DGIdb - CRENOLANIB Drug Record

CRENOLANIB chembl:CHEMBL2105728 Antineoplastic

Alternate Names:

ARO 002
CP-868596
CP-868,596
CP 868596
CRENOLANIB
ARO-002
chemidplus:670220-88-9
chembl:CHEMBL2105728
pubchem.compound:10366136

Drug Info:

Drug Class	Kinase Inhibitors

(7 More Sources)

Publications:

Smith et al., 2014, Crenolanib is a selective type I pan-FLT3 inhibitor., Proc. Natl. Acad. Sci. U.S.A.
Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
Zhang et al., 2014, Reversal of acquired drug resistance in FLT3-mutated acute myeloid leukemia cells via distinct drug combination strategies., Clin. Cancer Res.
Opatz et al., 2013, Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia., Blood
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
Dewaele et al., 2008, Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation., Clin. Cancer Res.
Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.
Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.

CRENOLANIB PDGFRA

Interaction Score: 2.54

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family FLT3 inhibitor

Alteration PDGFRA:D842V

Alteration PDGFRA:V658A,P577S,R841K,H845Y,G853D

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology TTD
CRENOLANIB FLT3

Interaction Score: 1.0

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

Approval Status Phase II

PMIDs:
24623852 23430109 22504184 24619500 23878140

Sources:
JAX-CKB ChemblInteractions CGI DoCM GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB
CRENOLANIB PDGFRB

Interaction Score: 0.2

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:
ChemblInteractions GuideToPharmacology
CRENOLANIB ALK

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
CRENOLANIB SRC

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CRENOLANIB CSF1R

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:
GuideToPharmacology
CRENOLANIB KIT

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
CRENOLANIB MET

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

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

CP-868569 Development Name

CRENOLANIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:

JAX-CKB: Crenolanib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Smith et al., 2014, Crenolanib is a selective type I pan-FLT3 inhibitor., Proc. Natl. Acad. Sci. U.S.A.

Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.

Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.

DoCM: CRENOLANIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.

Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology

Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

CIViC: CRENOLANIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.

Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.

TTD: CP-868596
- Version: 2020.06.01
Alternate Names:

D0J1GR TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 223366211
- Version: 29-September-2020
Alternate Names:

CRENOLANIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2105728
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:
ChemblInteractions: CHEMBL2105728
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Drug family	FLT3 inhibitor
Alteration	PDGFRA:D842V
Alteration	PDGFRA:V658A,P577S,R841K,H845Y,G853D

Indication/Tumor Type	acute myeloid leukemia
Response Type	sensitive
Approval Status	Phase II

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

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

CP-868569	Development Name
CRENOLANIB	Generic Name

CRENOLANIB Drug Record

CRENOLANIB chembl:CHEMBL2105728 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family FLT3 inhibitor Alteration PDGFRA:D842V Alteration PDGFRA:V658A,P577S,R841K,H845Y,G853D

PMIDs: 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921

Sources: MyCancerGenome JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type acute myeloid leukemia Response Type sensitive Approval Status Phase II

PMIDs: 24623852 23430109 22504184 24619500 23878140

Sources: JAX-CKB ChemblInteractions CGI DoCM GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB

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: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: 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: 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:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

MyCancerGenome: CRENOLANIB

Alternate Names: CP-868569 Development Name CRENOLANIB Generic Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

JAX-CKB: Crenolanib

Alternate Names:

Drug Info:

DoCM: CRENOLANIB

Alternate Names:

Drug Info:

CIViC: CRENOLANIB

Alternate Names:

Drug Info:

TTD: CP-868596

Alternate Names: D0J1GR TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 223366211

Alternate Names: CRENOLANIB GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL2105728

Alternate Names:

Drug Info:

Publications:

MyCancerGenomeClinicalTrial: CRENOLANIB

Alternate Names:

Drug Info:

Publications:

OncoKB: Crenolanib

Alternate Names:

Drug Info:

Publications:

CGI: Crenolanib

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL2105728

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family FLT3 inhibitor

Alteration PDGFRA:D842V

Alteration PDGFRA:V658A,P577S,R841K,H845Y,G853D

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

Approval Status Phase II

PMIDs:
24623852 23430109 22504184 24619500 23878140

Sources:
JAX-CKB ChemblInteractions CGI DoCM GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB

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:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
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:

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)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Alternate Names:

CP-868569 Development Name

CRENOLANIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

D0J1GR TTD Drug ID

Alternate Names:

CRENOLANIB GuideToPharmacology Ligand Name