DGIdb - INFIGRATINIB Drug Record

INFIGRATINIB chembl:CHEMBL1852688 Antineoplastic

Alternate Names:

BGJ398
NVP-BGJ398
BGJ-398
INFIGRATINIB
MVP-BGJ398
chembl:CHEMBL1852688
chemidplus:872511-34-7
drugbank:11886
pubchem.compound:53235510

Drug Info:

Pharmaceutical Developer	Novartis
Source Reported Drug Name(s)	BGJ398
Drug Class	Pan-FGFR Inhibitor
Notes	dual PI3K/mTOR inhibitor
Drug Class	Kinase Inhibitors

(6 More Sources)

Publications:

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
Singh et al., 2012, Transforming fusions of FGFR and TACC genes in human glioblastoma., Science
Göke et al., 2015, FGFR1 Expression Levels Predict BGJ398 Sensitivity of FGFR1-Dependent Head and Neck Squamous Cell Cancers., Clin. Cancer Res.
Chudasama et al., 2017, Targeting Fibroblast Growth Factor Receptor 1 for Treatment of Soft-Tissue Sarcoma., Clin. Cancer Res.
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
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
Guagnano et al., 2012, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor., Cancer Discov
Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.
Capelletti et al., 2014, Identification of recurrent FGFR3-TACC3 fusion oncogenes from lung adenocarcinoma., Clin. Cancer Res.
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
Chandrani et al., 2017, Drug-sensitive FGFR3 mutations in lung adenocarcinoma., Ann. Oncol.
Li et al., 2015, FGFR-Mediated Reactivation of MAPK Signaling Attenuates Antitumor Effects of Imatinib in Gastrointestinal Stromal Tumors., Cancer Discov

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
INFIGRATINIB FGFR3

Interaction Score: 0.86

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

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

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial OncoKB
INFIGRATINIB FGFR1

Interaction Score: 0.43

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Notes

Indication/Tumor Type uterus leiomyosarcoma

PMIDs:
22837387 27870574 26015511 27535980

Sources:
CancerCommons MyCancerGenomeClinicalTrial OncoKB TTD TALC JAX-CKB MyCancerGenome ChemblInteractions CIViC
INFIGRATINIB FGFR4

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions CancerCommons
INFIGRATINIB PIK3C3

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3C2A

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3C2B

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3C2G

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3R6

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3R4

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB KIT

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + Imatinib

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

PMIDs:
25673643

Sources:
JAX-CKB
INFIGRATINIB PIK3R3

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3R5

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3R1

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3R2

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3CD

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB PIK3CA

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy BGJ398 + BKM120

combination therapy BGJ398 + BYL719

Evidence Type Actionable

PMIDs:
28119489

Sources:
MyCancerGenome JAX-CKB
INFIGRATINIB PTEN

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BYL719

Indication/Tumor Type endometrial cancer

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB
INFIGRATINIB PIK3CB

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB KRAS

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
27338794

Sources:
JAX-CKB
INFIGRATINIB PIK3CG

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
INFIGRATINIB MTOR

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome

CancerCommons: BGJ398
- Version: 25-July-2013
Alternate Names:

BGJ398 PubChem Drug Name

53235510 PubChem Drug ID

BGJ398 Drug Trade Name

Drug Info:

Drug Class Pan-FGFR Inhibitor

Source Reported Drug Name(s) BGJ398

Pharmaceutical Developer Novartis

Publications:
MyCancerGenome: BGJ398
- Version: 20-Jun-2017
Alternate Names:

BGJ398 Development Name

NVP-BGJ398 Development Name

BGT226 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes dual PI3K/mTOR inhibitor

Publications:

JAX-CKB: BGJ398

Version: 27-September-2017

Alternate Names:

Drug 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

CIViC: INFIGRATINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Chandrani et al., 2017, Drug-sensitive FGFR3 mutations in lung adenocarcinoma., Ann. Oncol.

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.

TTD: BGJ398
- Version: 2020.06.01
Alternate Names:

D03LWG TTD Drug ID

Drug Info:

Publications:
TALC: BGJ398
- Version: 12-May-2016
Alternate Names:

BGJ398 Primary Drug Name

BGJ398 Drug Synonym

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1852688
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: BGJ398
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
OncoKB: BGJ398
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1852688
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

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

Reported Cancer Type	Melanoma
Notes
Indication/Tumor Type	uterus leiomyosarcoma

combination therapy	BGJ398 + Imatinib
Indication/Tumor Type	gastrointestinal stromal tumor
Response Type	sensitive

combination therapy	BGJ398 + BKM120
combination therapy	BGJ398 + BYL719
Evidence Type	Actionable

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

BGJ398	PubChem Drug Name
53235510	PubChem Drug ID
BGJ398	Drug Trade Name

BGJ398	Development Name
NVP-BGJ398	Development Name
BGT226	Development Name

INFIGRATINIB Drug Record

INFIGRATINIB chembl:CHEMBL1852688 Antineoplastic

Alternate Names:

Drug Info:

Publications:

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

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Melanoma Notes Indication/Tumor Type uterus leiomyosarcoma

PMIDs: 22837387 27870574 26015511 27535980

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Melanoma Mechanism of Interaction Fibroblast growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions CancerCommons

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BGJ398 + Imatinib Indication/Tumor Type gastrointestinal stromal tumor Response Type sensitive

PMIDs: 25673643

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: combination therapy BGJ398 + BKM120 combination therapy BGJ398 + BYL719 Evidence Type Actionable

PMIDs: 28119489

Sources: MyCancerGenome JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BGJ398 + BYL719 Indication/Tumor Type endometrial cancer Response Type sensitive

PMIDs: 28119489

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

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:

Notes

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Notes

Indication/Tumor Type uterus leiomyosarcoma

PMIDs:
22837387 27870574 26015511 27535980

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Mechanism of Interaction Fibroblast growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions CancerCommons

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + Imatinib

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

PMIDs:
25673643

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy BGJ398 + BKM120

combination therapy BGJ398 + BYL719

Evidence Type Actionable

PMIDs:
28119489

Sources:
MyCancerGenome JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BGJ398 + BYL719

Indication/Tumor Type endometrial cancer

Response Type sensitive

PMIDs:
28119489

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
27338794

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Alternate Names:

BGJ398 PubChem Drug Name

53235510 PubChem Drug ID

BGJ398 Drug Trade Name

Drug Info:

Drug Class Pan-FGFR Inhibitor

Source Reported Drug Name(s) BGJ398

Pharmaceutical Developer Novartis

Alternate Names:

BGJ398 Development Name

NVP-BGJ398 Development Name

BGT226 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes dual PI3K/mTOR inhibitor

Alternate Names:

D03LWG TTD Drug ID

Alternate Names:

BGJ398 Primary Drug Name

BGJ398 Drug Synonym