DGIdb - PEXIDARTINIB Drug Record

PEXIDARTINIB chembl:CHEMBL3813873 ApprovedAntineoplastic

Alternate Names:

CML-261
PEXIDARTINIB
PLX-3397
PLX3397

Drug Info:

Drug Class	Kinase Inhibitors
Pharmaceutical Developer	Plexxicon
Source Reported Drug Name(s)	PLX3397
Drug Class	Kinase Inhibitor

(5 More Sources)

Publications:

Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov
Cannarile MA et al., 2017, Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy., J Immunother Cancer
Kim et al., 2014, Increased KIT inhibition enhances therapeutic efficacy in gastrointestinal stromal tumor., Clin. Cancer Res.
Tap et al., 2015, Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor., N. Engl. J. Med.
Yan D et al., 2017, Inhibition of colony stimulating factor-1 receptor abrogates microenvironment-mediated therapeutic resistance in gliomas., Oncogene

PEXIDARTINIB CSF1

Interaction Score: 5.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26222558

Sources:
CIViC
PEXIDARTINIB CSF1R

Interaction Score: 0.89

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Macrophage colony stimulating factor receptor inhibitor

Direct Interaction yes

Approval Status Phase I

PMIDs:
26222558 25939769 28759044 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons
PEXIDARTINIB CSF3R

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PEXIDARTINIB KIT

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24583793 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons TTD
PEXIDARTINIB FLT3

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Prostate

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

PMIDs:
25847190 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons TTD
PEXIDARTINIB CDK19

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
PEXIDARTINIB NF1

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-TK inhibitor

Alteration NF1:del

Alteration NF1:.

PMIDs:
None found

Sources:
CGI
PEXIDARTINIB NTRK3

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
PEXIDARTINIB BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy PLX3397 + Vemurafenib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
25939769

Sources:
JAX-CKB
PEXIDARTINIB LCK

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
PEXIDARTINIB FLT1

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
PEXIDARTINIB KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

MyCancerGenome: PLX3397
- Version: 20-Jun-2017
Alternate Names:

PLX108-01 Development Name

PLX3397 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
CancerCommons: PLX3397
- Version: 25-July-2013
Alternate Names:

PLX3397 Drug Development Name

PLX3397 Drug Trade Name

Drug Info:

Drug Class Kinase Inhibitor

Source Reported Drug Name(s) PLX3397

Pharmaceutical Developer Plexxicon

Publications:

JAX-CKB: PLX3397

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer

Tap et al., 2015, Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor., N. Engl. J. Med.

Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov

CIViC: PEXIDARTINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Tap et al., 2015, Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor., N. Engl. J. Med.

Yan D et al., 2017, Inhibition of colony stimulating factor-1 receptor abrogates microenvironment-mediated therapeutic resistance in gliomas., Oncogene

Smith et al., 2015, Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397., Cancer Discov

TTD: PLX-3397
- Version: 2020.06.01
Alternate Names:

D09TAB TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 252827368
- Version: 29-September-2020
Alternate Names:

PEXIDARTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3813873
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3545158
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
CGI: PLX3397
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Macrophage colony stimulating factor receptor inhibitor
Direct Interaction	yes
Approval Status	Phase I

Indication/Tumor Type	gastrointestinal stromal tumor
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

Reported Cancer Type	Prostate
Indication/Tumor Type	Advanced Solid Tumor
Response Type	resistant

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

combination therapy	PLX3397 + Vemurafenib
Indication/Tumor Type	melanoma
Response Type	sensitive

Drug family	Pan-TK inhibitor
Alteration	NF1:del
Alteration	NF1:.

PLX108-01	Development Name
PLX3397	Development Name

PLX3397	Drug Development Name
PLX3397	Drug Trade Name

PEXIDARTINIB Drug Record

PEXIDARTINIB chembl:CHEMBL3813873 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26222558

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Macrophage colony stimulating factor receptor inhibitor Direct Interaction yes Approval Status Phase I

PMIDs: 26222558 25939769 28759044 28716061

Sources: MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type gastrointestinal stromal tumor Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 24583793 28716061

Sources: MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Prostate Indication/Tumor Type Advanced Solid Tumor Response Type resistant

PMIDs: 25847190 28716061

Sources: MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Drug family Pan-TK inhibitor Alteration NF1:del Alteration NF1:.

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: combination therapy PLX3397 + Vemurafenib Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 25939769

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

MyCancerGenome: PLX3397

Alternate Names: PLX108-01 Development Name PLX3397 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

CancerCommons: PLX3397

Alternate Names: PLX3397 Drug Development Name PLX3397 Drug Trade Name

Drug Info: Drug Class Kinase Inhibitor Source Reported Drug Name(s) PLX3397 Pharmaceutical Developer Plexxicon

Publications:

JAX-CKB: PLX3397

Alternate Names:

Drug Info:

CIViC: PEXIDARTINIB

Alternate Names:

Drug Info:

TTD: PLX-3397

Alternate Names: D09TAB TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 252827368

Alternate Names: PEXIDARTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL3813873

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL3545158

Interaction Types & Directionality:

n/a

PMIDs:
26222558

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Macrophage colony stimulating factor receptor inhibitor

Direct Interaction yes

Approval Status Phase I

PMIDs:
26222558 25939769 28759044 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24583793 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Prostate

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

PMIDs:
25847190 28716061

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CIViC GuideToPharmacology CancerCommons TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-TK inhibitor

Alteration NF1:del

Alteration NF1:.

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy PLX3397 + Vemurafenib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
25939769

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Alternate Names:

PLX108-01 Development Name

PLX3397 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

PLX3397 Drug Development Name

PLX3397 Drug Trade Name

Drug Info:

Drug Class Kinase Inhibitor

Source Reported Drug Name(s) PLX3397

Pharmaceutical Developer Plexxicon

Alternate Names:

D09TAB TTD Drug ID

Alternate Names:

PEXIDARTINIB GuideToPharmacology Ligand Name