DGIdb - LESTAURTINIB Drug Record

LESTAURTINIB chembl:CHEMBL603469 Antineoplastic

Alternate Names:

LESTAURTINIB
SPM-924
SP924
KT-5555
KT-555
A-1544750
CEP-701
SP-924
A-154475

Drug Info:

Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent

(5 More Sources)

Publications:

Vaishnavi et al., 2013, Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer., Nat. Med.
Jin et al., 2005, The ETV6-NTRK3 chimeric tyrosine kinase suppresses TGF-beta signaling by inactivating the TGF-beta type II receptor., Proc. Natl. Acad. Sci. U.S.A.
Kancha et al., 2007, Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations., Exp. Hematol.
Wang et al., 2012, MicroRNAs in liver disease., Gastroenterology
Piloto et al., 2007, Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways., Blood
Mathews et al., 2007, Impact of FLT3 mutations and secondary cytogenetic changes on the outcome of patients with newly diagnosed acute promyelocytic leukemia treated with a single agent arsenic trioxide regimen., Haematologica
Zimmerman et al., 2013, Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia., Blood
Bagrintseva et al., 2004, Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells., Blood
Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
Yamamoto et al., 2001, Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies., Blood
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Mardis et al., 2009, Recurring mutations found by sequencing an acute myeloid leukemia genome., N. Engl. J. Med.
Martelli et al., 2013, Mutational landscape of AML with normal cytogenetics: biological and clinical implications., Blood Rev.
Allen et al., 2013, The importance of relative mutant level for evaluating impact on outcome of KIT, FLT3 and CBL mutations in core-binding factor acute myeloid leukemia., Leukemia
Knapper et al., 2006, A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy., Blood
Man et al., 2012, Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation., Blood
Brown et al., 2005, FLT3 inhibition selectively kills childhood acute lymphoblastic leukemia cells with high levels of FLT3 expression., Blood
Eisenhoffer et al., 2012, Crowding induces live cell extrusion to maintain homeostatic cell numbers in epithelia., Nature
Clark et al., 2004, Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518., Blood
Smith et al., 2013, The role of kinase inhibitors in the treatment of patients with acute myeloid leukemia., Am Soc Clin Oncol Educ Book
Jourdan et al., 2013, Prospective evaluation of gene mutations and minimal residual disease in patients with core binding factor acute myeloid leukemia., Blood
Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
Fischer et al., 2010, Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3., J. Clin. Oncol.
Smith et al., 2004, Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia., Blood
Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

LESTAURTINIB FLT3

Interaction Score: 2.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name lestaurtinib , CEP-701

Clinical Status case report

PMIDs:
17889720 22504185 17047150 17606455 24046014 14604974 23430109 11290608 25157968 19657110 23261068 23783394 16857985 22368270 15374878 22504183 15256420 23714533 23321257 22504184 20733134 14726387 22858906

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM CIViC TTD
LESTAURTINIB ETV6

Interaction Score: 1.03

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
16258068

Sources:
JAX-CKB
LESTAURTINIB NTRK1

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name lestaurtinib , CEP-701

Mechanism of Interaction Nerve growth factor receptor Trk-A inhibitor

PMIDs:
24162815

Sources:
TdgClinicalTrial ChemblInteractions CIViC
LESTAURTINIB JAK2

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name lestaurtinib, CEP-701

Novel drug target Novel Target

Indication/Tumor Type hematologic cancer

PMIDs:
21926964

Sources:
TdgClinicalTrial JAX-CKB ChemblInteractions
LESTAURTINIB NTRK3

Interaction Score: 0.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction NT-3 growth factor receptor inhibitor

Direct Interaction yes

Novel drug target Novel Target

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
LESTAURTINIB NTRK2

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Neurotrophic tyrosine kinase receptor type 2 inhibitor

Direct Interaction yes

Trial Name lestaurtinib , CEP-701

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
LESTAURTINIB RET

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
LESTAURTINIB MTOR

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LESTAURTINIB HTT

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LESTAURTINIB AR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

CEP-701 Development Name

LESTAURTINIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: Lestaurtinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Jin et al., 2005, The ETV6-NTRK3 chimeric tyrosine kinase suppresses TGF-beta signaling by inactivating the TGF-beta type II receptor., Proc. Natl. Acad. Sci. U.S.A.

Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

DoCM: LESTAURTINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Kancha et al., 2007, Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations., Exp. Hematol.

Mardis et al., 2009, Recurring mutations found by sequencing an acute myeloid leukemia genome., N. Engl. J. Med.

Knapper et al., 2006, A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy., Blood

CIViC: LESTAURTINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Smith et al., 2004, Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia., Blood

Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia

Vaishnavi et al., 2013, Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer., Nat. Med.

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

CHEMBL603469 ChEMBL Drug ID

Drug Info:

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

D0V9WF TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL603469
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL603469
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	lestaurtinib , CEP-701
Clinical Status	case report

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	sensitive

Trial Name	lestaurtinib, CEP-701
Novel drug target	Novel Target
Indication/Tumor Type	hematologic cancer

Mechanism of Interaction	NT-3 growth factor receptor inhibitor
Direct Interaction	yes
Novel drug target	Novel Target

Mechanism of Interaction	Neurotrophic tyrosine kinase receptor type 2 inhibitor
Direct Interaction	yes
Trial Name	lestaurtinib , CEP-701

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

LESTAURTINIB Drug Record

LESTAURTINIB chembl:CHEMBL603469 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name lestaurtinib , CEP-701 Clinical Status case report

PMIDs: 17889720 22504185 17047150 17606455 24046014 14604974 23430109 11290608 25157968 19657110 23261068 23783394 16857985 22368270 15374878 22504183 15256420 23714533 23321257 22504184 20733134 14726387 22858906

Sources: MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM CIViC TTD

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical Response Type sensitive

PMIDs: 16258068

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name lestaurtinib , CEP-701 Mechanism of Interaction Nerve growth factor receptor Trk-A inhibitor

PMIDs: 24162815

Sources: TdgClinicalTrial ChemblInteractions CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name lestaurtinib, CEP-701 Novel drug target Novel Target Indication/Tumor Type hematologic cancer

PMIDs: 21926964

Sources: TdgClinicalTrial JAX-CKB ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction NT-3 growth factor receptor inhibitor Direct Interaction yes Novel drug target Novel Target

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Neurotrophic tyrosine kinase receptor type 2 inhibitor Direct Interaction yes Trial Name lestaurtinib , CEP-701

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

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

MyCancerGenome: LESTAURTINIB

Alternate Names: CEP-701 Development Name LESTAURTINIB Generic Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

TdgClinicalTrial: LESTAURTINIB

Alternate Names:

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

Publications:

JAX-CKB: Lestaurtinib

Alternate Names:

Drug Info:

DoCM: LESTAURTINIB

Alternate Names:

Drug Info:

CIViC: LESTAURTINIB

Alternate Names:

Drug Info:

DTC: LESTAURTINIB

Alternate Names: CHEMBL603469 ChEMBL Drug ID

Drug Info:

Publications:

TTD: Lestaurtinib

Alternate Names: D0V9WF TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL603469

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL603469

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name lestaurtinib , CEP-701

Clinical Status case report

PMIDs:
17889720 22504185 17047150 17606455 24046014 14604974 23430109 11290608 25157968 19657110 23261068 23783394 16857985 22368270 15374878 22504183 15256420 23714533 23321257 22504184 20733134 14726387 22858906

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM CIViC TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
16258068

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name lestaurtinib , CEP-701

Mechanism of Interaction Nerve growth factor receptor Trk-A inhibitor

PMIDs:
24162815

Sources:
TdgClinicalTrial ChemblInteractions CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name lestaurtinib, CEP-701

Novel drug target Novel Target

Indication/Tumor Type hematologic cancer

PMIDs:
21926964

Sources:
TdgClinicalTrial JAX-CKB ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction NT-3 growth factor receptor inhibitor

Direct Interaction yes

Novel drug target Novel Target

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Neurotrophic tyrosine kinase receptor type 2 inhibitor

Direct Interaction yes

Trial Name lestaurtinib , CEP-701

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

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

Alternate Names:

CEP-701 Development Name

LESTAURTINIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

CHEMBL603469 ChEMBL Drug ID

Alternate Names:

D0V9WF TTD Drug ID