DGIdb - FGFR2 Gene Record

FGFR2 2263 Druggable GenomeClinically Actionable

Alternate Names:

2263
FIBROBLAST GROWTH FACTOR RECEPTOR 2
FGFR2
BBDS
BEK
BFR-1
CD332
CEK3
CFD1
ECT1
JWS
K-SAM
KGFR
TK14
TK25
176943
3689
ENSG00000066468
OTTHUMG00000019175
FGFR-2
KSAM
CD_antigen=CD332
Keratinocyte growth factor receptor
FGFR2_HUMAN
P21802
22
FIBROBLAST GROWTH FACTOR RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (FGFR-2) (KERATINOCYTE GROWTH FACTOR RECEPTOR 2). [SOURCE:UNIPROT/SWISSPROT;ACC:P21802]
FGFR1-3
PA28128
T58454

Gene Info:

CancerCommons Reported Gene Name	FGFRs
Human Readable Name	DRUGGABLE GENOME
Transmembrane Helix Count	1
Target Main Class	Receptors
Target Subclass	Kinase
Target Subclass	FGFR
Target Class	Receptors
Target Subclass	EC:2.7.10.1
Initial Gene Query	FGFR2
Counted Citations from 1950-2000	944
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Human Readable Name	KINASE
Uniprot Status	Swiss-Prot
Interpro Acc	IPR001245
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Uniprot Evidence	1: Evidence at protein level
Interpro Type	Domain
Gene Biotype	PROTEIN_CODING

(24 More Sources)

Gene Categories: Category Details

CELL SURFACE
KINASE
TYROSINE KINASE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Mazzaferro V et al., 2019, Derazantinib (ARQ 087) in advanced or inoperable FGFR2 gene fusion-positive intrahepatic cholangiocarcinoma., Br J Cancer
Hall TG et al., 2016, Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation., PLoS One
Martignetti et al., 2014, Personalized ovarian cancer disease surveillance and detection of candidate therapeutic drug target in circulating tumor DNA., Neoplasia
Konecny et al., 2013, Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells., Mol. Cancer Ther.
Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
Tanizaki et al., 2015, Identification of Oncogenic and Drug-Sensitizing Mutations in the Extracellular Domain of FGFR2., Cancer Res.
Arai et al., 2014, Fibroblast growth factor receptor 2 tyrosine kinase fusions define a unique molecular subtype of cholangiocarcinoma., Hepatology
Künstlinger et al., 2015, FGFR2 is overexpressed in myxoid liposarcoma and inhibition of FGFR signaling impairs tumor growth in vitro., Oncotarget
Liu et al., 2017, c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors., 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
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.
Javle M et al., 2018, Phase II Study of BGJ398 in Patients With FGFR-Altered Advanced Cholangiocarcinoma., J Clin Oncol
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Guagnano et al., 2012, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor., 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.
Dutt et al., 2008, Drug-sensitive FGFR2 mutations in endometrial carcinoma., Proc. Natl. Acad. Sci. U.S.A.
Byron et al., 2013, The N550K/H mutations in FGFR2 confer differential resistance to PD173074, dovitinib, and ponatinib ATP-competitive inhibitors., Neoplasia
André et al., 2013, Targeting FGFR with dovitinib (TKI258): preclinical and clinical data in breast cancer., Clin. Cancer Res.
Eritja N et al., 2014, Combinatorial therapy using dovitinib and ICI182.780 (fulvestrant) blocks tumoral activity of endometrial cancer cells., Mol Cancer Ther
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.
Perera et al., 2017, Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor., Mol. Cancer Ther.
Loriot Y et al., 2019, Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma., N Engl J Med
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
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
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
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
Harding et al., 2013, Blockade of nonhormonal fibroblast growth factors by FP-1039 inhibits growth of multiple types of cancer., Sci Transl Med
Secrier et al., 2016, Mutational signatures in esophageal adenocarcinoma define etiologically distinct subgroups with therapeutic relevance., Nat. Genet.
Abou-Alfa GK et al., 2020, Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study., Lancet Oncol
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
Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
Koole et al., 2016, FGFR1 Is a Potential Prognostic Biomarker and Therapeutic Target in Head and Neck Squamous Cell Carcinoma., Clin. Cancer Res.
Eichholz et al., 2010, Anti-angiogenesis therapies: their potential in cancer management., Onco Targets Ther
Patrie et al., 1995, Conservation of ligand specificity between the mammalian and amphibian fibroblast growth factor receptors., J. Biol. Chem.
Zhu et al., 2007, Epigenetic silencing through DNA and histone methylation of fibroblast growth factor receptor 2 in neoplastic pituitary cells., Am. J. Pathol.
Beaven et al., 2007, Recombinant human keratinocyte growth factor palifermin reduces oral mucositis and improves patient outcomes after stem cell transplant., Drugs Today
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Radtke et al., 2005, Palifermin (Kepivance) for the treatment of oral mucositis in patients with hematologic malignancies requiring hematopoietic stem cell support., J Oncol Pharm Pract
Cardoso et al., 1997, FGF-1 and FGF-7 induce distinct patterns of growth and differentiation in embryonic lung epithelium., Dev. Dyn.
Huang et al., 2006, Effect of keratinocyte growth factor on cell viability in primary cultured human prostate cancer stromal cells., J. Steroid Biochem. Mol. Biol.
Berman et al., 1999, Similarities and differences between the effects of heparin and glypican-1 on the bioactivity of acidic fibroblast growth factor and the keratinocyte growth factor., J. Biol. Chem.
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.
Kim et al., 2016, Antitumor effects and molecular mechanisms of ponatinib on endometrial cancer cells harboring activating FGFR2 mutations., Cancer Biol. Ther.
Borad et al., 2014, Integrated genomic characterization reveals novel, therapeutically relevant drug targets in FGFR and EGFR pathways in sporadic intrahepatic cholangiocarcinoma., PLoS Genet.
Grünewald S et al., 2019, Rogaratinib: A potent and selective pan-FGFR inhibitor with broad antitumor activity in FGFR-overexpressing preclinical cancer models., Int J Cancer
Goyal L et al., 2019, TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma., Cancer Discov
Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
Yoon et al., 2009, Combination of EGFR and MEK1/2 inhibitor shows synergistic effects by suppressing EGFR/HER3-dependent AKT activation in human gastric cancer cells., Mol. Cancer Ther.
Wang et al., 2016, Recurrent Olfactory Neuroblastoma Treated With Cetuximab and Sunitinib: A Case Report., Medicine (Baltimore)
Liao et al., 2013, Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma., Cancer Res.
Jo et al., 2015, Targeting FGFR Pathway in Human Hepatocellular Carcinoma: Expressing pFGFR and pMET for Antitumor Activity., Mol. Cancer Ther.
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.

PALIFERMIN FGFR2

Interaction Score: 2.42

Interaction Types & Directionality:

agonist (activating)

binder

Interaction Info:

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

Novel drug target Established target

Mechanism of Interaction Fibroblast growth factor receptor 2 agonist

PMIDs:
7499435 17456767 17728847 11752352 16390600 9056643 16854582 10593896

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
FUTIBATINIB FGFR2

Interaction Score: 1.82

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type biliary tract cancer

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
31109923

Sources:
JAX-CKB CIViC
PEMIGATINIB FGFR2

Interaction Score: 1.62

Interaction Types & Directionality:

activator (activating)

inhibitor (inhibitory)

Interaction Info:

Response Type sensitive

Indication/Tumor Type Advanced Solid Tumor

Approval Status Preclinical - Cell culture

PMIDs:
32203698 32315352

Sources:
JAX-CKB CIViC
ERDAFITINIB FGFR2

Interaction Score: 1.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type urinary system cancer

Response Type sensitive

Approval Status Phase I

PMIDs:
26324363 28341788 31340094 28965185

Sources:
JAX-CKB CIViC PharmGKB OncoKB
E-7090 FGFR2

Interaction Score: 1.21

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
18552176 27535969

Sources:
JAX-CKB
DERAZANTINIB FGFR2

Interaction Score: 1.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
30420614 27627808

Sources:
ChemblInteractions CIViC
INFIGRATINIB FGFR2

Interaction Score: 0.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
24563622 23443805 28119489 26048680 24122810 26036639 27401245 28034880 27870574 29182496

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial OncoKB
ROGARATINIB FGFR2

Interaction Score: 0.97

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type breast cancer

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
30807645

Sources:
JAX-CKB ChemblInteractions CIViC
TRABECTEDIN FGFR2

Interaction Score: 0.81

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dovitinib + Trabectedin

Indication/Tumor Type myxoid liposarcoma

Response Type sensitive

PMIDs:
26036639

Sources:
JAX-CKB
PONATINIB FGFR2

Interaction Score: 0.77

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
26619011 23002168 22238366 18552176 23908597 23468082 26048680 26574622 24550739

Sources:
TALC MyCancerGenome JAX-CKB DoCM CIViC
FP-1039 FGFR2

Interaction Score: 0.73

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
23536011

Sources:
TdgClinicalTrial JAX-CKB
LY-2874455 FGFR2

Interaction Score: 0.61

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
TRAFERMIN FGFR2

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name trafermin, fibro/

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
BRIVANIB FGFR2

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type decreased response

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

PMIDs:
22238366 20124951

Sources:
JAX-CKB ChemblInteractions PharmGKB
PHA-665752 FGFR2

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type hepatocellular carcinoma

Response Type no benefit

Approval Status Preclinical - Cell culture

PMIDs:
26351320

Sources:
JAX-CKB
NINTEDANIB FGFR2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BIBF-1120,Vargatef

Novel drug target Established target

Notes

PMIDs:
18559524 22238366 31016670

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB
DEBIO-1347 FGFR2

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
OncoKB
RO-4987655 FGFR2

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal adenocarcinoma

Response Type decreased response

Approval Status Preclinical - Cell culture

PMIDs:
26438159

Sources:
JAX-CKB
AZD-4547 FGFR2

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DOVITINIB FGFR2

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name dovitinib, TKI-258, CHIR-258

Variant Effect gain-of-function

PMIDs:
26619011 23002168 22238366 18552176 23908597 23443805 26036639 23658459 24448819

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB DoCM CIViC
LUCITANIB FGFR2

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AEE-788 FGFR2

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
LENVATINIB FGFR2

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
17943726

Sources:
TALC
FULVESTRANT FGFR2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24448819

Sources:
CIViC
BRIVANIB ALANINATE FGFR2

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CP-459632 FGFR2

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XL-228 FGFR2

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome
RABEPRAZOLE SODIUM FGFR2

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome TTD
NINTEDANIB ESYLATE FGFR2

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ORANTINIB FGFR2

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
MUPARFOSTAT FGFR2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Muparfostat

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PAZOPANIB FGFR2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status case report

Pathway activation

Variant Effect gain-of-function

PMIDs:
24550739 23786770

Sources:
DoCM CIViC
XL-999 FGFR2

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SELUMETINIB FGFR2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type decreased response

Indication/Tumor Type endometrial carcinoma

Approval Status Preclinical - Cell culture

PMIDs:
26438159 19755509

Sources:
JAX-CKB
THALIDOMIDE FGFR2

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Thalomid

Novel drug target Established target

PMIDs:
20616958

Sources:
TdgClinicalTrial TEND
ENMD-2076 FGFR2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ENMD-2076

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial
MK-2461 FGFR2

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
BUPARLISIB FGFR2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BKM120

Indication/Tumor Type endometrial cancer

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB
LAPATINIB FGFR2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
27595477

Sources:
JAX-CKB
REGORAFENIB FGFR2

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial
MASITINIB FGFR2

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
PICTILISIB FGFR2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB
TG100-801 FGFR2

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ALPELISIB FGFR2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB
SUNITINIB FGFR2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
27149458

Sources:
JAX-CKB
TRAMETINIB FGFR2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type no benefit

PMIDs:
27338794

Sources:
JAX-CKB
CETUXIMAB FGFR2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
27149458

Sources:
JAX-CKB
CEDIRANIB FGFR2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type decreased response

Indication/Tumor Type Advanced Solid Tumor

Indication/Tumor Type endometrial cancer

PMIDs:
22238366

Sources:
JAX-CKB
ENMD-981693 FGFR2

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GEFITINIB FGFR2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
26936917

Sources:
JAX-CKB
RG-1530 FGFR2

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Ensembl: ENSG00000066468
- Version: 101_38
Alternate Names:

FGFR2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:

RussLampel: ENSG00000066468

Version: 26-July-2011

Alternate Names:

FGFR2 Display Id

ENSG00000066468 Ensembl Gene Id

FIBROBLAST GROWTH FACTOR RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (FGFR-2) (KERATINOCYTE GROWTH FACTOR RECEPTOR 2). [SOURCE:UNIPROT/SWISSPROT;ACC:P21802] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

HopkinsGroom: P21802
- Version: 11-September-2012
Alternate Names:

ENSG00000066468 Ensembl Gene Id

FGFR2 Uniprot Gene Name

P21802 Uniprot Accession

Gene Info:

Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

Human Readable Name KINASE

Uniprot Status Swiss-Prot

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
TEND: P21802
- Version: 01-August-2011
Alternate Names:

ENSG00000066468 Ensembl Gene Id

P21802 Uniprot Accession

2263 Entrez Gene Id

Gene Info:

Transmembrane Helix Count 1

Target Main Class Receptors

Target Subclass Kinase

Publications:
CancerCommons: FGFR2
- Version: 25-July-2013
Alternate Names:

2263 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name FGFRs

Publications:
TdgClinicalTrial: P21802
- Version: January-2014
Alternate Names:

FGFR2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:
BaderLabGenes: FGFR2
- Version: February-2014
Alternate Names:

2263 Entrez Gene ID

Gene Info:

Initial Gene Query FGFR2

Counted Citations from 1950-2000 944

Gene Categories:

KINASE

Publications:

JAX-CKB: FGFR2

Version: 27-September-2017

Alternate Names:

2263 CKB Entrez Id

FGFR2 CKB Gene Synonym

BBDS CKB Gene Synonym

Gene Info:

Publications:

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

Konecny et al., 2013, Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells., Mol. Cancer Ther.

Arai et al., 2014, Fibroblast growth factor receptor 2 tyrosine kinase fusions define a unique molecular subtype of cholangiocarcinoma., Hepatology

PharmGKB: FGFR2
- Version: 18-August-2020
Alternate Names:

PA28128 PharmGKB ID

Gene Info:

Publications:

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

CIViC: FGFR2

Version: 14-September-2020

Alternate Names:

2263 Entrez Gene ID

22 CIViC Gene ID

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Liao et al., 2013, Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma., Cancer Res.

Borad et al., 2014, Integrated genomic characterization reveals novel, therapeutically relevant drug targets in FGFR and EGFR pathways in sporadic intrahepatic cholangiocarcinoma., PLoS Genet.

Eritja N et al., 2014, Combinatorial therapy using dovitinib and ICI182.780 (fulvestrant) blocks tumoral activity of endometrial cancer cells., Mol Cancer Ther

DoCM: FGFR2

Version: 27-September-2017

Alternate Names:

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.

Greulich et al., 2011, Targeting mutant fibroblast growth factor receptors in cancer., Trends Mol Med

Dutt et al., 2008, Drug-sensitive FGFR2 mutations in endometrial carcinoma., Proc. Natl. Acad. Sci. U.S.A.

TALC: FGFR2
- Version: 12-May-2016
Alternate Names:

FGFR2 Gene Symbol

Gene Info:

Publications:
MyCancerGenome: FGFR2
- Version: 20-Jun-2017
Alternate Names:

2263 Entrez Gene Id

FGFR2 MyCancerGenome Gene Symbol

FGFR1-3 MyCancerGenome Reported Gene Name

Gene Info:

Publications:
HingoraniCasas: ENSG00000066468
- Version: 31-May-2017
Alternate Names:

ENSG00000066468 Gene Symbol

FGFR2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TALC: FGFR-2
- Version: 12-May-2016
Alternate Names:

FGFR-2 Gene Symbol

Gene Info:

Publications:
ChemblInteractions: BEK
- Version: chembl_23
Alternate Names:

KGFR GENE_SYMBOL

KSAM GENE_SYMBOL

FGFR2 GENE_SYMBOL

Gene Info:

Publications:
OncoKB: FGFR2
- Version: 23-July-2020
Alternate Names:

2263 OncoKB Entrez Id

BBDS OncoKB Gene Synonym

BFR-1 OncoKB Gene Synonym

Gene Info:

Publications:
GO: FGFR2
- Version: 01-February-2022
Alternate Names:

BEK GO Gene Synonym

KGFR GO Gene Synonym

KSAM GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, TYROSINE KINASE

Publications:
Tempus: FGFR2
- Version: 11-November-2018
Alternate Names:

FGFR2 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: FGFR2
- Version: 27-Jun-2013
Alternate Names:

2263 Gene ID

BBDS dGene Synonym

BEK dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
TTD: Fibroblast growth factor receptor 2
- Version: 2020.06.01
Alternate Names:

FGFR2 TTD Gene Abbreviation

T58454 TTD Target ID

Gene Info:

Publications:
Pharos: FGFR2
- Version: 01-February-2022
Alternate Names:

Fibroblast growth factor receptor 2 Gene Name

P21802 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
MskImpact: FGFR2
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
ClearityFoundationClinicalTrial: FGFR2
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: FGFR2
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
FoundationOneGenes: FGFR2
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: FGFR2
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
Oncomine: FGFR2
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Trial Name	rHu-KGF, keratinocyte growth factor (KGF),Kepivance
Novel drug target	Established target
Mechanism of Interaction	Fibroblast growth factor receptor 2 agonist

Indication/Tumor Type	biliary tract cancer
Response Type	predicted – sensitive
Approval Status	Phase I

Response Type	sensitive
Indication/Tumor Type	Advanced Solid Tumor
Approval Status	Preclinical - Cell culture

Indication/Tumor Type	urinary system cancer
Response Type	sensitive
Approval Status	Phase I

Indication/Tumor Type	breast cancer
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

Mechanism of Interaction	Fibroblast growth factor receptor inhibitor
Direct Interaction	yes

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

combination therapy	Dovitinib + Trabectedin
Indication/Tumor Type	myxoid liposarcoma
Response Type	sensitive

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

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

agonist (activating)
binder

activator (activating)
inhibitor (inhibitory)

Trial Name	trafermin, fibro/
Novel drug target	Established target

Response Type	decreased response
Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive

Indication/Tumor Type	hepatocellular carcinoma
Response Type	no benefit
Approval Status	Preclinical - Cell culture

Trial Name	BIBF-1120,Vargatef
Novel drug target	Established target
Notes

Indication/Tumor Type	colorectal adenocarcinoma
Response Type	decreased response
Approval Status	Preclinical - Cell culture

Mechanism of Interaction	Fibroblast growth factor receptor 2 inhibitor
Direct Interaction	yes

Clinical Status	case report
Pathway	activation
Variant Effect	gain-of-function

combination therapy	BGJ398 + BKM120
Indication/Tumor Type	endometrial cancer
Response Type	sensitive

combination therapy	Cetuximab + Sunitinib
Indication/Tumor Type	olfactory neuroblastoma
Response Type	sensitive

FGFR2	Display Id
ENSG00000066468	Ensembl Gene Id
FIBROBLAST GROWTH FACTOR RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (FGFR-2) (KERATINOCYTE GROWTH FACTOR RECEPTOR 2). [SOURCE:UNIPROT/SWISSPROT;ACC:P21802]	Description

FGFR2 Gene Record

FGFR2 2263 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating) binder

Interaction Info: Trial Name rHu-KGF, keratinocyte growth factor (KGF),Kepivance Novel drug target Established target Mechanism of Interaction Fibroblast growth factor receptor 2 agonist

PMIDs: 7499435 17456767 17728847 11752352 16390600 9056643 16854582 10593896

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type biliary tract cancer Response Type predicted – sensitive Approval Status Phase I

PMIDs: 31109923

Sources: JAX-CKB CIViC

Interaction Types & Directionality: activator (activating) inhibitor (inhibitory)

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

PMIDs: 32203698 32315352

Sources: JAX-CKB CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type urinary system cancer Response Type sensitive Approval Status Phase I

PMIDs: 26324363 28341788 31340094 28965185

Sources: JAX-CKB CIViC PharmGKB OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast cancer Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 18552176 27535969

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 30420614 27627808

Sources: ChemblInteractions CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 24563622 23443805 28119489 26048680 24122810 26036639 27401245 28034880 27870574 29182496

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type breast cancer Response Type predicted – sensitive Approval Status Phase I

PMIDs: 30807645

Sources: JAX-CKB ChemblInteractions CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Dovitinib + Trabectedin Indication/Tumor Type myxoid liposarcoma Response Type sensitive

PMIDs: 26036639

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 26619011 23002168 22238366 18552176 23908597 23468082 26048680 26574622 24550739

Sources: TALC MyCancerGenome JAX-CKB DoCM CIViC

Interaction Types & Directionality: n/a

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

PMIDs: 23536011

Sources: TdgClinicalTrial JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Response Type decreased response Indication/Tumor Type Advanced Solid Tumor Response Type sensitive

PMIDs: 22238366 20124951

Sources: JAX-CKB ChemblInteractions PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type hepatocellular carcinoma Response Type no benefit Approval Status Preclinical - Cell culture

PMIDs: 26351320

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name BIBF-1120,Vargatef Novel drug target Established target Notes

PMIDs: 18559524 22238366 31016670

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal adenocarcinoma Response Type decreased response Approval Status Preclinical - Cell culture

PMIDs: 26438159

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality:

agonist (activating)

binder

Interaction Info:

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

Novel drug target Established target

Mechanism of Interaction Fibroblast growth factor receptor 2 agonist

PMIDs:
7499435 17456767 17728847 11752352 16390600 9056643 16854582 10593896

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type biliary tract cancer

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
31109923

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

activator (activating)

inhibitor (inhibitory)

Interaction Info:

Response Type sensitive

Indication/Tumor Type Advanced Solid Tumor

Approval Status Preclinical - Cell culture

PMIDs:
32203698 32315352

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type urinary system cancer

Response Type sensitive

Approval Status Phase I

PMIDs:
26324363 28341788 31340094 28965185

Sources:
JAX-CKB CIViC PharmGKB OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
18552176 27535969

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
30420614 27627808

Sources:
ChemblInteractions CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction yes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

PMIDs:
24563622 23443805 28119489 26048680 24122810 26036639 27401245 28034880 27870574 29182496

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type breast cancer

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
30807645

Sources:
JAX-CKB ChemblInteractions CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dovitinib + Trabectedin

Indication/Tumor Type myxoid liposarcoma

Response Type sensitive

PMIDs:
26036639

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
26619011 23002168 22238366 18552176 23908597 23468082 26048680 26574622 24550739

Sources:
TALC MyCancerGenome JAX-CKB DoCM CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
23536011

Sources:
TdgClinicalTrial JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name trafermin, fibro/

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type decreased response

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

PMIDs:
22238366 20124951

Sources:
JAX-CKB ChemblInteractions PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type hepatocellular carcinoma

Response Type no benefit

Approval Status Preclinical - Cell culture

PMIDs:
26351320

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name BIBF-1120,Vargatef

Novel drug target Established target

Notes

PMIDs:
18559524 22238366 31016670

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal adenocarcinoma

Response Type decreased response

Approval Status Preclinical - Cell culture

PMIDs:
26438159

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name dovitinib, TKI-258, CHIR-258

Variant Effect gain-of-function

PMIDs:
26619011 23002168 22238366 18552176 23908597 23443805 26036639 23658459 24448819

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB DoCM CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

2263	Entrez Gene Id
FGFR2	MyCancerGenome Gene Symbol
FGFR1-3	MyCancerGenome Reported Gene Name

2263	OncoKB Entrez Id
BBDS	OncoKB Gene Synonym
BFR-1	OncoKB Gene Synonym

Fibroblast growth factor receptor 2	Gene Name
P21802	UniProt ID