Gene Detail

Gene Symbol FGFR3
Synonyms ACH | CD333 | CEK2 | HSFGFR3EX | JTK4
Gene Description FGFR3 is a receptor tyrosine kinase activated upon binding of the FGF ligand, which activates RAS-MAPK and PI3K-AKT pathways. Altered function of FGFR3 in cancer may lead to increased cell proliferation and decreased apoptosis (PMID: 22508544).
Entrez Id 2261
Chromosome 4
Map Location 4p16.3
Canonical Transcript NM_000142

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Variant Impact Protein Effect Variant Description Associated with drug Resistance
FGFR3 - TACC3 fusion gain of function FGFR3-TACC3 results from the fusion of FGFR3 and TACC3, demonstrating constitutive kinase activity, transforming activity in culture and ability to drive tumor growth in xenografts (PMID: 25294908, PMID: 22837387).
R248C missense gain of function FGFR3 R248C lies within the extracellular domain of the Fgfr3 protein (UniProt.org). R248C confers a gain of function to the Fgfr3 protein as demonstrated by constitutive ligand-independent cell proliferation (PMID: 19381019) and increased activation of the Mapk signaling pathway (PMID: 24626198).
D786N missense gain of function - predicted FGFR3 D786N does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). D786N has not been biochemically characterized, but is predicted to confer a gain of function on the Fgfr3 protein as demonstrated by increased transformation ability (PMID: 29533785).
A391E missense gain of function FGFR3 A391E lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). A391E results in increased dimerization and ligand-independent activation of Fgfr3 in cell culture (PMID: 21536014, PMID: 23437153)
E360Q missense loss of function - predicted FGFR3 E360Q does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). E360Q has not been biochemically characterized, but is predicted to confer a loss of function on the Fgfr3 protein as demonstrated by decreased transformation ability as compared to wild-type Fgfr3 (PMID: 29533785).
K413N missense unknown FGFR3 K413N lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). K413N has been identified in the scientific literature (PMID: 25056374), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
K650N missense gain of function - predicted FGFR3 K650N lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K650N results in constitutive activation of the Fgfr3 protein (PMID: 11055896) and therefore, is predicted to result in a gain of Fgfr3 protein function.
L794R missense unknown FGFR3 L794R lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). L794R has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
K650T missense gain of function - predicted FGFR3 K650T lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K650T results in constitutive activation of the Fgfr3 protein (PMID: 11055896) and therefore, is predicted to result in a gain of Fgfr3 protein function.
V677I missense no effect FGFR3 V677I lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). V677I demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
amp unknown no effect FGFR3 amp indicates an increased number of copies of the FGFR3 gene. However, the mechanism causing the increase is unspecified.
mutant unknown unknown FGFR3 mutant indicates an unspecified mutation in the FGFR3 gene.
S371C missense gain of function FGFR3 S371C lies within the extracellular domain of the Fgfr3 protein (UniProt.org). S371C confers a gain of function to the Fgfr3 protein, resulting in dimerization, constitutive activation, and increased MAPK pathway signaling (PMID: 12009017).
P283S missense unknown FGFR3 P283S lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). P283S has been identified in sequencing studies (PMID: 26003532, PMID: 27998968), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
V306I missense unknown FGFR3 V306I lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). V306I has been identified in the scientific literature (PMID: 23443805), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
D764H missense unknown FGFR3 D764H (corresponds to D762H in the canonical isoform) lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). D764H has not been fully biochemically characterized, and is conflicting as it results in increased proliferation in some cell culture conditions, but not others (PMID: 27053219) and therefore, its effect on Fgfr3 protein function is unknown.
F384L missense no effect FGFR3 F384L lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). F384L does not result in activation of Fgfr3 and is not transforming in cell culture (PMID: 11157491, PMID: 29533785).
K319del missense no effect - predicted FGFR3 K319del results in the deletion of an amino acid in the Fgfr3 protein at amino acid 319 (UniProt.org). K319del has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
V172I missense loss of function - predicted FGFR3 V172I lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). V172I has not been biochemically characterized, but is predicted to confer a loss of function on the Fgfr3 protein as demonstrated by decreased transformation ability in cell culture as compared to wild-type Fgfr3 (PMID: 29533785).
T79S missense unknown FGFR3 T79S lies within the Ig-like C2-type domain 1 of the Fgfr3 protein (UniProt.org). T79S has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
R805Q missense no effect - predicted FGFR3 R805Q does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). R805Q has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
D646Y missense no effect FGFR3 D646Y lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). D646Y demonstrates autophosphorylation and substrate phosphorylation similar to the level of wild-type Fgfr3 in cell culture (PMID: 26992226).
L794fs frameshift unknown FGFR3 L794fs results in a change in the amino acid sequence of the Fgfr3 protein beginning at aa 794 of 806, likely resulting in a premature truncation of the functional protein (UniProt.org). L794fs has been identified in sequencing studies (PMID: 25157968), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
N653H missense no effect FGFR3 N653H lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). N653H demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
E456K missense unknown FGFR3 E456K lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). E456K has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, May 2018).
Y375C missense gain of function FGFR3 Y375C (corresponds to Y373C in the canonical isoform) lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). Y375C confers a gain of function to the Fgfr3 protein as demonstrated by ligand-independent constitutive phosphorylation in vitro and transformation of cells in culture (PMID: 19749790).
inact mut unknown loss of function FGFR3 inact mut indicates that this variant results in a loss of function of the Fgfr3 protein. However, the specific amino acid change has not been identified.
G235D missense unknown FGFR3 G235D lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). G235D has been identified in the scientific literature (PMID: 27271022), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
D788N missense unknown FGFR3 D788N (corresponds to D785N in the canonical isoform) lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). D788N has not been fully biochemically characterized, and is conflicting as it results in increased proliferation in some cell culture conditions, but not others (PMID: 27053219) and therefore, its effect on Fgfr3 protein function is unknown.
E322K missense unknown FGFR3 E322K lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). E322K has been identified in sequencing studies (PMID: 26003532, PMID: 11325814), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
V700A missense unknown FGFR3 V700A lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). V700A has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
S351C missense loss of function - predicted FGFR3 S351C lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). S351C has not been biochemically characterized, but is predicted to confer a loss of function on the Fgfr3 protein as demonstrated by decreased transformation ability in cell culture as compared to wild-type Fgfr3 (PMID: 29533785).
R669Q missense gain of function - predicted FGFR3 R669Q lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). R669Q results in increased Fgfr3 autophosphorylation in cell culture (PMID: 26992226) and therefore, is predicted to result in a gain of Fgfr3 protein function.
Y647C missense gain of function - predicted FGFR3 Y647C lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). Y647C results in increased Fgfr3 autophosphorylation in cell culture (PMID: 26992226) and therefore, is predicted to result in a gain of Fgfr3 protein function.
V50I missense gain of function - predicted FGFR3 V50I lies within the Ig-like C2-type domain 1 of the Fgfr3 protein (UniProt.org). V50I has not been biochemically characterized, but is predicted to confer a gain of function on the Fgfr3 protein as demonstrated by increased transformation ability in cell culture (PMID: 29533785).
R640W missense unknown FGFR3 R640W lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). R640W has been identified in sequencing studies (PMID: 26517354), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
C582F missense no effect FGFR3 C582F lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). C582F demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
G197S missense unknown FGFR3 G197S lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). G197S has been identified in sequencing studies (PMID: 17344920), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
Y373C missense gain of function FGFR3 Y373C lies within the extracellular domain of the Fgfr3 protein (UniProt.org). Y373C confers a gain of function to the Fgfr3 protein resulting in constitutive activation, downstream signaling, and transformation of cultured cells (PMID: 11429702).
K508M missense loss of function FGFR3 K508M lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K508M confers a loss of function to the Fgfr3 protein as demonstrated by induction of growth arrest in cell culture and inactivation of Stat1 in vitro (PMID: 19088846) and loss of kinase activity in the context of Fgfr3-Tacc3 (PMID: 22837387).
G697C missense no effect FGFR3 G697C lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). G697C demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3, and is not transforming in cell culture (PMID: 26992226).
I376C missense unknown FGFR3 I376C lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). I376C has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
dec exp none no effect FGFR3 dec exp indicates decreased expression of the Fgfr3 protein. However, the mechanism causing the decreased expression is unspecified.
R421Q missense unknown FGFR3 R421Q lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). R421Q has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
D617G missense loss of function - predicted FGFR3 D617G lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). D617G results in a loss of Fgfr3 activity in cell culture (PMID: 26992226) and therefore, is predicted to result in a loss of Fgfr3 protein function.
S249C missense gain of function FGFR3 S249C lies within the linker region between IgD2 and IgD3 of the Fgfr3 protein (PMID: 19381019). S249C confers a gain of function to the Fgfr3 protein as demonstrated by stabilized homodimer formation and constitutive phosphorylation in vitro (PMID: 17384684) and constitutive ligand-independent cell proliferation in culture (PMID: 19381019, PMID: 29533785).
F386L missense unknown FGFR3 F386L lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). F386L is a common Fgfr3 polymorphism (PMID: 19377444), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
K652E missense gain of function - predicted FGFR3 K652E (corresponds to K649E in the canonical isoform) lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K652E was demonstrated to induce transformation of mouse fibroblasts, but had a lesser degree of signaling and phenotypic effect in immortalized normal human urothelial cells (PMID: 19749790) and therefore, is predicted to result in a gain of Fgfr3 protein function.
P795A missense unknown FGFR3 P795A lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). P795A has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
V329A missense unknown FGFR3 V329A lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). V329A has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
L645V missense unknown FGFR3 L645V lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). L645V has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
P253_I254insHIA insertion unknown FGFR3 P253_I254insHIA results in the insertion of three amino acids in the Ig-like C2-type domain 3 of the Fgfr3 protein between amino acids 253 and 254 (UniProt.org). P253_I254insHIA has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
D762H missense no effect - predicted FGFR3 D762H does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). D762H has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
H643D missense no effect FGFR3 H643D lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). H643D demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
G382R missense gain of function FGFR3 G382R lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). G382R results in increased Fgfr3 protein dimerization and constitutive activation (PMID: 16841094), and has also been shown to inhibit receptor internalization (PMID: 17172848).
V555M missense gain of function FGFR3 V555M lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). V555M results in increased Fgfr3 autophosphorylation and substrate phosphorylation in cell culture (PMID: 26992226).
N540S missense gain of function - predicted FGFR3 N540S lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). N540S results in increased Fgfr3 autophosphorylation in cell culture (PMID: 26992226) and therefore, is predicted to result in a gain of Fgfr3 protein function.
V390M missense no effect - predicted FGFR3 V390M does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). V390M has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
S187Y missense no effect - predicted FGFR3 S187Y lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). S187Y has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
I538F missense no effect FGFR3 I538F lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). I538F demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
R603Q missense unknown FGFR3 R603Q lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). R603Q has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
S400fs frameshift loss of function - predicted FGFR3 S400fs results in a change in the amino acid sequence of the Fgfr3 protein beginning at aa 400 of 806, likely resulting in a premature truncation of the functional protein (UniProt.org). Due to a loss of the protein kinase domain (UniProt.org), S400fs is predicted to lead to a loss of Fgfr3 protein function.
D222N missense unknown FGFR3 D222N lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). D222N has been identified in the scientific literature (PMID: 27271022), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
fusion fusion unknown FGFR3 fusion indicates a fusion of the FGFR3 gene, but the fusion partner is unknown.
S679F missense unknown FGFR3 S679F lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). S679F has been identified in sequencing studies (PMID: 27998968) but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
R124W missense gain of function - predicted FGFR3 R124W lies within the Ig-like C2-type domain 1 of the Fgfr3 protein (UniProt.org). R124W has not been biochemically characterized, but is predicted to confer a gain of function on the Fgfr3 protein as demonstrated by increased transformation ability in cell culture (PMID: 29533785).
G637W missense loss of function - predicted FGFR3 G637W lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). G637W results in a loss of Fgfr3 kinase activity in cell culture (PMID: 26992226) and therefore, is predicted to result in a loss of Fgfr3 protein function.
T394M missense no effect - predicted FGFR3 T394M does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). T394M has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
G65R missense unknown FGFR3 G65R lies within the Ig-like C2-type domain 1 of the Fgfr3 protein (UniProt.org). G65R has not been characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
V630M missense no effect FGFR3 V630M lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). V630M demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
Q209H missense unknown FGFR3 Q209H lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). Q209H has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
P572A missense no effect FGFR3 P572A lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). P572A demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
V555L missense unknown FGFR3 V555L lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). V555L has not been biochemically has been demonstrated to confer resistance to Fgfr inhibitors in cell culture (PMID: 28034880), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018). Y
G372C missense gain of function FGFR3 G372C (equivalent to G370C in isoform1) lies within the extracellular domain of the Fgfr3 protein (UniProt.org). G372C confers a gain of function on Fgfr3, as indicated by ligand-independent phosphorylation and dimerization of Fgfr3, and activation of MAPK pathway in cell culture (PMID: 16841094, PMID: 12009017).
G380R missense gain of function FGFR3 G380R lies within the transmembrane domain of the Fgfr3 protein (PMID: 20624921). G380R results in increased ligand-independent phosphorylation of Fgfr3 and enhanced ligand-dependent activation of downstream signaling, but is not transforming in cell culture (PMID: 20624921, PMID: 9136983, PMID: 10611230).
K650E missense gain of function - predicted FGFR3 K650E lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K650E results in constitutive activation of the Fgfr3 protein (PMID: 11055896) and therefore, is predicted to result in a gain of Fgfr3 protein function.
L608V missense unknown FGFR3 L608V lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). L608V has been demonstrated to confer resistance to Fgfr inhibitors in cell culture (PMID: 28034880), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018). Y
Y241C missense unknown FGFR3 Y241C lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). Y241C has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
R248H missense unknown FGFR3 R248H lies within the extracellular domain of the Fgfr3 protein (UniProt.org). R248H has been identified in the scientific literature (PMID: 24452392), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
K650Q missense gain of function - predicted FGFR3 K650Q lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K650Q has not been characterized, however other K650 mutations result in constitutive activation of the Fgfr3 protein thus K650Q is predicted to result in a gain of function (PMID: 11055896).
P91L missense unknown FGFR3 P91L lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). P91L has been identified in the scientific literature (PMID: 26907448), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
act mut unknown gain of function FGFR3 act mut indicates that this variant results in a gain of function in the FGFR3 protein. However, the specific amino acid change has not been identified.
E216K missense unknown FGFR3 E216K lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). E216K has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
K715M missense unknown FGFR3 K715M lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K715M has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
Q256R missense unknown FGFR3 Q256R lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). Q256R has been identified in sequencing studies (PMID: 28199989) but has not been biochemically and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
A452S missense no effect - predicted FGFR3 A452S does not lie within any known functional domains of Fgfr3 protein (UniProt.org). A452S has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
FGFR3 - BAIAP2L1 fusion gain of function FGFR3-BAIAP2L1 results from the fusion of FGFR3 and BAIAP2L1, demonstrating constitutive activation and transformation of cells in culture (PMID: 23175443).
A634T missense unknown FGFR3 A634T lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). A634T has not been biochemically characterized and demonstrates decreased transformation ability in one of two different cell lines as compared to wild-type Fgfr3 (PMID: 29533785) and therefore, its effect on Fgfr3 protein function is unknown.
R112Q missense unknown FGFR3 R112Q lies within the Ig-like C2-type domain 1 of the Fgfr3 protein (UniProt.org). R112Q has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
K650M missense gain of function FGFR3 K650M lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). K650M confers a gain of function to the Fgfr3 protein as demonstrated by ligand-dependent autophosphorylation, activation of Mapk signaling (PMID: 9857065), and activation of Stat1 in kinase assays (PMID: 19088846).
wild-type none no effect Wild-type FGFR3 indicates that no mutation has been detected within the FGFR3 gene.
A391V missense no effect - predicted FGFR3 A391V lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). A391V has not been biochemically characterized, but results in similar cell proliferation and viability levels to wild-type Fgfr3 in culture (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
rearrange unknown unknown FGFR3 rearrangement indicates an unspecified rearrangement of the FGFR3 gene.
G370C missense gain of function FGFR3 G370C lies within the juxtamembrane region of the Fgfr3 protein (PMID: 12009017). G370C confers a gain of function to the Fgfr3 protein, resulting in increased Fgfr3 phosphorylation compared to wild-type and constitutive activation of the mitogen activated protein kinase (MAPK) signaling pathway (PMID: 12009017).
C228R missense gain of function - predicted FGFR3 C228R lies within the Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). C228R results in stabilization of Fgfr3 dimers in culture (PMID: 27596331) and therefore, is predicted to result in a gain of Fgfr3 protein function.
R669G missense gain of function FGFR3 R669G lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). R669G results in increased Fgfr3 autophosphorylation and substrate phosphorylation in cell culture (PMID: 26992226).
V788M missense gain of function - predicted FGFR3 V788M does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). V788M has not been biochemically characterized, but is predicted to confer a gain of function on the Fgfr3 protein as demonstrated by increased transformation ability in cell culture (PMID: 29533785).
G382D missense gain of function - predicted FGFR3 G382D lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). G382D results in constitutive activation of Fgfr3 and downstream signaling, but is not transforming in cell culture (PMID: 11429702).
N540V missense unknown FGFR3 N540V lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). N540V has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
H274Y missense no effect - predicted FGFR3 H274Y lies within the Ig-like C2 type domain 3 of the Fgfr3 protein (UniProt.org). H274Y has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
I538V missense gain of function - predicted FGFR3 I538V lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). I538V results in increased Fgfr3 autophosphorylation in cell culture (PMID: 26992226) and therefore, is predicted to result in a gain of Fgfr3 protein function.
FGFR3 - ELAVL3 fusion unknown FGFR3-ELAVL3 results from the fusion of FGFR3 and ELAVL3 (PMID: 25204415). FGFR3-ELAVL3 has been identified in glioma (PMID: 25204415, PMID: 26061751), but has not been biochemically characterized and therefore, its effect on protein function is unknown (PubMed, Jan 2018).
D785N missense no effect - predicted FGFR3 D785N does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). D785N has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
Y379C missense unknown FGFR3 Y379C lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). Y379C has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
E627D missense no effect FGFR3 E627D lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). E627D demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
R399C missense no effect - predicted FGFR3 R399C lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). R399C has not been biochemically characterized, but results in similar cell proliferation and viability levels to wild-type Fgfr3 in culture (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
over exp none no effect FGFR3 over exp indicates an over expression of the Fgfr3 protein. However, the mechanism causing the over expression is unspecified.
S433C missense unknown FGFR3 S433C lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). S433C has been identified in the scientific literature (PMID: 17344920), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
G384D missense unknown FGFR3 G384D (corresponds to G382D in the canonical isoform) lies within a pentameric consensus region in the transmembrane domain of the Fgfr3 protein (PMID: 11429702). G384D has variable effects on activation of Fgfr3, and is not transforming in cell culture (PMID: 11429702), and therefore, its effect on Fgfr3 protein function is unknown.
L385M missense unknown FGFR3 L385M lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). L385M has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
positive unknown unknown FGFR3 positive indicates the presence of the ESR1 gene, mRNA, and/or protein.
H349Y missense unknown FGFR3 H349Y lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). H349Y has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
R200C missense gain of function FGFR3 R200C lies within the Ig-like C2-type 2 domain of the Fgfr3 protein (UniProt.org). R200C confers a gain of function to the Fgfr3 protein resulting in dimerization and constitutive activation (PMID: 16912704).
S131L missense unknown FGFR3 S131L lies within the extracellular domain of the Fgfr3 protein (UniProt.org). S131L has not been biochemically characterized, but results in increased proliferation under some cell culture conditions (PMID: 27053219), and in another study, S131L had decreased cell proliferation and cell viability as compared to wild-type Fgfr3 (PMID: 29533785).
V642M missense no effect - predicted FGFR3 V642M lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). V642M has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
S780C missense no effect - predicted FGFR3 S780C does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). S780C has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
E466K missense no effect FGFR3 E466K lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). E466K demonstrates Fgfr3 autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
A500T missense no effect FGFR3 A500T lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). A500T demonstrates autophosphorylation and substrate phosphorylation similar to wild-type Fgfr3 in cell culture (PMID: 26992226).
G710D missense unknown FGFR3 G710D lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). G710D has not been characterized in the scientific literature and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
D641N missense gain of function FGFR3 D641N lies within the TK-2 domain of the Fgfr3 protein (PMID: 19287463). D641N results in increased Fgfr3 autophosphorylation and substrate phosphorylation in cell culture (PMID: 26992226).
P402S missense no effect - predicted FGFR3 P402S does not lie within any known functional domains of the Fgfr3 protein (UniProt.org). P420S has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Fgfr3 (PMID: 29533785) and therefore, is predicted to have no effect on Fgfr3 protein function.
A341T missense unknown FGFR3 A341T lies within the Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). A341T has been identified in sequencing studies (PMID: 26003532), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
D641G missense gain of function FGFR3 D641G lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). D641G results in increased Fgfr3 autophosphorylation and substrate phosphorylation in cell culture (PMID: 26992226).
E686K missense unknown FGFR3 E686K lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). E686K has been identified in the scientific literature (PMID: 19327639), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
N540T missense unknown FGFR3 N540T lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). N540T has been identified in the scientific literature (PMID: 9452043), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jan 2018).
N540K missense gain of function FGFR3 N540K lies within the protein kinase domain of the Fgfr3 protein (UniProt.org). N540K results in increased Fgfr3 autophosphorylation and substrate phosphorylation, and is transforming in cell culture (PMID: 26992226).
A257V missense unknown FGFR3 A257V lies within the Ig-like C2 type domain 3 of the Fgfr3 protein (UniProt.org). A257V has been identified in sequencing studies (PMID: 27502722), but has not been biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown (PubMed, Jun 2018).
Molecular Profile Protein Effect Treatment Approaches
EGFR L747_A750delinsP FGFR3-TACC3
FGFR3-TACC3 gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor U0126
EGFR L858R FGFR3-TACC3
EGFR E746_A750del FGFR3-TACC3
FGFR2 fusion FGFR3 - TACC3
FGFR3 R248C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 D786N gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 A391E gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 E360Q loss of function - predicted
FGFR3 K413N unknown
FGFR3 K650N gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 L794R unknown
FGFR3 K650T gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V677I no effect
FGFR3 amp no effect FGFR Inhibitor (Pan) FGFR3 Antibody FGFR3 Inhibitor
ROS1 fusion ERBB2 amp FGFR3 amp RET amp
FGFR3 mut FGFR3 over exp
FGFR3 mutant unknown
FGFR3 S371C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 P283S unknown
FGFR3 V306I unknown
FGFR3 D764H unknown
FGFR3 F384L no effect
FGFR3 K319del no effect - predicted
FGFR3 V172I loss of function - predicted
FGFR3 T79S unknown
FGFR3 R805Q no effect - predicted
FGFR3 D646Y no effect
FGFR3 L794fs unknown
FGFR3 N653H no effect
FGFR3 E456K unknown
FGFR3 Y375C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 inact mut loss of function
FGFR3 G235D unknown
FGFR3 D788N unknown
FGFR3 E322K unknown
FGFR3 V700A unknown
FGFR3 S351C loss of function - predicted
FGFR3 R669Q gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 Y647C gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V50I gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R640W unknown
FGFR3 C582F no effect
FGFR3 G197S unknown
FGFR3 Y373C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 Y373C FGFR3 over exp
AKT1 E17K FGFR3 Y373C
FGFR3 K508M loss of function
FGFR3 G697C no effect
FGFR3 I376C unknown
FGFR3 dec exp KRAS mut
FGFR3 wild-type FGFR3 dec exp HRAS G12V
FGFR3 dec exp no effect
FGFR3 R421Q unknown
FGFR3 D617G loss of function - predicted
FGFR3 S249C FGFR3 over exp
FGFR3 S249C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 F386L unknown
FGFR3 K652E gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 P795A unknown
FGFR3 V329A unknown
FGFR3 L645V unknown
FGFR3 P253_I254insHIA unknown
FGFR3 D762H no effect - predicted
FGFR3 H643D no effect
FGFR3 G382R gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 L608V FGFR3 V555M
FGFR3 V555M gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 N540S gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V390M no effect - predicted
FGFR3 S187Y no effect - predicted
FGFR3 I538F no effect
FGFR3 R603Q unknown
FGFR3 S400fs loss of function - predicted
FGFR3 D222N unknown
FGFR3 fusion unknown
FGFR3 S679F unknown
FGFR3 R124W gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G637W loss of function - predicted
FGFR3 T394M no effect - predicted
FGFR3 G65R unknown
FGFR3 V630M no effect
FGFR3 Q209H unknown
FGFR3 P572A no effect
FGFR3 V555L unknown
FGFR3 G372C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G380R gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 K650E FGFR3 over exp HRAS K117E
FGFR3 K650E gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
HRAS K117E FGFR3 K650E
FGFR3 L608V unknown
FGFR3 Y241C unknown
FGFR3 R248H unknown
FGFR3 K650Q gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 P91L unknown
FGFR3 act mut gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 E216K unknown
FGFR3 K715M unknown
FGFR3 Q256R unknown
FGFR3 A452S no effect - predicted
FGFR3-BAIAP2L1 gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 A634T unknown
FGFR3 R112Q unknown
FGFR3 K650M gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 wild-type no effect
FGFR3 A391V no effect - predicted
FGFR3 rearrange unknown
FGFR3 G370C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 C228R gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R669G gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V788M gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G382D FGFR3 over exp
FGFR3 G382D gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 N540V unknown
FGFR3 H274Y no effect - predicted
FGFR3 I538V gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3-ELAVL3 unknown
FGFR3 D785N no effect - predicted
FGFR3 Y379C unknown
FGFR3 E627D no effect
FGFR3 R399C no effect - predicted
FGFR3 G384D FGFR3 over exp
FGFR3 over exp no effect FGFR Inhibitor (Pan) FGFR3 Antibody FGFR3 Inhibitor
FGFR3 S433C unknown
FGFR3 G384D unknown
FGFR3 L385M unknown
FGFR3 positive unknown
FGFR2 pos FGFR3 pos
FGFR3 H349Y unknown
FGFR3 R200C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 S131L unknown
FGFR3 V642M no effect - predicted
FGFR3 S780C no effect - predicted
FGFR3 E466K no effect
FGFR3 A500T no effect
FGFR3 G710D unknown
FGFR3 D641N gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 P402S no effect - predicted
FGFR3 A341T unknown
FGFR3 D641G gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 E686K unknown
FGFR3 N540T unknown
FGFR3 N540K gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 A257V unknown
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
EGFR L747_A750delinsP FGFR3-TACC3 non-small cell lung carcinoma predicted - resistant Erlotinib Clinical Study Actionable In a clinical study, a patient with non-small cell lung cancer initially responded to Tarceva (erlotinib), EGFR L747_A750delinsP and FGFR3-TACC3 were identified in post-progression tumor samples (PMID: 29883838). 29883838
FGFR3-TACC3 urinary bladder cancer sensitive FIIN-01 Preclinical Actionable In a preclinical study, FIIN-1 inhibited growth of the RT4 bladder cancer cell line, which has been demonstrated to harbor an FGFR3-TACC3 fusion, in culture (PMID: 20338520, PMID: 23175443). 23175443 20338520
FGFR3-TACC3 malignant glioma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). 22837387
FGFR3-TACC3 urinary bladder cancer sensitive AZ8010 Preclinical Actionable In a preclinical study, AZ12908010 (AZ8010) induced cell cycle arrest and inhibited proliferation of urothelial cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 22869148, PMID: 23175443). 22869148 23175443
FGFR3-TACC3 non-small cell lung carcinoma sensitive Erdafitinib Preclinical - Pdx Actionable In a preclinical study, Erdafitinib (JNJ-42756493) inhibited pERK signaling and tumor growth in a patient-derived xenograft (PDX) model of non-small cell lung cancer harboring FGFR3-TACC3 (PMID: 28341788). 28341788
FGFR3-TACC3 urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cell lines harboring FGFR3-TACC3 fusion in culture (PMID: 27627808). 27627808
FGFR3-TACC3 urinary bladder cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of bladder cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 24325461, PMID: 23175443). 23175443 24325461
FGFR3-TACC3 oligodendroglioma sensitive PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in tumor regression in patient-derived xenograft models of anaplastic oligodendroglioma harboring FGFR3-TACC3 fusion (PMID: 28978721). 28978721
FGFR3-TACC3 lung adenocarcinoma sensitive BGJ398 Preclinical Actionable In a preclinical study, BGJ398 inhibited growth and FGFR3 phosphorylation in cells expressing FGFR3-TACC3 fusion in culture (PMID: 25294908). 25294908
FGFR3-TACC3 transitional cell carcinoma predicted - sensitive Alpelisib + BGJ398 Phase I Actionable In a Phase Ib trial, BGJ398 and Alpelisib (BYL719) combination treatment resulted in partial response and a complete shrinkage of target lesions lasting 4 months in one urothelial carcinoma patient harboring a FGFR3-TACC3 fusion (J Clin Oncol 34, 2016 (suppl; abstr 2500)). detail...
FGFR3-TACC3 urinary bladder cancer sensitive SU5402 Preclinical Actionable In a preclinical study, SU5402 induced cell-cycle arrest and inhibited proliferation of bladder cancer cells that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 21119661, PMID: 23175443). 21119661 23175443
FGFR3-TACC3 malignant glioma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BJG398 inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). 22837387
FGFR3-TACC3 urinary system cancer sensitive Erdafitinib Phase I Actionable In a Phase I clinical trial, Erdafitinib (JNJ-42756493) treatment resulted in partial response in 2 urothelial cancer patients harboring FGFR3-TACC3 (PMID: 26324363). 26324363
FGFR3-TACC3 urinary bladder cancer sensitive LY2874455 Preclinical Actionable In a preclinical study, LY2874455 induced tumor regression in bladder cancer xenograft models that have been demonstrated to harbor an FGFR3-TACC3 fusion (PMID: 21900693, PMID: 23175443). 21900693 23175443
FGFR3-TACC3 urinary bladder cancer sensitive R3Mab Preclinical - Cell line xenograft Actionable In a preclinical study, R3Mab inhibited FGFR3 signaling and tumor growth in bladder cancer cell line xenograft models harboring FGFR3-TACC3 (PMID: 25326231). 25326231
FGFR3-TACC3 bladder transitional cell papilloma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3-TACC3 malignant glioma sensitive Erdafitinib Preclinical Actionable In a preclinical study, Erdafitinib (JNJ-42756493) inhibited proliferation of glioma cells harboring FGFR3 - TACC3 fusion in culture and xenograft tumor growth in animal models (PMID: 25609060). 25609060
FGFR3-TACC3 bladder urothelial carcinoma sensitive PRN1371 Preclinical - Cell line xenograft Actionable In a preclinical study, PRN1371 inhibited proliferation of bladder transitional cell carcinoma cell lines harboring FGFR3-TACC3 fusion in culture and tumor growth in cell line xenograft models (PMID: 28978721). 28978721
FGFR3-TACC3 urinary bladder cancer sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, urinary bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability, and antitumor activity in xenograft models (PMID: 27535969). 23175443 27535969
FGFR3-TACC3 glioblastoma multiforme sensitive U0126 Preclinical Actionable In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells expressing the FGFR3-TACC3 fusion in culture (PMID: 23298836). 23298836
FGFR3-TACC3 transitional cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell line xenograft 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 harboring FGFR3-TACC3 in culture, and inhibited tumor growth in xenograft models, with increased efficacy over either agent alone (PMID: 28108151). 28108151
FGFR3-TACC3 urinary bladder cancer sensitive ASP5878 Preclinical - Cell line xenograft Actionable In a preclinical study, ASP5878 treatment inhibited proliferation of bladder cancer cell lines harboring a FGFR3-TACC3 fusion in culture, and resulted in tumor regression in a FGFR3-TACC3 positive bladder cancer cell line xenograft model (Mol Cancer Ther December 2015 14; A170). detail...
FGFR3-TACC3 urinary bladder cancer sensitive FF-284 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of bladder cancer cell lines harboring an FGFR3-TACC3 fusion in culture and inhibited tumor growth in FGFR3-TACC3-positive bladder cancer cell line xenograft models (PMID: 25169980). 25169980
FGFR3-TACC3 urinary bladder cancer sensitive Pazopanib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to Votrient (pazopanib) in culture (PMID: 23558953). 23558953
FGFR3-TACC3 bladder transitional cell papilloma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3-TACC3 urinary bladder cancer no benefit Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3-TACC were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR3-TACC3 malignant glioma sensitive PD173074 Preclinical - Cell line xenograft Actionable In a preclinical study, PD173074 inhibited Fgfr3 kinase activity and growth in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture and in cell line xenograft models (PMID: 22837387). 22837387
FGFR3-TACC3 transitional cell carcinoma predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with urothelial transitional cell carcinoma harboring FGFR3-TACC3 (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR3-TACC3 cervical squamous cell carcinoma predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with squamous cell carcinoma of the cervix harboring FGFR3-TACC3 (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR3-TACC3 glioblastoma multiforme sensitive Erdafitinib Phase I Actionable In a Phase I trial, Erdafitinib (JNJ-42756493) treatment resulted in tumor reduction and stable disease in 2 glioblastoma multiforme patients harboring FGFR3 - TACC3 fusion (PMID: 25609060). 25609060
FGFR3-TACC3 glioblastoma multiforme sensitive Erdafitinib Phase I Actionable In a Phase I trial, Erdafitinib (JNJ-42756493) treatment resulted in partial response in a glioblastoma patient harboring FGFR3 - TACC3 fusion (PMID: 26324363). 26324363
FGFR3-TACC3 lung adenocarcinoma sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatanib) inhibited growth and FGFR3 phosphorylation in cells expressing FGFR3-TACC3 fusion in culture (PMID: 25294908). 25294908
FGFR3-TACC3 Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinicl study, AZD4547 inhibited proliferation of transformed cells over expressing FGFR3-TACC3 in culture (PMID: 26992226). 26992226
FGFR3-TACC3 urinary bladder cancer sensitive PRN1109 Preclinical - Cell line xenograft Actionable In a preclinical study, PRN1109 treatment resulted in tumor regression in bladder cancer cell line xenograft models harboring FGFR3-TACC3 fusion (Eu J Cancer 2014 Vol 50, Suppl 6:157). detail...
FGFR3-TACC3 Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinicl study, Erdafitinib (JNJ-42756493) inhibited proliferation of transformed cells over expressing FGFR3-TACC3 in culture (PMID: 26992226). 26992226
FGFR3-TACC3 urinary bladder cancer predicted - sensitive S-49076 Preclinical Actionable In a preclinical study, S-49076 inhibited autophosphorylation of FGFR3 and downstream signaling in bladder cancer cells that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 23804704, PMID: 23175443). 23175443 23804704
EGFR L858R FGFR3-TACC3 non-small cell lung carcinoma resistant Afatinib + Cetuximab Clinical Study Actionable In a clinical study, FGFR3-TACC3 was identified as an acquired resistance mutation in a patient with non-small cell lung cancer harboring EGFR L858R, whose disease progressed after initial response to Gilotrif (afatinib) and Erbitux (cetuximab) combination therapy (PMID: 29883838). 29883838
EGFR E746_A750del FGFR3-TACC3 non-small cell lung carcinoma resistant Naquotinib Clinical Study Actionable In a clinical study, FGFR3-TACC3 was identified as an acquired resistance mutation in a patient with non-small cell lung cancer harboring EGFR E746_A750del, whose disease progressed after initial response to Tarceva (erlotinib) followed by Naquotinib (ASP8273) (PMID: 29883838). 29883838
EGFR E746_A750del FGFR3-TACC3 non-small cell lung carcinoma resistant Osimertinib Clinical Study Actionable In a clinical study, FGFR3-TACC3 was identified as an acquired resistance mutation in a patient with non-small cell lung cancer harboring EGFR E746_A750del, whose disease progressed after initial response to Tarceva (erlotinib), followed by Tagrisso (osimertinib) (PMID: 29883838). 29883838
EGFR E746_A750del FGFR3-TACC3 non-small cell lung carcinoma resistant Afatinib Clinical Study Actionable In a clinical study, FGFR3-TACC3 was identified as an acquired resistance mutation in a patient with non-small cell lung cancer harboring EGFR E746_A750del, whose disease progressed after initial response to Gilotrif (afatinib) (PMID: 29883838). 29883838
FGFR2 fusion FGFR3 - TACC3 adrenal carcinoma sensitive Erdafitinib Phase I Actionable In a Phase I trial, Erdafitinib (JNJ-42756493) treatment resulted tumor shrinkage and no disease progression for 10 months in an adrenal carcinoma patient harboring FGFR3 - TACC3 and FGFR2 - CCDC6 fusions (PMID: 26324363). 26324363
FGFR3 R248C Advanced Solid Tumor sensitive Pazopanib Preclinical - Cell culture Actionable In a preclinical study, Votrient (pazopanib) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR3 R248C Advanced Solid Tumor sensitive R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-independent proliferation induced by FGFR3 R248C in cultured cells (PMID: 19381019). 19381019
FGFR3 R248C Advanced Solid Tumor sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR3 R248C Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR3 amp urinary system cancer sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). 27401245
FGFR3 amp Advanced Solid Tumor predicted - sensitive BGJ398 Phase I Actionable In a Phase I trial, BGJ398 demonstrated safety and preliminary efficacy in patients with select solid tumors harboring FGFR alterations (Cancer Res October 1, 2014 74:CT326). detail...
FGFR3 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...
FGFR3 amp Advanced Solid Tumor predicted - sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of several tumor cell lines with FGFR alterations in culture (Cancer Res April 15, 2011 71:3560). detail...
FGFR3 amp non-small cell lung carcinoma sensitive PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 28.2% tumor growth inhibition in patient-derived xenograft models of FGFR3-amplified non-small cell lung cancer (PMID: 28978721). 28978721
FGFR3 amp urinary system cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). 27401245
ROS1 fusion ERBB2 amp FGFR3 amp RET amp non-small cell lung carcinoma predicted - resistant Crizotinib Clinical Study Actionable In a clinical study, a non-small cell lung carcinoma patient harboring a ROS1 fusion treated with Xalkori (crizotinib) responded, but eventually progressed, and was subsequently found to harbor presumed resistance alterations, including amplification of ERBB2 (HER2), FGFR3, and RET (PMID: 29636358). 29636358
FGFR3 mut FGFR3 over exp urinary bladder cancer sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 33% (1/3) of non-muscle invasive bladder cancer patients harboring both FGFR3 mutations and FGFR3 over expression (J Clin Oncol 34, 2016 (suppl; abstr 4526)). detail...
FGFR3 mutant bladder urothelial carcinoma sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in 33% (1/3) of patients with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 mutations (PMID: 27932416). 27932416
FGFR3 mutant urinary bladder cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 mutation in culture (PMID: 27550940). 27550940
FGFR3 mutant Advanced Solid Tumor sensitive BGJ398 Preclinical Actionable In a preclinical study, tumor cell lines with FGFR3 mutations demonstrated sensitivity to BGJ398 in culture (PMID: 23002168). 23002168
FGFR3 mutant transitional cell carcinoma sensitive BGJ398 Phase I Actionable In a Phase I trial, BGJ398 treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517)). detail...
FGFR3 mutant transitional cell carcinoma sensitive BGJ398 Clinical Study Actionable In a clinical study, BGJ398 treatment led to 25.4% (17/67) confirmed responses and a disease control rate of 64% (43/67), which included complete responses, partial responses, and stable disease, and resulted in a median progression-free survival of 3.75 months and a median overall survival of 7.75 months (PMID: 29848605). 29848605
FGFR3 mutant transitional cell carcinoma predicted - sensitive B-701 + Docetaxel Phase Ib/II Actionable In a Phase I/II trial, B-701 in combination with Taxotere (docetaxel) demonstrated safety and preliminary efficacy, resulted in enhanced activity in patients with locally advanced or metastatic urothelial carcinoma harboring FGFR3 mutations or fusions comparing to wild-type patients (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 4534-4534; NCT02401542). detail...
FGFR3 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...
FGFR3 mutant bladder urothelial carcinoma sensitive BGJ398 Phase I Actionable In a Phase I trial, patients with bladder urothelial carcinoma harboring an FGFR3 mutation demonstrated a disease control rate of 75% (6/8) when treated with BGJ398, including 3 patients with a partial response and 3 with stable disease (PMID: 27870574; NCT01004224). 27870574
FGFR3 mutant urinary system cancer sensitive Erdafitinib Phase I Actionable In a Phase I trial, Erdafitinib (JNJ-42756493) treatment resulted in 25% tumor shrinkage at week 8 in an urothelial cancer patient harboring FGFR3 mutations (PMID: 26324363). 26324363
FGFR3 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...
FGFR3 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...
FGFR3 D764H head and neck squamous cell carcinoma no benefit BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D764H in culture, however, cells expressing FGFR3 D764H did not demonstrate increased sensitivity to BGJ398 compared to cells expressing wild-type FGFR3 (PMID: 27053219). 27053219
FGFR3 Y375C urinary bladder cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer resistant Nintedanib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3 Y375C were resistant to growth inhibition by Ofev (Nintedanib) in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
FGFR3 Y375C Advanced Solid Tumor sensitive R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-dependent proliferation of cells expressing FGFR3 Y375C in culture (PMID: 19381019). 19381019
FGFR3 Y375C urinary bladder cancer resistant Cediranib Preclinical Actionable In a preclinical study, bladder cancer cells harboring an FGFR3 Y375C mutation were resistant to growth inhibition by Cediranib (AZD-2171) in culture (PMID: 22238366). 22238366
FGFR3 D788N head and neck squamous cell carcinoma no benefit BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D788N in culture, however, cells expressing FGFR3 D788N did not demonstrate increased sensitivity to BGJ398 compared to cells expressing wild-type FGFR3 (PMID: 27053219). 27053219
FGFR3 Y373C myeloid neoplasm no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3 Y373C myeloid neoplasm sensitive FF-284 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 Y373C in culture (PMID: 25169980). 25169980
FGFR3 Y373C multiple myeloma sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, a multiple myeloma cell line harboring FGFR3 Y373C (PMID: 19901323) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 19901323 27535969
FGFR3 Y373C myeloid neoplasm no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR3 Y373C myeloid neoplasm no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3 Y373C FGFR3 over exp multiple myeloma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited Fgfr3 signaling and decreased proliferation and survival of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). 22869148
FGFR3 Y373C FGFR3 over exp multiple myeloma sensitive AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). 22869148
AKT1 E17K FGFR3 Y373C urinary bladder cancer sensitive AZD5363 + AZD4547 Preclinical Actionable In a preclinical study, the combined therapy of AZD5363 and AZD4547 resulted in tumor regression in urinary bladder cancer xenograft models simultaneously harboring the mutations, AKT1 E17K and FGFR3 Y373C (PMID: 26351323). 26351323
FGFR3 dec exp KRAS mut lung cancer no benefit Trametinib Preclinical Actionable In a preclinical study, knocking down of Fgfr3 through shRNA did not sensitize KRAS mutant lung cancer cells to Mekinist (trametinib) induced growth inhibition in culture (PMID: 27338794). 27338794
FGFR3 wild-type FGFR3 dec exp HRAS G12V transitional cell carcinoma decreased response AZ8010 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZ8010 in culture (PMID: 22869148). 22869148
FGFR3 wild-type FGFR3 dec exp HRAS G12V transitional cell carcinoma resistant AZD4547 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZD4547 in culture (PMID: 22869148). 22869148
FGFR3 wild-type FGFR3 dec exp HRAS G12V transitional cell carcinoma resistant PD173074 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to PD173074 in culture (PMID: 22869148). 22869148
FGFR3 S249C FGFR3 over exp transitional cell carcinoma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited growth of urothelial carcinoma (UC) cells expressing high levels of FGFR3 S249C, but had reduced efficacy against UC cells with low levels of FGFR3 S249C expression (PMID: 22869148). 22869148
FGFR3 S249C urinary bladder cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). 22238366
FGFR3 S249C urinary bladder cancer sensitive Ponatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of bladder cancer cells harboring FGFR3 S249C in culture and in cell line xenograft models (PMID: 22238366). 22238366
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR3 S249C renal pelvis transitional cell carcinoma predicted - sensitive Pazopanib Clinical Study Actionable In a case study, a patient with urothelial carcinoma of the renal pelvis harboring FGFR3 S249C demonstrated a partial response lasting 9 months following treatment with Votrient (pazopanib) (PMID: 27271022). 27271022
FGFR3 S249C urinary bladder cancer sensitive FF-284 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of bladder cancer cells harboring FGFR3 S249C in culture and inhibited tumor growth in FGFR3 S249C-positive bladder cancer cell line xenograft models (PMID: 25169980). 25169980
FGFR3 S249C Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR3 S249C urinary system cancer sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture (PMID: 27401245). 27401245
FGFR3 S249C urinary bladder cancer sensitive ASP5878 Preclinical - Cell line xenograft Actionable In a preclinical study, ASP5878 treatment inhibited proliferation of a bladder cancer cell line harboring FGFR3 S249C in culture, and resulted in tumor regression in xenograft models (Mol Cancer Ther December 2015 14; A170). detail...
FGFR3 S249C urinary bladder cancer resistant Nintedanib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3 S249C were resistant to Ofev (Nintedanib) induced inhibition of cell proliferation in culture (PMID: 22238366). 22238366
FGFR3 S249C Advanced Solid Tumor sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR3 S249C Advanced Solid Tumor sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3 S249C urinary bladder cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of bladder cancer cells harboring FGFR3 S249C in culture (PMID: 22238366). 22238366
FGFR3 S249C bladder carcinoma sensitive R3Mab Preclinical - Cell line xenograft Actionable In a preclinical study, R3Mab decreased dimer formation and constitutive activation of FGFR3 S249C, and inhibited growth of bladder cancer cell lines harboring FGFR3 S249C in culture and in xenograft models (PMID: 19381019). 19381019
FGFR3 S249C Advanced Solid Tumor sensitive R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited proliferation of transformed cells expressing FGFR3 S249C in culture (PMID: 19381019). 19381019
FGFR3 S249C urinary system cancer sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture and in xenograft models (PMID: 27401245). 27401245
FGFR3 S249C urinary bladder cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). 22238366
FGFR3 S249C bladder urothelial carcinoma sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in a patient with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 S249C (PMID: 27932416). 27932416
FGFR3 F386L myeloid neoplasm sensitive FF-284 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 F386L in culture (PMID: 25169980). 25169980
FGFR3 K652E urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3 K652E in culture (PMID: 27627808). 27627808
FGFR3 K652E Advanced Solid Tumor sensitive R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-dependent cell proliferation in cells expressing FGFR3 K652E in culture (PMID: 19381019). 19381019
FGFR3 L608V FGFR3 V555M transitional cell carcinoma resistant BGJ398 Clinical Study Actionable In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with BGJ398 and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) and FGFR3 L608V (also corresponds to L496V) (PMID: 29848605). 29848605
FGFR3 V555M Advanced Solid Tumor decreased response FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M demonstrated reduced sensitivity to FIIN-2 in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor resistant BGJ398 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to BGJ398 in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to AZD4547 in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor sensitive LY2874455 Preclinical - Cell culture Actionable In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 V555M transitional cell carcinoma resistant BGJ398 Clinical Study Actionable In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with BGJ398 and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) (PMID: 29848605). 29848605
FGFR3 V555M Advanced Solid Tumor decreased response FF-284 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). 28034880
FGFR3 fusion transitional cell carcinoma sensitive BGJ398 Phase I Actionable In a Phase I trial, BGJ398 treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517)). detail...
FGFR3 fusion urinary bladder cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 fusion in culture (PMID: 27550940). 27550940
FGFR3 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...
FGFR3 fusion transitional cell carcinoma predicted - sensitive B-701 + Docetaxel Phase Ib/II Actionable In a Phase I/II trial, B-701 in combination with Taxotere (docetaxel) demonstrated safety and preliminary efficacy, resulted in enhanced activity in patients with locally advanced or metastatic urothelial carcinoma harboring FGFR3 mutations or fusions comparing to wild-type patients (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 4534-4534; NCT02401542). detail...
FGFR3 fusion Advanced Solid Tumor predicted - sensitive TAS-120 Preclinical - Cell line xenograft Actionable In a preclinical study, TAS-120 demonstrated growth inhibition and reduced FGFR phosphorylation in human cancer cell lines and xenograft models harboring FGFR mutations (Mol Cancer Ther 2013;12(11 Suppl):A270). detail...
FGFR3 V555L Advanced Solid Tumor decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555L demonstrated reduced sensitivity to BGJ398 in culture (PMID: 28034880). 28034880
FGFR3 V555L transitional cell carcinoma resistant BGJ398 Clinical Study Actionable In a clinical study, two patients with metastatic urothelial carcinoma progressed while being treated with BGJ398 and subsequent cell-free DNA testing revealed FGFR3 V555L (also corresponds to V443M) (PMID: 29848605). 29848605
FGFR3 G372C Advanced Solid Tumor sensitive R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-dependent proliferation in cells expressing FGFR3 G372C (PMID: 19381019). 19381019
FGFR3 K650E FGFR3 over exp HRAS K117E myeloid neoplasm sensitive AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited Fgfr3 signaling and decreased proliferation of myeloma cells with HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). 22869148
FGFR3 K650E FGFR3 over exp HRAS K117E multiple myeloma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS H117E and over expression of FGFR3 K650E in culture (PMID: 22869148). 22869148
FGFR3 K650E Advanced Solid Tumor decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR3 K650E Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinicl study, Erdafitinib (JNJ-42756493) inhibited proliferation of transformed cells over expressing FGFR3 K560E in culture (PMID: 26992226). 26992226
FGFR3 K650E Advanced Solid Tumor sensitive LY2874455 Preclinical - Cell culture Actionable In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to BGJ398 in culture (PMID: 28034880). 28034880
FGFR3 K650E myeloid neoplasm no benefit SSR128129E Preclinical Actionable In a preclinical study, SSR128129E did not inhibit proliferation of myeloma cells expressing FGFR3 K650E in culture (PMID: 23597562). 23597562
FGFR3 K650E Advanced Solid Tumor sensitive FF-284 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E myeloid neoplasm sensitive SU5402 Preclinical - Cell culture Actionable In a preclinical study, SU5402 inhibited proliferation of myeloma cells expressing FGFR3 K650E in culture (PMID: 23597562). 23597562
FGFR3 K650E Advanced Solid Tumor sensitive FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, FIIN-2 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor sensitive PD98059 Preclinical Actionable In a preclinical study, PD98059 inhibited FGFR3 K650E-induced transformation of cells in culture (PMID: 14534538). 14534538
FGFR3 K650E myeloid neoplasm sensitive FF-284 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 K650E in culture (PMID: 25169980). 25169980
FGFR3 K650E Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor decreased response FF-284 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive LY2874455 Preclinical - Cell culture Actionable In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to BGJ398 in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to AZD4547 in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, FIIN-2 inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 act mut urinary bladder cancer predicted - sensitive S-49076 Preclinical Actionable In a preclinical study, S-49076 inhibited autophosphorylation of FGFR3 and downstream signaling in bladder cancer cells over expressing constitutively active FGFR3 in culture (PMID: 23804704). 23804704
FGFR3 act mut Advanced Solid Tumor decreased response Cediranib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR3 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
FGFR3 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 FGFR3 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). detail...
FGFR3 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 FGFR3 in culture (PMID: 22238366). 22238366
FGFR3 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
FGFR3 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 FGFR3 in culture (PMID: 22238366). 22238366
FGFR3 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 FGFR3 in culture (PMID: 22238366). 22238366
FGFR3 act mut Advanced Solid Tumor decreased response Nintedanib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR3 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR3-BAIAP2L1 urinary bladder cancer sensitive Cediranib Preclinical - Cell culture Actionable In a preclinical study, Cediranib (AZD-2171) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3-BAIAP2L1 urinary bladder cancer sensitive ASP5878 Preclinical - Cell culture Actionable In a preclinical study, ASP5878 treatment inhibited proliferation of a bladder cancer cell line harboring an FGFR3-BAIAP2L1 fusion in culture (Mol Cancer Ther December 2015 14; A170). detail...
FGFR3-BAIAP2L1 urinary bladder cancer sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3-BAIAP2L1 urinary bladder cancer sensitive FF-284 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 decreased phosphorylation of ERK and FRS and inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture, and inhibited tumor growth in bladder cancer cell line xenograft models with FGFR3-BAIAP2L1 (PMID: 25589496) 25589496
FGFR3-BAIAP2L1 urinary bladder cancer sensitive FF-284 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 inhibited proliferation of a bladder cancer cell line harboring an FGFR3-BAIAP2L1 fusion in culture (PMID: 25169980). 25169980
FGFR3-BAIAP2L1 urinary bladder cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3-BAIAP2L1 urinary bladder cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3-BAIAP2L1 urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3-BAIAP2L1 fusion in culture (PMID: 27627808). 27627808
FGFR3-BAIAP2L1 Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR3-BAIAP2L1 in culture (PMID: 27627808). 27627808
FGFR3-BAIAP2L1 urinary bladder cancer sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 K650M Advanced Solid Tumor sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR3 K650M in culture (PMID: 28978721). 28978721
FGFR3 wild-type urinary bladder cancer resistant Ponatinib Preclinical Actionable In a preclinical study, bladder cancer cells with wild-type FGFR3 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR3 wild-type bladder carcinoma sensitive R3Mab Preclinical - Cell line xenograft Actionable In a preclinical study, R3Mab decreased wild-type FGFR3 activation, thereby inhibited cell proliferation of FGFR3 wild-type human bladder cancer cells in culture and in cell line xenograft models (PMID: 19381019). 19381019
FGFR3 wild-type myeloid neoplasm sensitive SU5402 Preclinical - Cell culture Actionable In a preclinical study, SU5402 inhibited proliferation of myeloma cells expressing wild-type FGFR3 in culture (PMID: 23597562). 23597562
FGFR3 wild-type myeloid neoplasm sensitive SSR128129E Preclinical Actionable In a preclinical study, SSR128129E inhibited proliferation of myeloma cells expressing wild-type FGFR3 in culture (PMID: 23597562). 23597562
FGFR3 rearrange myeloid neoplasm sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of myeloma cells harboring FGFR3 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR3 rearrange myeloid neoplasm sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of myeloma cells harboring FGFR3 rearrangements in culture (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249). detail...
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response AZ8010 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZ8010 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response AZD4547 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZD4547 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response PD173074 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to PD173074 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 over exp glioblastoma multiforme sensitive U0126 Preclinical Actionable In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells over-expressing Fgfr3 in culture (PMID: 23298836). 23298836
FGFR3 over exp urinary bladder cancer sensitive Sorafenib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, the combination of BEZ235 and Nexavar (sorafenib) resulted in improved progression-free survival in an FGFR3-over expressing patient-derived xenograft (PDX) model of bladder cancer with secondary resistance to BGJ398 due to reactivation of downstream signaling, as evidenced by increased activation of Akt and Erk (PMID: 26270481). 26270481
FGFR3 over exp Advanced Solid Tumor sensitive LY2874455 Preclinical Actionable In a preclinical study, LY2874455 induced tumor regression in FGFR3-over expressing bladder and multiple myeloma xenograft models (PMID: 21900693). 21900693
FGFR3 over exp urinary bladder cancer sensitive SU5402 Preclinical Actionable In a preclinical study, SU5402 inhibited growth of bladder cancer cells over expressing wild-type FGFR3 in culture (PMID: 21119661). 21119661
FGFR3 over exp transitional cell carcinoma sensitive AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). 22869148
FGFR3 over exp transitional cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). 22869148
FGFR3 over exp urinary bladder cancer sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 8% (1/13) of non-muscle invasive bladder cancer patients over expressing FGFR3 (J Clin Oncol 34, 2016 (suppl; abstr 4526)). detail...
FGFR3 over exp urinary bladder cancer sensitive BGJ398 Preclinical - Pdx Actionable In a preclinical study, treatment with BGJ398 led to improved progression-free survival in a patient-derived xenograft (PDX) model of bladder cancer with FGFR3 over expression (PMID: 26270481). 26270481
FGFR3 over exp Advanced Solid Tumor sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation in transformed cells overexpressing wild-type FGFR3 in culture (PMID: 28978721). 28978721
FGFR3 over exp head and neck squamous cell carcinoma sensitive Rogaratinib Preclinical Actionable In a preclinical study, Rogaratinib (BAY 1163877) inhibited tumor growth in a head and neck squamous cell carcinoma xenograft model with FGFR3 overexpression (Cancer Res August 1, 2015 75:772). detail...
FGFR3 over exp multiple myeloma sensitive MFGR1877S Phase I Actionable In a Phase I trial, MFGR1877S demonstrated safety and resulted in stable disease in 42% (6/14) of multiple myeloma patients overexpressing FGFR3 (Blood (ASH Annual Meeting Abstracts) 2012 120: Abstract 4029). detail...
FGFR3 positive lung squamous cell 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 long lasting stable disease in a patient with FGFR3-positive lung squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR3 positive stomach cancer 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 in a patient with FGFR3-positive gastric cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR3 positive lung adenocarcinoma 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 in a patient with FGFR3-positive lung adenocarcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR3 positive head and neck squamous cell 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 FGFR3-positive head and neck squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR2 pos FGFR3 pos breast carcinoma sensitive E7090 Preclinical Actionable In a preclinical study, a mouse breast carcinoma cell line xenograft model demonstrated inhibition of tumor growth when treated with E7090, a result of decreased FGFR2 and FGFR3 activity (PMID: 27535969). 27535969
FGFR3 S131L head and neck squamous cell carcinoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, a head and neck squamous cell carcinoma cell line expressing FGFR3 S131L demonstrated decreased sensitivity to BGJ398 compared to cells expressing wild-type FGFR3 in culture (PMID: 27053219). 27053219
FGFR3 N540K Advanced Solid Tumor decreased response FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to FIIN-2 in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor decreased response FF-284 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinicl study, Erdafitinib (JNJ-42756493) inhibited proliferation of transformed cells over expressing FGFR3 K560E in culture (PMID: 26992226). 26992226
FGFR3 N540K Advanced Solid Tumor resistant BGJ398 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K were resistant to BGJ398 in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K were reistant to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR3 N540K Advanced Solid Tumor decreased response LY2874455 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to LY2874455 in culture (PMID: 28034880). 28034880