNJ-42756493) in culture (PMID: 28341788). 28341788
FGFR1 amp FGFR2 amp breast cancer sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line, harboring FGFR1 amplification and FGFR2 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp KRAS G12V non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling, resulting in growth inhibition in FGFR1-amplified non-small cell lung carcinoma cells overexpressing KRAS G12V in culture (PMID: 28630215). 28630215
FGFR1 amp KRAS G12V lung cancer resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, a lung cancer cell line harboring FGFR1 amplification and KRAS G13C demonstrated insensitivity to Erdafitinib (JNJ-42756493) in culture (PMID: 28341788). 28341788
FGFR1 amp KRAS G12V non-small cell lung carcinoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, overexpression of KRAS G12V in FGFR1-amplified non-small cell lung carcinoma cells resulted in decreased response to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp MET dec exp lung cancer sensitive Rogaratinib Preclinical - Cell culture Actionable In a preclinical study, Rogaratinib (BAY 1163877) inhibited Erk signaling and proliferation of FGFR1-amplified lung cancer cell lines with undetectable Met expression in culture (PMID: 27429073). 27429073
FGFR1 amp MET dec exp lung cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Erk signaling and proliferation of FGFR1-amplified lung cancer cell lines with undetectable Met expression in culture (PMID: 27429073). 27429073
FGFR1 amp MET pos lung cancer resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, FGFR1-amplified lung cancer cell lines with Met expression were resistant to Rogaratinib (BAY 1163877) in culture (PMID: 27429073). 27429073
FGFR1 amp MET pos lung cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, FGFR1-amplified lung cancer cell lines with Met expression were resistant to AZD4547 in culture (PMID: 27429073). 27429073
FGFR1 amp NRAS amp non-small cell lung carcinoma resistant BGJ398 Preclinical - Cell culture Actionable In a preclinical study, amplification of NRAS was identified in a non-small cell lung cancer cell line harboring FGFR1 amplification that acquired resistance to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp NRAS amp non-small cell lung carcinoma resistant Trametinib Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung carcinoma cells harboring both FGFR1 and NRAS amplification were resistant to Mekinist (trametinib) in culture (PMID: 28630215). 28630215
FGFR1 amp NRAS amp non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling, resulting in growth inhibition in non-small cell lung carcinoma cells harboring both FGFR1 and NRAS amplification in culture (PMID: 28630215). 28630215
EML4-ALK FGFR1 amp non-small cell lung carcinoma predicted - resistant Brigatinib Clinical Study Actionable In a clinical study, a non-small cell lung carcinoma patient harboring EML4-ALK treated with Alunbrig (brigatinib) responded, but eventually progressed, and was subsequently found to harbor a presumed resistance alteration, FGFR1 amplification (PMID: 29636358). 29636358
AKT1 S266L FGFR1 amp lung cancer predicted - resistant PD173074 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification demonstrated resistance to increasing concentrations of PD173074 in culture and was subsequently, found to have acquired AKT1 S266L (PMID: 30140389). 30140389
AKT1 S266L FGFR1 amp lung cancer predicted - sensitive GSK2141795 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification and AKT1 S266L demonstrated sensitivity to Uprosertib (GSK2141795) in culture, showing decreased phosphorylation of Akt1 targets and reduced cell growth (PMID: 30140389). 30140389
FGFR1 amp KRAS amp lung cancer resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, a lung cancer cell line with co-amplification of FGFR1 and KRAS demonstrated insensitivity to Erdafitinib (JNJ-42756493) in culture (PMID: 28341788). 28341788
EGFR over exp FGFR1 amp head and neck squamous cell carcinoma sensitive AZD4547 + Gefitinib Preclinical - Cell culture Actionable In a preclinical study, head and neck squamous cell carcinoma cells harboring FGFR1 amplification and over expressing EGFR demonstrated sensitivity to the combination treatment of AZD4547 and Iressa (gefitinib) in culture, which also resulted in a synergistic effect (PMID: 26936917). 26936917
EGFR over exp FGFR1 amp head and neck squamous cell carcinoma resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, head and neck squamous cell carcinoma cells with EGFR over expression and FGFR1 amplification demonstrated resistance to treatment with AZD4547 in culture (PMID: 26936917). 26936917
FGFR1 amp MET over exp lung small cell carcinoma sensitive BGJ398 + Crizotinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Xalkori (crizotinib) synergistically inhibited Erk signaling, resulted in growth inhibition in small cell lung carcinoma cells harboring FGFR1 amplification and Met overexpression in culture (PMID: 28630215). 28630215
FGFR1 amp MET over exp lung small cell carcinoma sensitive BGJ398 + EMD 1214063 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and EMD 1214063 synergistically inhibited growth of small cell lung carcinoma cells harboring FGFR1 amplification and Met overexpression in culture (PMID: 28630215). 28630215
FGFR1 amp MET over exp lung small cell carcinoma resistant BGJ398 Preclinical - Cell culture Actionable In a preclinical study, overexpression and activation of Met was identified in a small cell lung cancer cell line harboring FGFR1 amplification that acquired resistance to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp MET over exp lung cancer resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, MET overexpression and activation was identified as the mechanism mediating acquired Rogaratinib (BAY 1163877) resistance in a FGFR1 amplified lung cancer cell line in culture (PMID: 27429073). 27429073
FGFR1 amp MET over exp lung cancer sensitive Crizotinib + Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Rogaratinib (BAY 1163877) and Xalkori (crizotinib) synergistically inhibited proliferation of FGFR1 amplified lung cancer cells that acquired resistance to Rogaratinib (BAY 1163877) through MET overexpression and activation in culture (PMID: 27429073). 27429073
FGFR1 amp NRAS over exp non-small cell lung carcinoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, overexpression of Nras in FGFR1-amplified non-small cell lung carcinoma cells resulted in decreased response to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp NRAS over exp non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling, resulting in growth inhibition in FGFR1-amplified non-small cell lung carcinoma cells overexpressing Nras in culture (PMID: 28630215). 28630215
EML4-ALK CDKN2A del FGFR1 T141R SMAD4 Q83* pancreatic ductal adenocarcinoma predicted - sensitive Alectinib Clinical Study Actionable In a clinical case study, a pancreatic ductal adenocarcinoma patient harboring EML4-ALK along with CDKN2A deletion, FGFR1 T141R, SMAD4 Q83*, and a TP53 splice site mutation, experienced disease progression after 2 months of Xalkori (crizotinib) treatment, then received Alecensa (alectinib) and remained on treatment for at least 3 months (PMID: 28476735). 28476735
EML4-ALK CDKN2A del FGFR1 T141R SMAD4 Q83* pancreatic ductal adenocarcinoma resistant Crizotinib Clinical Study Actionable In a clinical case study, a pancreatic ductal adenocarcinoma patient harboring EML4-ALK along with CDKN2A deletion, FGFR1 T141R, SMAD4 Q83*, and a TP53 splice site mutation, experienced disease progression after 2 months of Xalkori (crizotinib) treatment, then received Alecensa (alectinib) and remained on treatment for at least 3 months (PMID: 28476735). 28476735
FGFR1 pos FGFR2 pos hepatocellular carcinoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, hepatocellular carcinoma cell lines treated with AZD4547 demonstrated decreased phosphorylation of FGFR1 and FGFR2, reduced colony formation, and evidence of apoptotic activity in culture (PMID: 26351320). 26351320
FGFR1 pos FGFR2 pos hepatocellular carcinoma no benefit PHA-665752 Preclinical - Cell culture Actionable In a preclinical study, PHA-665752 treatment did not result in decreased colony formation or reduced phosphorylation levels of FGFR1 and FGFR2 in hepatocellular carcinoma cells in culture (PMID: 26351320). 26351320
FGFR1 positive leiomyosarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive hemangioma predicted - sensitive Rogaratinib Phase I Actionable In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease with resolution of edema in a patient with FGFR1-positive hemangioendothelioma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR1 positive lung large cell carcinoma sensitive AZD4547 + AZD8055 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and AZD8055 synergistically inhibited survival of FGFR1-dependent lung large cell carcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive synovial sarcoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to BGJ398 in culture (PMID: 27535980). 27535980
FGFR1 positive salivary gland adenoid cystic carcinoma predicted - sensitive Rogaratinib Phase I Actionable In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including a partial remission in a patient with FGFR1-positive adenoid cystic carcinoma of the tongue (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR1 positive leiomyosarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR1 positive lung adenocarcinoma sensitive AZD4547 + AZD8055 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and AZD8055 synergistically inhibited survival of FGFR1-dependent lung adenocarcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive lung large cell carcinoma sensitive AZD4547 + Sirolimus Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Rapamune (sirolimus) synergistically inhibited survival of FGFR1-dependent lung large cell carcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive lung adenocarcinoma sensitive AZD4547 + Sirolimus Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Rapamune (sirolimus) synergistically inhibited survival of FGFR1-dependent lung adenocarcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive synovial sarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR1 positive uterus leiomyosarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR1 positive lung adenocarcinoma sensitive AZD4547 + Vistusertib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 and Vistusertib (AZD2014) synergistically inhibited survival of FGFR1-dependent lung adenocarcinoma cells in culture and in cell line xenograft models (PMID: 26359452). 26359452
FGFR1 positive synovial sarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive head and neck squamous cell carcinoma sensitive AZD4547 + Vistusertib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Vistusertib (AZD2014) synergistically inhibited survival of FGFR1-dependent head and neck squamous cell carcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive uterus leiomyosarcoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to BGJ398 in culture (PMID: 27535980). 27535980
FGFR1 positive leiomyosarcoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to BGJ398 in culture (PMID: 27535980). 27535980
FGFR1 positive uterus leiomyosarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive lung large cell carcinoma sensitive AZD4547 + Vistusertib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 and Vistusertib (AZD2014) synergistically inhibited survival of FGFR1-dependent lung large cell carcinoma cells in culture and in cell line xenograft models (PMID: 26359452). 26359452
EGFR over exp FGFR1 over exp esophageal cancer sensitive Theliatinib Preclinical - Pdx Actionable In a preclinical study, Theliatinib treatment demonstrated decreased efficcacy in patient-derived xenograft (PDX) models of esophageal cancer with both Egfr and Fgfr1 overexpression compared to models with only Egfr overexpression (PMID: 28881608). 28881608
EGFR over exp FGFR1 over exp esophageal cancer sensitive AZD4547 Preclinical - Pdx Actionable In a preclinical study, AZD4547 treatment resulted in tumor regression in patient-derived xenograft (PDX) models, with both Egfr and Fgfr1 overexpression (PMID: 28881608), 28881608
FGFR1 over exp renal cell carcinoma not applicable Sorafenib Phase II Emerging In a clinical analysis of a Phase II trial, high Fgfr1 expression level was associated with decreased progression free survival in renal cell carcinoma patients treated with Nexavar (sorafenib) (PMID: 25900027). 25900027
FGFR1 over exp uterus leiomyosarcoma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp Advanced Solid Tumor sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing wild-type FGFR1 in culture (PMID: 28978721). 28978721
FGFR1 over exp Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr1 in culture (PMID: 27627808). 27627808
FGFR1 over exp head and neck squamous cell carcinoma sensitive BGJ398 Preclinical Actionable In a preclinical study, BGJ398 inhibited cell growth and induced apoptosis in HNSCC cells over expressing Fgfr1 in culture and in xenograft models (PMID: 26015511). 26015511
FGFR1 over exp uterus leiomyosarcoma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp uterus leiomyosarcoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp thyroid cancer sensitive Lenvatinib Preclinical Actionable In a preclinical study, Lenvima (lenvatinib) inhibited FGFR1 phosphorylation and signaling in thyroid cancer cells overexpressing FGFR1 (PMID: 25295214). 25295214
FGFR1 over exp PIK3CA mut estrogen-receptor positive breast cancer sensitive Alpelisib + Lucitanib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line over expressing FGFR1 and expressing a PIK3CA mutation demonstrated sensitivity to the combination of Alpelisib (BYL719) and Lucitanib (E-3810) in culture (PMID: 27126994). 27126994
EGFR neg FGFR1 over exp head and neck squamous cell carcinoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment of head and neck squamous cell carcinoma cells over expressing FGFR1 and negative for EGFR resulted in decreased cell growth and reduced downstream signaling of Erk1/2 (PMID: 26936917). 26936917
FGFR1 act mut Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor decreased response Nintedanib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR1 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor decreased response Cediranib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR1 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Cediranib (AZD-2171) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor sensitive FF-284 Phase I Actionable In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR1 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). detail...
FGFR1 act mut Advanced Solid Tumor sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 act mut breast cancer sensitive FIIN-01 Preclinical Actionable In a preclinical study, FIIN-01 inhibited Fgfr1 activation-induced proliferation and transformation of human breast epithelial cell lines in culture (PMID: 20338520). 20338520
FGFR1 act mut Advanced Solid Tumor sensitive Erdafitinib Phase I Actionable In a Phase I trial, Erdafitinib (JNJ-42756493) treatment resulted in stable disease in 70% (16/23) and partial response in 22% (5/23) of patients with advanced solid tumors harboring FGFR 1-4 activating mutations (including amplifications, mutations and translocations), while no antitumor activity was observed in patients with unknown or no known changes in FGFR (PMID: 26324363). 26324363
FGFR1-TACC1 malignant glioma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR1-TACC1 malignant glioma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR1-TACC1 malignant glioma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BJG398 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR1 fusion Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in 22% (2/9) and stable disease in 55% (5/9) of patients with advanced solid tumors harboring FGFR fusions, with a 6-month progression-free survival rate of 42% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 fusion Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited Erk, Stat5 signaling and survival of transformed cell lines overexpressing FGFR1 fusion proteins (ZMYM2-FGFR1 or BCR-FGFR1) in culture (PMID: 17698633). 17698633
FGFR1 fusion acute myeloid leukemia sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) increased apoptosis and inhibited survival of acute myelogenous leukemia cell lines harboring FGFR1OP2-FGFR1 fusion in culture (PMID: 17698633). 17698633
FGFR1 fusion hematologic cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of hematologic cancer cells harboring FGFROP2-FGFR1 fusion in culture (PMID: 27627808). 27627808