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FGFR3 Gene Record

  • Summary
  • Interactions
  • Claims
  • FGFR3 2261 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    2261
    FIBROBLAST GROWTH FACTOR RECEPTOR 3
    FGFR3
    ACH
    CD333
    CEK2
    HSFGFR3EX
    JTK4
    134934
    3690
    ENSG00000068078
    OTTHUMG00000121148
    CD_antigen=CD333
    FGFR-3
    BE0002133
    P22607
    FGFR3_HUMAN
    FIBROBLAST GROWTH FACTOR RECEPTOR 3 PRECURSOR (EC 2.7.1.112) (FGFR-3). [SOURCE:UNIPROT/SWISSPROT;ACC:P22607]
    FGFR1-3
    1810
    23
    NP_000133
    NM_000142
    PA28129
    T91331

    Gene Info:

    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR001245
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Human Readable Name KINASE
    Human Readable Name DRUGGABLE GENOME
    CancerCommons Reported Gene Name FGFRs
    CancerCommons Reported Gene Name FGFR3 and others (VEGFR)
    Target Class Receptors
    Target Subclass EC:2.7.10.1
    Target Main Class Receptors
    Target Subclass Kinase
    Target Subclass FGFR
    Transmembrane Helix Count 1
    GuideToPharmacology Gene Category Name Type V RTKs: FGF (fibroblast growth factor) receptor family
    GuideToPharmacology Gene Category ID 323
    Gene Biotype PROTEIN_CODING
    (27 More Sources)

    Gene Categories: Category Details

    CELL SURFACE
    KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE

    Publications:

    Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.
    Williams et al., 2013, Oncogenic FGFR3 gene fusions in bladder cancer., Hum. Mol. Genet.
    Hänze et al., 2013, Epithelial mesenchymal transition status is associated with anti-cancer responses towards receptor tyrosine-kinase inhibition by dovitinib in human bladder cancer cells., BMC Cancer
    Hahn et al., 2017, A Phase II Trial of Dovitinib in BCG-Unresponsive Urothelial Carcinoma with FGFR3 Mutations or Overexpression: Hoosier Cancer Research Network Trial HCRN 12-157., Clin. Cancer Res.
    Goyal et al., 2017, Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma., Cancer Discov
    Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. Cancer
    Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.
    Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
    Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
    Yamanaka et al., 2000, Isolation and serum-free culture of epithelial cells derived from epithelial rests of Malassez in human periodontal ligament., In Vitro Cell. Dev. Biol. Anim.
    Cancilla et al., 2001, Fibroblast growth factor receptors and their ligands in the adult rat kidney., Kidney Int.
    Launay et al., 1994, Comparative analysis of the tissue distribution of three fibroblast growth factor receptor mRNAs during amphibian morphogenesis., Differentiation
    Beer et al., 2000, Fibroblast growth factor (FGF) receptor 1-IIIb is a naturally occurring functional receptor for FGFs that is preferentially expressed in the skin and the brain., J. Biol. Chem.
    Mummery et al., 1993, Fibroblast growth factor-mediated growth regulation and receptor expression in embryonal carcinoma and embryonic stem cells and human germ cell tumours., Biochem. Biophys. Res. Commun.
    Liu PCC et al., 2020, INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models., PLoS One
    Wang et al., 2017, A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma., Eur. Urol.
    Tabernero et al., 2015, Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors., J. Clin. Oncol.
    Di Stefano et al., 2015, Detection, Characterization, and Inhibition of FGFR-TACC Fusions in IDH Wild-type Glioma., Clin. Cancer Res.
    Patani et al., 2016, Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use., Oncotarget
    Loriot Y et al., 2019, Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma., N Engl J Med
    Perera et al., 2017, Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor., Mol. Cancer Ther.
    Nishina T et al., 2018, Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors., Invest New Drugs
    Davies et al., 2015, Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors., Mol. Cancer Ther.
    Capelletti et al., 2014, Identification of recurrent FGFR3-TACC3 fusion oncogenes from lung adenocarcinoma., Clin. Cancer Res.
    Gozgit et al., 2013, Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models., Cancer Chemother. Pharmacol.
    Yang Z et al., 2018, Somatic FGFR3 Mutations Distinguish a Subgroup of Muscle-Invasive Bladder Cancers with Response to Neoadjuvant Chemotherapy., EBioMedicine
    Chandrani et al., 2017, Drug-sensitive FGFR3 mutations in lung adenocarcinoma., Ann. Oncol.
    von Mässenhausen et al., 2016, Evaluation of FGFR3 as a Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Target Oncol
    Singh et al., 2012, Transforming fusions of FGFR and TACC genes in human glioblastoma., Science
    Liu et al., 2017, c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors., Clin. Cancer Res.
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
    Guagnano et al., 2012, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor., Cancer Discov
    Pal SK et al., 2018, Efficacy of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Inhibitor, in Patients with Previously Treated Advanced Urothelial Carcinoma with <i>FGFR3</i> Alterations., Cancer Discov
    Nogova et al., 2017, Evaluation of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Kinase Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in Fibroblast Growth Factor Receptors: Results of a Global Phase I, Dose-Escalation and Dose-Expansion Study., J. Clin. Oncol.
    Zhao et al., 2011, A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models., Mol. Cancer Ther.
    Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
    Watanabe Miyano et al., 2016, E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models., Mol. Cancer Ther.
    St-Germain et al., 2009, Multiple myeloma phosphotyrosine proteomic profile associated with FGFR3 expression, ligand activation, and drug inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
    Xie X et al., 2019, FGFR<sup>3S249C</sup> mutation promotes chemoresistance by activating Akt signaling in bladder cancer cells., Exp Ther Med
    Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
    Sethakorn N et al., 2016, Spectrum of genomic alterations in FGFR3: current appraisal of the potential role of FGFR3 in advanced urothelial carcinoma., BJU Int
    Wu et al., 2013, Identification of targetable FGFR gene fusions in diverse cancers., Cancer Discov
    Deeks, 2012, Pazopanib: in advanced soft tissue sarcoma., Drugs
    Matsui et al., 2008, E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition., Int. J. Cancer
    Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.
    Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol
    Qing et al., 2009, Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice., J. Clin. Invest.
    Otsuka et al., 2011, Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy., Anticancer Res.
    Chell et al., 2013, Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance., Oncogene
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
  • VOFATAMAB   FGFR3

    Interaction Score: 1.78

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type multiple myeloma
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    None found


    Sources:
    JAX-CKB TTD

  • E-7090   FGFR3

    Interaction Score: 1.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type breast carcinoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23175443 27535969 19901323


    Sources:
    JAX-CKB

  • PALIFERMIN   FGFR3

    Interaction Score: 1.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name rHu-KGF, keratinocyte growth factor (KGF),Kepivance
    Novel drug target Established target

    PMIDs:
    11149756 11422746 7890137 10821861 7680555


    Sources:
    TEND TdgClinicalTrial DrugBank

  • LY-2874455   FGFR3

    Interaction Score: 1.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23175443 28034880 21900693


    Sources:
    JAX-CKB GuideToPharmacology ChemblInteractions

  • PEMIGATINIB   FGFR3

    Interaction Score: 0.89

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell line xenograft
    Response Type sensitive

    PMIDs:
    32315352


    Sources:
    JAX-CKB DrugBank GuideToPharmacology

  • ERDAFITINIB   FGFR3

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    26324363 25609060 26992226 31340094 28341788 28965185


    Sources:
    OncoKB PharmGKB JAX-CKB CIViC DrugBank GuideToPharmacology

  • INFIGRATINIB   FGFR3

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    27998968 27053219 25294908 22837387 27401245 26270481 23002168 28034880 29848605 27870574 25589496


    Sources:
    CancerCommons MyCancerGenomeClinicalTrial OncoKB JAX-CKB CIViC TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • ROGARATINIB   FGFR3

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    JAX-CKB GuideToPharmacology ChemblInteractions

  • FUTIBATINIB   FGFR3

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    JAX-CKB GuideToPharmacology

  • DERAZANTINIB   FGFR3

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • BRIVANIB   FGFR3

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor
    Direct Interaction yes
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    22238366 20124951


    Sources:
    PharmGKB JAX-CKB ChemblInteractions

  • NINTEDANIB   FGFR3

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type resistant
    Indication/Tumor Type urinary bladder cancer
    Evidence Type Actionable

    PMIDs:
    22238366 18559524 31016670


    Sources:
    ClearityFoundationClinicalTrial JAX-CKB TdgClinicalTrial DrugBank TALC MyCancerGenome GuideToPharmacology

  • DEBIO-1347   FGFR3

    Interaction Score: 0.36

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    OncoKB GuideToPharmacology

  • PONATINIB   FGFR3

    Interaction Score: 0.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type resistant
    Approval Status Preclinical - Cell line xenograft
    Response Type predicted – sensitive

    PMIDs:
    22238366 25294908 28034880 23468082


    Sources:
    JAX-CKB CIViC DrugBank TALC MyCancerGenome

  • RO-4987655   FGFR3

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type bladder transitional cell papilloma
    Response Type no benefit
    Approval Status Preclinical - Cell culture

    PMIDs:
    26438159


    Sources:
    JAX-CKB

  • BRIVANIB ALANINATE   FGFR3

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • TRAFERMIN   FGFR3

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name trafermin, fibro/
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • AZD-4547   FGFR3

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TRAPIDIL   FGFR3

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CAPIVASERTIB   FGFR3

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    26351323


    Sources:
    JAX-CKB

  • MASITINIB   FGFR3

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial MyCancerGenome ChemblInteractions

  • FP-1039   FGFR3

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name FP-1039
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • DOVITINIB   FGFR3

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Indication/Tumor Type bladder urothelial carcinoma
    Approval Status Preclinical - Cell culture

    PMIDs:
    22238366 23175443 24325461 27932416 28034880 21119661 25589496


    Sources:
    ClearityFoundationClinicalTrial CancerCommons DTC JAX-CKB TdgClinicalTrial CIViC TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • ENMD-2076   FGFR3

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor
    Direct Interaction yes
    Notes

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial TALC MyCancerGenome ChemblInteractions

  • AEE-788   FGFR3

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LENVATINIB   FGFR3

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    17943726


    Sources:
    DrugBank

  • MK-2461   FGFR3

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • PAZOPANIB   FGFR3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type urinary bladder cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    27271022 23558953 23072642


    Sources:
    JAX-CKB CIViC DrugBank

  • CP-459632   FGFR3

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • XL-228   FGFR3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome

  • RABEPRAZOLE SODIUM   FGFR3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD MyCancerGenome

  • NINTEDANIB ESYLATE   FGFR3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BORTEZOMIB   FGFR3

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Clinical Status preclinical
    Pathway activation
    Variant Effect gain-of-function

    PMIDs:
    26619011 19331127 20542753 19381019 21273588 22869148 25157968


    Sources:
    DoCM CGI

  • ORANTINIB   FGFR3

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PAZOPANIB HYDROCHLORIDE   FGFR3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • XL-999   FGFR3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CEDIRANIB   FGFR3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type resistant
    Approval Status Preclinical - Cell culture
    Response Type sensitive

    PMIDs:
    22238366 25589496


    Sources:
    DTC JAX-CKB

  • BUPARLISIB   FGFR3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell line xenograft
    Response Type sensitive

    PMIDs:
    28108151


    Sources:
    JAX-CKB

  • SELUMETINIB   FGFR3

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type urinary bladder cancer
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    26438159


    Sources:
    JAX-CKB

  • TRAMETINIB   FGFR3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung cancer
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    27338794


    Sources:
    JAX-CKB

  • DACTOLISIB   FGFR3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sorafenib + BEZ235
    Indication/Tumor Type urinary bladder cancer
    Response Type sensitive

    PMIDs:
    26270481


    Sources:
    JAX-CKB

  • CHEMBL578061   FGFR3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MLN-8054   FGFR3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ENMD-981693   FGFR3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Fibroblast growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SORAFENIB   FGFR3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sorafenib + BEZ235
    Indication/Tumor Type urinary bladder cancer
    Response Type sensitive

    PMIDs:
    26270481


    Sources:
    DTC JAX-CKB

  • ALPELISIB   FGFR3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BGJ398 + BYL719
    Indication/Tumor Type transitional cell carcinoma
    Response Type predicted – sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • HESPERADIN   FGFR3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19035792


    Sources:
    DTC

  • GEMCITABINE   FGFR3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29941343


    Sources:
    CIViC

  • ALISERTIB   FGFR3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • OSI-632   FGFR3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CISPLATIN   FGFR3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31316618 29941343


    Sources:
    CIViC

  • ENTRECTINIB   FGFR3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TOZASERTIB   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LINIFANIB   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • R-406   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RG-1530   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SP-600125   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CYC-116   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAE-684   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PF-00562271   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • FOSTAMATINIB   FGFR3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26516587


    Sources:
    DrugBank

  • Ensembl: ENSG00000068078

    • Version: 101_38

    Alternate Names:
    FGFR3 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TEND: P22607

    • Version: 01-August-2011

    Alternate Names:
    ENSG00000068078 Ensembl Gene Id
    FGFR3_HUMAN Uniprot Id
    2261 Entrez Gene Id

    Gene Info:
    Target Main Class Receptors
    Target Subclass Kinase
    Target Subclass FGFR

    Publications:

  • TdgClinicalTrial: P22607

    • Version: January-2014

    Alternate Names:
    FGFR3 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass EC:2.7.10.1

    Publications:

  • RussLampel: ENSG00000068078

    • Version: 26-July-2011

    Alternate Names:
    FGFR3 Display Id
    ENSG00000068078 Ensembl Gene Id
    FIBROBLAST GROWTH FACTOR RECEPTOR 3 PRECURSOR (EC 2.7.1.112) (FGFR-3). [SOURCE:UNIPROT/SWISSPROT;ACC:P22607] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • HopkinsGroom: P22607

    • Version: 11-September-2012

    Alternate Names:
    FGFR3 Uniprot Gene Name
    FGFR3_HUMAN Uniprot Id
    P22607 Uniprot Accession

    Gene Info:
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR001245
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • CancerCommons: FGFR3

    • Version: 25-July-2013

    Alternate Names:
    2261 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name FGFRs
    CancerCommons Reported Gene Name FGFR3 and others (VEGFR)

    Publications:

  • GuideToPharmacology: 2261

    • Version: 29-September-2020

    Alternate Names:
    3690 HUGO Gene ID
    3690 HUGO Gene Symbol
    fibroblast growth factor receptor 3 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Type V RTKs: FGF (fibroblast growth factor) receptor family
    GuideToPharmacology Gene Category ID 323

    Publications:

  • JAX-CKB: FGFR3

    • Version: 27-September-2017

    Alternate Names:
    2261 CKB Entrez Id
    FGFR3 CKB Gene Synonym
    ACH CKB Gene Synonym

    Gene Info:

    Publications:
    Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.
    Wang et al., 2017, A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma., Eur. Urol.
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE

  • PharmGKB: FGFR3

    • Version: 18-August-2020

    Alternate Names:
    PA28129 PharmGKB ID

    Gene Info:

    Publications:
    Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics

  • CIViC: FGFR3

    • Version: 14-September-2020

    Alternate Names:
    2261 Entrez Gene ID
    23 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE, CLINICALLY ACTIONABLE

    Publications:
    Chandrani et al., 2017, Drug-sensitive FGFR3 mutations in lung adenocarcinoma., Ann. Oncol.
    Wu et al., 2013, Identification of targetable FGFR gene fusions in diverse cancers., Cancer Discov
    Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. Cancer

  • DrugBank: BE0002133

    • Version: 5.1.7

    Alternate Names:
    FGFR3 DrugBank Gene Name
    P22607 UniProt Accession
    2261 Entrez Gene Id

    Gene Info:

    Publications:
    Gozgit et al., 2013, Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models., Cancer Chemother. Pharmacol.
    Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
    Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet

  • CGI: FGFR3

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.
    Otsuka et al., 2011, Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy., Anticancer Res.

  • DoCM: FGFR3

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.
    Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol

  • DTC: FGFR3

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.

  • HingoraniCasas: ENSG00000068078

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000068078 Gene Symbol
    FGFR3 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TALC: FGFR-3

    • Version: 12-May-2016

    Alternate Names:
    FGFR-3 Gene Symbol

    Gene Info:

    Publications:

  • ChemblInteractions: JTK4

    • Version: chembl_23

    Alternate Names:
    JTK4 GENE_SYMBOL
    FGFR3 GENE_SYMBOL
    Fibroblast growth factor receptor 3 UNIPROT

    Gene Info:

    Publications:

  • MyCancerGenome: FGFR3

    • Version: 20-Jun-2017

    Alternate Names:
    2261 Entrez Gene Id
    FGFR3 MyCancerGenome Gene Symbol
    FGFR1-3 MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • TALC: FGFR3

    • Version: 12-May-2016

    Alternate Names:
    FGFR3 Gene Symbol

    Gene Info:

    Publications:

  • OncoKB: FGFR3

    • Version: 23-July-2020

    Alternate Names:
    2261 OncoKB Entrez Id
    JTK4 OncoKB Gene Synonym
    HSFGFR3EX OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Pharos: FGFR3

    • Version: 03-September-2020

    Alternate Names:
    Fibroblast growth factor receptor 3 Gene Name
    P22607 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • GO: FGFR3

    • Version: 05-September-2020

    Alternate Names:
    JTK4 GO Gene Synonym

    Gene Info:

    Gene Categories:
    CELL SURFACE, TYROSINE KINASE

    Publications:

  • Tempus: FGFR3

    • Version: 11-November-2018

    Alternate Names:
    FGFR3 Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: FGFR3

    • Version: 27-Jun-2013

    Alternate Names:
    2261 Gene ID
    ACH dGene Synonym
    CD333 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, TYROSINE KINASE

    Publications:

  • TTD: Fibroblast growth factor receptor 3

    • Version: 2020.06.01

    Alternate Names:
    FGFR3 TTD Gene Abbreviation
    T91331 TTD Target ID

    Gene Info:

    Publications:

  • ClearityFoundationClinicalTrial: FGFR3

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: FGFR3

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: FGFR3

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FoundationOneGenes: FGFR3

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: FGFR3

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • Oncomine: FGFR3

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21