DGIdb - FORETINIB Drug Record

FORETINIB chembl:CHEMBL1230609 Antineoplastic

Alternate Names:

EXEL-2880
XL880
GSK-1363089G
GSK1363089G
XL-880
GSK089
GSK1363089
FORETINIB
GSK 1363089G
XL 880
chembl:CHEMBL1230609
drugbank:12307
chemidplus:849217-64-7
pubchem.compound:42642645

Drug Info:

Pharmaceutical Developer	GlaxoSmithKline
Source Reported Drug Name(s)	GSK1363089
Drug Class	MET/VEGFR Inhibitor
Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	small molecule
Drug Indications	antineoplastic agent
Drug Categories	amides
Drug Categories	amines
Drug Categories	aniline compounds
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	receptors, vascular endothelial growth factor, antagonists & inhibitors
Drug Categories	tyrosine kinase inhibitors

(9 More Sources)

Publications:

Choueiri et al., 2013, Phase II and biomarker study of the dual MET/VEGFR2 inhibitor foretinib in patients with papillary renal cell carcinoma., J. Clin. Oncol.
Du et al., 2016, Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors., Nat. Med.
Song et al., 2015, Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1-Rearranged Non-Small Cell Lung Cancer., Clin. Cancer Res.
Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.

FORETINIB PTCH1

Interaction Score: 1.35

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family MET inhibitor

Alteration PTCH1:.

PMIDs:
None found

Sources:
CGI
FORETINIB ROS1

Interaction Score: 0.41

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25688157 26372962

Sources:
CIViC
FORETINIB MET

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Approval Status Preclinical

combination therapy Foretinib + Rucaparib

Evidence Type Actionable

PMIDs:
23213094 26779812

Sources:
CancerCommons JAX-CKB TdgClinicalTrial CIViC TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions
FORETINIB HGF

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
FORETINIB KDR

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions
FORETINIB TEK

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase TIE-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FORETINIB MST1R

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
FORETINIB FLT1

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
MyCancerGenome GuideToPharmacology ChemblInteractions
FORETINIB FLT4

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
MyCancerGenome GuideToPharmacology ChemblInteractions
FORETINIB PDGFRA

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
FORETINIB KIT

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Stem cell growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FORETINIB PDGFRB

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FORETINIB FLT3

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FORETINIB YES1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

CancerCommons: GSK1363089
- Version: 25-July-2013
Alternate Names:

GSK1363089 PubChem Drug Name

42642645 PubChem Drug ID

Foretinib Drug Trade Name

Drug Info:

Drug Class MET/VEGFR Inhibitor

Source Reported Drug Name(s) GSK1363089

Pharmaceutical Developer GlaxoSmithKline

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

EXEL-2880 Development Name

GSK1363089 Development Name

XL880 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
DrugBank: DB12307
- Version: 5.1.7
Alternate Names:

FORETINIB DrugBank Drug Name

849217-64-7 CAS Number

CHEMBL1230609 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Categories amides

Publications:
TdgClinicalTrial: XL880
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:
JAX-CKB: Foretinib
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Du et al., 2016, Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors., Nat. Med.

CIViC: FORETINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Choueiri et al., 2013, Phase II and biomarker study of the dual MET/VEGFR2 inhibitor foretinib in patients with papillary renal cell carcinoma., J. Clin. Oncol.

Song et al., 2015, Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1-Rearranged Non-Small Cell Lung Cancer., Clin. Cancer Res.

Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.

TTD: XL880
- Version: 2020.06.01
Alternate Names:

D0D1GF TTD Drug ID

Drug Info:

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

FORETINIB Primary Drug Name

FORETINIB Drug Generic Name

GSK1363089 Drug Synonym

Drug Info:

Publications:
DTC: FORETINIB
- Version: 02-September-2020
Alternate Names:

CHEMBL1230609 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178102306
- Version: 29-September-2020
Alternate Names:

FORETINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1230609
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1230609
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

Approval Status	Preclinical
combination therapy	Foretinib + Rucaparib
Evidence Type	Actionable

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

Mechanism of Interaction	Tyrosine-protein kinase TIE-2 inhibitor
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Platelet-derived growth factor receptor inhibitor

Mechanism of Interaction	Stem cell growth factor receptor inhibitor
Direct Interaction	yes

Mechanism of Interaction	Tyrosine-protein kinase receptor FLT3 inhibitor
Direct Interaction	yes

GSK1363089	PubChem Drug Name
42642645	PubChem Drug ID
Foretinib	Drug Trade Name

EXEL-2880	Development Name
GSK1363089	Development Name
XL880	Development Name

FORETINIB	DrugBank Drug Name
849217-64-7	CAS Number
CHEMBL1230609	ChEMBL ID

Drug Type	small molecule
Drug Groups	investigational
Drug Categories	amides

Drug family	MET inhibitor
Alteration	PTCH1:.

FORETINIB	Primary Drug Name
FORETINIB	Drug Generic Name
GSK1363089	Drug Synonym

FORETINIB Drug Record

FORETINIB chembl:CHEMBL1230609 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Drug family MET inhibitor Alteration PTCH1:.

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25688157 26372962

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Approval Status Preclinical combination therapy Foretinib + Rucaparib Evidence Type Actionable

PMIDs: 23213094 26779812

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase TIE-2 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes

PMIDs: None found

Sources: TALC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Stem cell growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

CancerCommons: GSK1363089

Alternate Names: GSK1363089 PubChem Drug Name 42642645 PubChem Drug ID Foretinib Drug Trade Name

Drug Info: Drug Class MET/VEGFR Inhibitor Source Reported Drug Name(s) GSK1363089 Pharmaceutical Developer GlaxoSmithKline

Publications:

MyCancerGenome: FORETINIB

Alternate Names: EXEL-2880 Development Name GSK1363089 Development Name XL880 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

DrugBank: DB12307

Alternate Names: FORETINIB DrugBank Drug Name 849217-64-7 CAS Number CHEMBL1230609 ChEMBL ID

Drug Info: Drug Type small molecule Drug Groups investigational Drug Categories amides

Publications:

TdgClinicalTrial: XL880

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class small molecule FDA Approval not approved

Publications:

JAX-CKB: Foretinib

Alternate Names:

Drug Info:

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family MET inhibitor

Alteration PTCH1:.

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

n/a

PMIDs:
25688157 26372962

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Approval Status Preclinical

combination therapy Foretinib + Rucaparib

Evidence Type Actionable

PMIDs:
23213094 26779812

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

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase TIE-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Stem cell growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor FLT3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

GSK1363089 PubChem Drug Name

42642645 PubChem Drug ID

Foretinib Drug Trade Name

Drug Info:

Drug Class MET/VEGFR Inhibitor

Source Reported Drug Name(s) GSK1363089

Pharmaceutical Developer GlaxoSmithKline

Alternate Names:

EXEL-2880 Development Name

GSK1363089 Development Name

XL880 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

FORETINIB DrugBank Drug Name

849217-64-7 CAS Number

CHEMBL1230609 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Categories amides

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:

Du et al., 2016, Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors., Nat. Med.

Alternate Names:

D0D1GF TTD Drug ID

Alternate Names:

FORETINIB Primary Drug Name

FORETINIB Drug Generic Name

GSK1363089 Drug Synonym

Alternate Names:

CHEMBL1230609 ChEMBL Drug ID

Alternate Names:

FORETINIB GuideToPharmacology Ligand Name