DGIdb - FGFR3 Gene Record

FGFR3 2261 Druggable GenomeClinically Actionable

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
TTDC00131
23
NP_000133
NM_000142
PA28129
T91331

Gene Info:

Human Readable Name	TYROSINE KINASE
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
Source Reported Gene Name	FGFR3
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
GuideToPharmacology Gene Type	catalytic_receptor
Gene Biotype	PROTEIN_CODING

(27 More Sources)

Gene Categories: Category Details

CELL SURFACE
KINASE
TYROSINE KINASE
PHOSPHOLIPASE
DRUGGABLE GENOME
LIPID KINASE
CLINICALLY ACTIONABLE

Publications:

Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. 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.
Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.
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
Williams et al., 2013, Oncogenic FGFR3 gene fusions in bladder cancer., Hum. Mol. Genet.
Goyal et al., 2017, Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma., Cancer Discov
Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.
Liao et al., 2013, Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma., Cancer Res.
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
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.
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
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.
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.
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.
Perera et al., 2017, Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor., Mol. Cancer Ther.
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
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.
Loriot Y et al., 2019, Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma., N Engl J Med
Karkera JD et al., 2017, Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib., Mol Cancer Ther
Bahleda R et al., 2019, Multicenter Phase I Study of Erdafitinib (JNJ-42756493), Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients with Advanced or Refractory Solid Tumors., Clin Cancer Res
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
Schuler M et al., 2019, Rogaratinib in patients with advanced cancers selected by FGFR mRNA expression: a phase 1 dose-escalation and dose-expansion study., Lancet Oncol
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
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.
Liu et al., 2017, c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors., Clin. Cancer Res.
Guagnano et al., 2012, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor., Cancer Discov
Singh et al., 2012, Transforming fusions of FGFR and TACC genes in human glioblastoma., Science
von Mässenhausen et al., 2016, Evaluation of FGFR3 as a Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Target Oncol
Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
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.
Hall TG et al., 2016, Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation., PLoS One
Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
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.
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.
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
Wu et al., 2013, Identification of targetable FGFR gene fusions in diverse cancers., Cancer Discov
Deeks, 2012, Pazopanib: in advanced soft tissue sarcoma., Drugs
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
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.
Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol
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.
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
Qing et al., 2009, Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice., J. Clin. Invest.
McCoach CE et al., 2018, Resistance Mechanisms to Targeted Therapies in <i>ROS1</i><sup>+</sup> and <i>ALK</i><sup>+</sup> Non-small Cell Lung Cancer., Clin Cancer Res
Wang L et al., 2019, Fibroblast Growth Factor Receptor 3 Alterations and Response to PD-1/PD-L1 Blockade in Patients with Metastatic Urothelial Cancer., Eur Urol
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

DOVITINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Indication/Tumor Type bladder urothelial carcinoma

Approval Status Preclinical - Cell culture

Publications:

Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. 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.

Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.

NINTEDANIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Indication/Tumor Type urinary bladder cancer

Evidence Type 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.

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

PEMIGATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

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

ERDAFITINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Perera et al., 2017, Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor., Mol. Cancer Ther.

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

ROGARATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Schuler M et al., 2019, Rogaratinib in patients with advanced cancers selected by FGFR mRNA expression: a phase 1 dose-escalation and dose-expansion study., Lancet Oncol

PONATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

Publications:

Capelletti et al., 2014, Identification of recurrent FGFR3-TACC3 fusion oncogenes from lung adenocarcinoma., 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

Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.

INFIGRATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Publications:

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 FGFR3 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.

Liu et al., 2017, c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors., Clin. Cancer Res.

LY-2874455 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

Publications:

Williams et al., 2013, Oncogenic FGFR3 gene fusions in bladder cancer., Hum. Mol. Genet.

Goyal et al., 2017, Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma., Cancer Discov

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.

DERAZANTINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Hall TG et al., 2016, Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation., PLoS One

BRIVANIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Indication/Tumor Type Advanced Solid Tumor

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.

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

PAZOPANIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Approval Status Preclinical

Publications:

Wu et al., 2013, Identification of targetable FGFR gene fusions in diverse cancers., Cancer Discov

Deeks, 2012, Pazopanib: in advanced soft tissue sarcoma., Drugs

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

ENMD-981693 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Publications:
ENMD-2076 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Direct Interaction yes

Notes

Publications:
NINTEDANIB ESYLATE FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Publications:
XL-999 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Publications:
AZD-4547 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Publications:
ORANTINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Publications:
BRIVANIB ALANINATE FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Publications:
MASITINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Publications:
PAZOPANIB HYDROCHLORIDE FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Direct Interaction yes

Publications:
DEBIO-1347 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
MK-2461 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
FUTIBATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
CP-459632 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Publications:
HESPERADIN FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

LENVATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

FOSTAMATINIB FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
RABEPRAZOLE SODIUM FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
XL-228 FGFR3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Publications:

BUPARLISIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

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.

CAPIVASERTIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

Publications:

Davies et al., 2015, Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors., Mol. Cancer Ther.

CEDIRANIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.

Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.

SORAFENIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sorafenib + BEZ235

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Publications:

Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE

E-7090 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast carcinoma

Response Type sensitive

Approval Status Preclinical

Publications:

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.

Williams et al., 2013, Oncogenic FGFR3 gene fusions in bladder cancer., Hum. Mol. Genet.

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.

TRAMETINIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung cancer

Response Type no benefit

Approval Status Preclinical

Publications:

Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
DACTOLISIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sorafenib + BEZ235

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Publications:

Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
RO-4987655 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type bladder transitional cell papilloma

Response Type no benefit

Approval Status Preclinical - Cell culture

Publications:

Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
SELUMETINIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type no benefit

Approval Status Preclinical

Publications:

Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
CRIZOTINIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Case Reports/Case Series

Response Type predicted - resistant

Publications:

McCoach CE et al., 2018, Resistance Mechanisms to Targeted Therapies in ROS1+ and ALK+ Non-small Cell Lung Cancer., Clin Cancer Res
NIVOLUMAB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type no benefit

Publications:

Wang L et al., 2019, Fibroblast Growth Factor Receptor 3 Alterations and Response to PD-1/PD-L1 Blockade in Patients with Metastatic Urothelial Cancer., Eur Urol
ATEZOLIZUMAB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type no benefit

Publications:

Wang L et al., 2019, Fibroblast Growth Factor Receptor 3 Alterations and Response to PD-1/PD-L1 Blockade in Patients with Metastatic Urothelial Cancer., Eur Urol
TRAFERMIN FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name trafermin, fibro/

Novel drug target Established target

Publications:
FP-1039 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name FP-1039

Novel drug target Established target

Publications:
ALPELISIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BYL719

Indication/Tumor Type transitional cell carcinoma

Response Type predicted – sensitive

Publications:
VOFATAMAB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type multiple myeloma

Response Type sensitive

Approval Status Phase I

Publications:
DOCETAXEL FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase Ib/II

Response Type predicted - sensitive

Publications:

PALIFERMIN FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name rHu-KGF, keratinocyte growth factor (KGF),Kepivance

Novel drug target Established target

Publications:

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.

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

GEMCITABINE FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Yang Z et al., 2018, Somatic FGFR3 Mutations Distinguish a Subgroup of Muscle-Invasive Bladder Cancers with Response to Neoadjuvant Chemotherapy., EBioMedicine
CISPLATIN FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Yang Z et al., 2018, Somatic FGFR3 Mutations Distinguish a Subgroup of Muscle-Invasive Bladder Cancers with Response to Neoadjuvant Chemotherapy., EBioMedicine

BORTEZOMIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

Publications:

Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol

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.

ENTRECTINIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TRAPIDIL FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
R-406 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL578061 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RG-1530 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CYC-116 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL606964 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ILORASERTIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TAE-684 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
OSI-632 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SP-600125 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MLN-8054 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LINIFANIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CENISERTIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
AEE-788 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PF-00562271 FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DASATINIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ALISERTIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TOZASERTIB FGFR3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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:

GuideToPharmacologyGenes: 1810

Version: 4-March-2015

Alternate Names:

fibroblast growth factor receptor 3 HUGO Gene Name

3690 HUGO Gene ID

FGFR3 Gene Symbol

Gene Info:

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

GuideToPharmacology Gene Category ID 323

GuideToPharmacology Gene Type catalytic_receptor

Gene Categories:

KINASE, TYROSINE KINASE

Publications:

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

DrugBank: BE0002133

Version: 5.1.7

Alternate Names:

FGFR3 DrugBank Gene Name

P22607 UniProt Accession

2261 Entrez Gene Id

Gene Info:

Publications:

Cancilla et al., 2001, Fibroblast growth factor receptors and their ligands in the adult rat kidney., Kidney Int.

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.

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.

JAX-CKB: FGFR3

Version: 15-September-2020

Alternate Names:

2261 CKB Entrez Id

FGFR3 CKB Gene Synonym

ACH CKB Gene Synonym

Gene Info:

Publications:

Chae YK et al., 2020, Phase II Study of AZD4547 in Patients With Tumors Harboring Aberrations in the FGFR Pathway: Results From the NCI-MATCH Trial (EAY131) Subprotocol W., J Clin Oncol

Liu et al., 2017, c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors., Clin. Cancer 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

DoCM: FGFR3

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Qing et al., 2009, Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice., J. Clin. Invest.

MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn

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

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.

CGI: FGFR3

Version: 14-September-2020

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.

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:
GuideToPharmacologyInteractions: ENSG00000068078
- Version: 20-July-2020
Alternate Names:

fibroblast growth factor receptor 3 GuideToPharmacology Name

P22607 UniProtKB ID

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:
TTD: Fibroblast growth factor receptor 3
- Version: 2020.06.01
Alternate Names:

FGFR3 TTD Gene Abbreviation

T91331 TTD Target ID

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:

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:
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:

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

Response Type	resistant
Indication/Tumor Type	urinary bladder cancer
Evidence Type	Actionable

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

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

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

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

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

Indication/Tumor Type	breast carcinoma
Response Type	sensitive
Approval Status	Preclinical

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

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

Trial Name	trafermin, fibro/
Novel drug target	Established target

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

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

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

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

ENSG00000068078	Ensembl Gene Id
FGFR3_HUMAN	Uniprot Id
2261	Entrez Gene Id

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

FGFR3	Uniprot Gene Name
FGFR3_HUMAN	Uniprot Id
P22607	Uniprot Accession

fibroblast growth factor receptor 3	HUGO Gene Name
3690	HUGO Gene ID
FGFR3	Gene Symbol

FGFR3	DrugBank Gene Name
P22607	UniProt Accession
2261	Entrez Gene Id

FGFR3 Gene Record

FGFR3 2261 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: 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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Schuler M et al., 2019, Rogaratinib in patients with advanced cancers selected by FGFR mRNA expression: a phase 1 dose-escalation and dose-expansion study., Lancet Oncol

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Hall TG et al., 2016, Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation., PLoS One

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: 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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Indication/Tumor Type bladder urothelial carcinoma

Approval Status Preclinical - Cell culture

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Indication/Tumor Type urinary bladder cancer

Evidence Type Actionable

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Schuler M et al., 2019, Rogaratinib in patients with advanced cancers selected by FGFR mRNA expression: a phase 1 dose-escalation and dose-expansion study., Lancet Oncol

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Hall TG et al., 2016, Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation., PLoS One

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Indication/Tumor Type Advanced Solid Tumor

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.

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Approval Status Preclinical

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Direct Interaction yes

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 3 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

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.

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

Publications:

Davies et al., 2015, Tumors with AKT1E17K Mutations Are Rational Targets for Single Agent or Combination Therapy with AKT Inhibitors., Mol. Cancer Ther.

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type resistant

Approval Status Preclinical - Cell culture

Response Type sensitive

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sorafenib + BEZ235

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Publications:

Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast carcinoma

Response Type sensitive

Approval Status Preclinical

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung cancer

Response Type no benefit

Approval Status Preclinical

Publications:

Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sorafenib + BEZ235

Indication/Tumor Type urinary bladder cancer

Response Type sensitive

Publications:

Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE

JTK4	GENE_SYMBOL
FGFR3	GENE_SYMBOL
Fibroblast growth factor receptor 3	UNIPROT

fibroblast growth factor receptor 3	GuideToPharmacology Name
P22607	UniProtKB ID

2261	OncoKB Entrez Id
JTK4	OncoKB Gene Synonym
HSFGFR3EX	OncoKB Gene Synonym

Fibroblast growth factor receptor 3	Gene Name
P22607	UniProt ID