DGIdb - DOVITINIB Drug Record

DOVITINIB chembl:CHEMBL522892 Antineoplastic

Alternate Names:

CHIR-258
GFKI-258
NVP-TKI258
TKI-258
DOVITINIB
CHIR 258
4-AMINO-5-FLUORO-3-[5-(4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL]QUINOLIN-2(1H)-ONE
TKI258
TKI 258
chemidplus:405169-16-6
chembl:CHEMBL522892
drugbank:05928

Drug Info:

Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
Pharmaceutical Developer	Novartis
Source Reported Drug Name(s)	Dovitinib/TKI258
Drug Class	FGFR Inhibitor
Drug Type	small molecule
Drug Groups	investigational
Drug Categories	bcrp/abcg2 inducers
Drug Categories	bcrp/abcg2 inhibitors
Drug Categories	cytochrome p-450 cyp1a2 inducers
Drug Categories	cytochrome p-450 cyp1a2 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2c19 inhibitors
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (weak)
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	oatp1b1/slco1b1 inhibitors
Drug Categories	oatp1b3 inhibitors
Drug Categories	p-glycoprotein inhibitors
Drug Categories	quinolines
Drug Categories	tyrosine kinase inhibitors
Drug Categories	ugt1a3 inhibitors
Drug Categories	ugt2b7 inhibitors

(11 More Sources)

Publications:

Gozgit et al., 2012, Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models., Mol. Cancer Ther.
Williams et al., 2013, Oncogenic FGFR3 gene fusions in bladder cancer., Hum. Mol. Genet.
Hänze et al., 2013, Epithelial mesenchymal transition status is associated with anti-cancer responses towards receptor tyrosine-kinase inhibition by dovitinib in human bladder cancer cells., BMC Cancer
Hahn et al., 2017, A Phase II Trial of Dovitinib in BCG-Unresponsive Urothelial Carcinoma with FGFR3 Mutations or Overexpression: Hoosier Cancer Research Network Trial HCRN 12-157., Clin. Cancer Res.
Goyal et al., 2017, Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma., Cancer Discov
Lamont et al., 2011, Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo., Br. J. Cancer
Nakanishi et al., 2015, Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1., Mol. Cancer Ther.
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
André et al., 2013, Targeting FGFR with dovitinib (TKI258): preclinical and clinical data in breast cancer., 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.
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
Guagnano et al., 2012, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor., Cancer Discov
Künstlinger et al., 2015, FGFR2 is overexpressed in myxoid liposarcoma and inhibition of FGFR signaling impairs tumor growth in vitro., Oncotarget
Eritja N et al., 2014, Combinatorial therapy using dovitinib and ICI182.780 (fulvestrant) blocks tumoral activity of endometrial cancer cells., Mol Cancer Ther
Lim et al., 2016, Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 study., Cancer
Chase et al., 2007, Activity of TKI258 against primary cells and cell lines with FGFR1 fusion genes associated with the 8p11 myeloproliferative syndrome., Blood
Li SQ et al., 2013, Targeting wild-type and mutationally activated FGFR4 in rhabdomyosarcoma with the inhibitor ponatinib (AP24534)., PLoS One
Yan D et al., 2017, Inhibition of colony stimulating factor-1 receptor abrogates microenvironment-mediated therapeutic resistance in gliomas., Oncogene
Quintela-Fandino et al., 2014, Selective activity over a constitutively active RET-variant of the oral multikinase inhibitor dovitinib: results of the CNIO-BR002 phase I-trial., Mol Oncol
Weiss J et al., 2014, Interaction potential of the multitargeted receptor tyrosine kinase inhibitor dovitinib with drug transporters and drug metabolising enzymes assessed in vitro., Pharmaceutics

DOVITINIB FGF3

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family FGFR inhibitor

Alteration FGF3:amp

PMIDs:
None found

Sources:
CGI
DOVITINIB FGFR2

Interaction Score: 0.19

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:
22238366 26619011 23658459 23443805 18552176 23908597 23002168 26036639 24448819

Sources:
ClearityFoundationClinicalTrial DoCM JAX-CKB TdgClinicalTrial CIViC TALC MyCancerGenome CGI
DOVITINIB FGFR3

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Indication/Tumor Type bladder urothelial carcinoma

Approval Status Preclinical - Cell culture

PMIDs:
22238366 23175443 24325461 27932416 28034880 21119661 25589496

Sources:
ClearityFoundationClinicalTrial CancerCommons DTC JAX-CKB TdgClinicalTrial CIViC TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions
DOVITINIB FGF4

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family FGFR inhibitor

Alteration FGF4:amp

PMIDs:
None found

Sources:
CGI
DOVITINIB CAMKK2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CFLAR

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
DOVITINIB MARK4

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP3K10

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB RPS6KA5

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PIM2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB FGFR1

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
22238366 23658459 27315356 17698633

Sources:
ClearityFoundationClinicalTrial DTC JAX-CKB TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology
DOVITINIB TSSK1B

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB FGFR4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24124571

Sources:
ClearityFoundationClinicalTrial CIViC
DOVITINIB SIK2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PHKG2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB NEK4

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB SRPK1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CSF1R

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
28759044

Sources:
ClearityFoundationClinicalTrial DTC CIViC GuideToPharmacology
DOVITINIB IKBKE

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB SGK2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PRKX

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB FLT1

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Reported Cancer Type Prostate

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial CancerCommons DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions
DOVITINIB PDGFRB

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dovitinib, TKI-258, CHIR-258

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions
DOVITINIB NEK2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CAMK2D

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP3K20

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PDGFRA

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC GuideToPharmacology ChemblInteractions
DOVITINIB RET

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Phase I

PMIDs:
25103625

Sources:
ClearityFoundationClinicalTrial DTC JAX-CKB
DOVITINIB MELK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MARK2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB FLT4

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name dovitinib, TKI-258, CHIR-258

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions
DOVITINIB KIT

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Stem cell growth factor receptor inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC GuideToPharmacology ChemblInteractions
DOVITINIB PAK4

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB TYRO3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB IRAK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB BRSK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CAMK2G

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PKN2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MARK3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB ACVR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB ITK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CSNK1D

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB HCK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CLK2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB LIMK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB LRRK2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB KDR

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC TdgClinicalTrial TALC GuideToPharmacology ChemblInteractions
DOVITINIB CDK7

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP4K2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MST1R

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB STK3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB AXL

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PRKAA1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CHEK2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PLK4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MINK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB NTRK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC
DOVITINIB RPS6KB1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB FLT3

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
DTC GuideToPharmacology ChemblInteractions
DOVITINIB TYK2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PRKD2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB INSR

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DTC GuideToPharmacology
DOVITINIB SLK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PDPK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP4K5

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB RPS6KA3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PRKCD

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB NTRK3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB ROCK2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PRKD3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB BTK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP4K4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB BLK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB FYN

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP2K2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB LYN

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAPK10

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAPK8

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB NTRK2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CLK4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB MAP2K1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CHEK1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB ALK

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB AURKB

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB LCK

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB NR1I2

Interaction Score: 0.01

Interaction Types & Directionality:

suppressor (inhibitory)

Interaction Info:

PMIDs:
25521244

Sources:
DrugBank
DOVITINIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB JAK2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB SRC

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB EGFR

Interaction Score: 0.0

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DOVITINIB YES1

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB05928

Version: 5.1.7

Alternate Names:

DOVITINIB DrugBank Drug Name

405169-16-6 CAS Number

CHEMBL522892 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Categories bcrp/abcg2 inducers

Publications:

Weiss J et al., 2014, Interaction potential of the multitargeted receptor tyrosine kinase inhibitor dovitinib with drug transporters and drug metabolising enzymes assessed in vitro., Pharmaceutics

MyCancerGenome: DOVITINIB
- Version: 20-Jun-2017
Alternate Names:

TKI258 Development Name

CHIR-258 Development Name

DOVITINIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

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

4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one PubChem Drug Name

9886808 PubChem Drug ID

Dovitinib Drug Trade Name

Drug Info:

Drug Class FGFR Inhibitor

Source Reported Drug Name(s) Dovitinib/TKI258

Pharmaceutical Developer Novartis

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: Dovitinib

Version: 27-September-2017

Alternate Names:

Drug 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.

André et al., 2013, Targeting FGFR with dovitinib (TKI258): preclinical and clinical data in breast cancer., Clin. Cancer Res.

Lim et al., 2016, Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 study., Cancer

DoCM: DOVITINIB

Version: 27-September-2017

Alternate Names:

Drug 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.

Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

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

CIViC: DOVITINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

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.

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

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

DTC: DOVITINIB
- Version: 02-September-2020
Alternate Names:

CHEMBL522892 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178102585
- Version: 29-September-2020
Alternate Names:

DOVITINIB GuideToPharmacology Ligand Name

Drug Info:

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

DOVITINIB Primary Drug Name

DOVITINIB Drug Generic Name

TKI-258 Drug Synonym

Drug Info:

Publications:
TTD: TKI258
- Version: 2020.06.01
Alternate Names:

D07OZR TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL522892
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
CGI: Dovitinib
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL522892
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	dovitinib, TKI-258, CHIR-258
Variant Effect	gain-of-function

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

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

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

Mechanism of Interaction	Vascular endothelial growth factor receptor inhibitor
Direct Interaction	yes
Reported Cancer Type	Prostate

Mechanism of Interaction	Platelet-derived growth factor receptor inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

Mechanism of Interaction	Stem cell growth factor receptor inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

Mechanism of Interaction	Tyrosine-protein kinase receptor FLT3 inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

DOVITINIB	DrugBank Drug Name
405169-16-6	CAS Number
CHEMBL522892	ChEMBL ID

TKI258	Development Name
CHIR-258	Development Name
DOVITINIB	Generic Name

Drug family	FGFR inhibitor
Alteration	FGF3:amp

Drug family	FGFR inhibitor
Alteration	FGF4:amp

4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one	PubChem Drug Name
9886808	PubChem Drug ID
Dovitinib	Drug Trade Name

DOVITINIB	Primary Drug Name
DOVITINIB	Drug Generic Name
TKI-258	Drug Synonym

DOVITINIB Drug Record

DOVITINIB chembl:CHEMBL522892 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Drug family FGFR inhibitor Alteration FGF3:amp

PMIDs: None found

Sources: CGI

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: 22238366 26619011 23658459 23443805 18552176 23908597 23002168 26036639 24448819

Sources: ClearityFoundationClinicalTrial DoCM JAX-CKB TdgClinicalTrial CIViC TALC MyCancerGenome CGI

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 22238366 23175443 24325461 27932416 28034880 21119661 25589496

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

Interaction Types & Directionality: n/a

Interaction Info: Drug family FGFR inhibitor Alteration FGF4:amp

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 22238366 23658459 27315356 17698633

Sources: ClearityFoundationClinicalTrial DTC JAX-CKB TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24124571

Sources: ClearityFoundationClinicalTrial CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 28759044

Sources: ClearityFoundationClinicalTrial DTC CIViC GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family FGFR inhibitor

Alteration FGF3:amp

PMIDs:
None found

Sources:
CGI

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:
22238366 26619011 23658459 23443805 18552176 23908597 23002168 26036639 24448819

Sources:
ClearityFoundationClinicalTrial DoCM JAX-CKB TdgClinicalTrial CIViC TALC MyCancerGenome CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Indication/Tumor Type bladder urothelial carcinoma

Approval Status Preclinical - Cell culture

PMIDs:
22238366 23175443 24325461 27932416 28034880 21119661 25589496

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

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family FGFR inhibitor

Alteration FGF4:amp

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
22238366 23658459 27315356 17698633

Sources:
ClearityFoundationClinicalTrial DTC JAX-CKB TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24124571

Sources:
ClearityFoundationClinicalTrial CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
28759044

Sources:
ClearityFoundationClinicalTrial DTC CIViC GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Reported Cancer Type Prostate

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial CancerCommons DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dovitinib, TKI-258, CHIR-258

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC