DGIdb - BOSUTINIB Drug Record

BOSUTINIB chembl:CHEMBL288441 ApprovedAntineoplasticImmunotherapy

Alternate Names:

BOSUTINIB MONOHYDRATE
BOSULIF
SKI-606
SK-606
BOSUTINIB
SKI 606
BOSUTINIBUM
SK 606
4-((2,4-DICHLORO-5-METHOXYPHENYL)AMINO)-6-METHOXY-7-(3-(4-METHYL-1-PIPERAZINYL)PROPOXY)-3-QUINOLINECARBONITRILE
4-((2,4-DICHLORO-5-METHOXYPHENYL)AMINO)-6-METHOXY-7-(3-(4-METHYLPIPERAZIN-1-YL)PROPOXY)QUINOLINE-3-CARBONITRILE
3-QUINOLINECARBONITRILE, 4-((2,4-DICHLORO-5-METHOXYPHENYL)AMINO)-6-METHYL-1-PIPERAZINYL)PROPOXY)-
BOSULIF®
chemidplus:380843-75-4
pubchem.compound:5328940
drugbank:06616
chembl:CHEMBL288441
rxcui:1307619

Drug Info:

FDA Approval	Chronic myelogenous leukemia (Philadelphia chromosome positive)
Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent

(8 More Sources)

Publications:

Cang et al., 2008, P-loop mutations and novel therapeutic approaches for imatinib failures in chronic myeloid leukemia., J Hematol Oncol
Soverini et al., 2006, Presence or the emergence of a F317L BCR-ABL mutation may be associated with resistance to dasatinib in Philadelphia chromosome-positive leukemia., J. Clin. Oncol.
Eskazan et al., 2011, Chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation are resistant to dasatinib: is that true for all the patients?, Leuk. Res.
Oyekunle et al., 2011, F317L BCR-ABL1 kinase domain mutation associated with a sustained major molecular response in a CML patient on dasatinib., Leuk. Res.
Branford et al., 2003, Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis., Blood
Strhakova et al., 2011, Use of direct sequencing for detection of mutations in the BCR-ABL kinase domain in Slovak patients with chronic myeloid leukemia., Neoplasma
Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma
Sorel et al., 2004, Evidence of ABL-kinase domain mutations in highly purified primitive stem cell populations of patients with chronic myelogenous leukemia., Biochem. Biophys. Res. Commun.
Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology
Doi et al., 2009, High-resolution melting analysis for a reliable and two-step scanning of mutations in the tyrosine kinase domain of the chimerical bcr-abl gene., Int. J. Hematol.
O'Hare et al., 2004, Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML., Blood
Elias et al., 2014, BCR-ABL kinase domain mutations, including 2 novel mutations in imatinib resistant Malaysian chronic myeloid leukemia patients-Frequency and clinical outcome., Leuk. Res.
Qin et al., 2011, Characteristics of BCR-ABL kinase domain point mutations in Chinese imatinib-resistant chronic myeloid leukemia patients., Ann. Hematol.
Hughes et al., 2009, Impact of baseline BCR-ABL mutations on response to nilotinib in patients with chronic myeloid leukemia in chronic phase., J. Clin. Oncol.
Al-Ali et al., 2004, High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib., Hematol. J.
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Jones et al., 2008, Kinase domain point mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia emerge after therapy with BCR-ABL kinase inhibitors., Cancer
von Bubnoff et al., 2003, Inhibition of wild-type and mutant Bcr-Abl by pyrido-pyrimidine-type small molecule kinase inhibitors., Cancer Res.
von Bubnoff et al., 2002, BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study., Lancet
Branford et al., 2002, High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance., Blood
Eide et al., 2011, The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile., Cancer Res.
Hochhaus et al., 2002, Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy., Leukemia
Soverini et al., 2011, BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet., Blood
Nam et al., 2016, Src as a Therapeutic Target in Biliary Tract Cancer., Mol. Cancer Ther.
Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.

BOSUTINIB ABL1

Interaction Score: 5.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status NCCN guidelines

PMIDs:
18828913 17114651 21605905 21489624 12623848 21895409 20367437 15381060 23676790 19466505 15256422 24456693 20697894 19652056 14745431 25157968 18615627 14559829 11853795 11964322 21505103 12399961 21562040

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM COSMIC PharmGKB TTD FDA OncoKB
BOSUTINIB BCR

Interaction Score: 1.72

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Fusion protein BCR:ABL1

PMIDs:
None found

Sources:
PharmGKB FDA
BOSUTINIB SRC

Interaction Score: 1.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase SRC inhibitor

Direct Interaction yes

Notes

PMIDs:
27196758

Sources:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions TTD
BOSUTINIB HCK

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase HCK inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
BOSUTINIB LYN

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase Lyn inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BOSUTINIB EGFR

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Osimertinib + Bosutinib + PF-573328

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
28416483

Sources:
JAX-CKB

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

SKI-606 Development Name

BOSUTINIB Generic Name

BOSULIF Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive)

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: Bosutinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Nam et al., 2016, Src as a Therapeutic Target in Biliary Tract Cancer., Mol. Cancer Ther.

Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.

DoCM: BOSUTINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Al-Ali et al., 2004, High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib., Hematol. J.

O'Hare et al., 2004, Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML., Blood

Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology

TALC: BOSUTINIB
- Version: 12-May-2016
Alternate Names:

BOSUTINIB Primary Drug Name

BOSUTINIB Drug Generic Name

SKI-606 Drug Synonym

Drug Info:

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

D0OB0F TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL288441
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Bosutinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL288441
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
PharmGKB: bosutinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
COSMIC: Bosutinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Variant Effect	gain-of-function
Pathway	activation
Clinical Status	NCCN guidelines

Mechanism of Interaction	Tyrosine-protein kinase SRC inhibitor
Direct Interaction	yes
Notes

Direct Interaction	yes
Mechanism of Interaction	Tyrosine-protein kinase HCK inhibitor

Mechanism of Interaction	Tyrosine-protein kinase Lyn inhibitor
Direct Interaction	yes

combination therapy	Osimertinib + Bosutinib + PF-573328
Indication/Tumor Type	lung cancer
Response Type	sensitive

SKI-606	Development Name
BOSUTINIB	Generic Name
BOSULIF	Trade Name

BOSUTINIB	Primary Drug Name
BOSUTINIB	Drug Generic Name
SKI-606	Drug Synonym

BOSUTINIB Drug Record

BOSUTINIB chembl:CHEMBL288441 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

BOSUTINIB ABL1

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Variant Effect gain-of-function Pathway activation Clinical Status NCCN guidelines

PMIDs: 18828913 17114651 21605905 21489624 12623848 21895409 20367437 15381060 23676790 19466505 15256422 24456693 20697894 19652056 14745431 25157968 18615627 14559829 11853795 11964322 21505103 12399961 21562040

Sources: MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM COSMIC PharmGKB TTD FDA OncoKB

BOSUTINIB BCR

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Fusion protein BCR:ABL1

PMIDs: None found

Sources: PharmGKB FDA

BOSUTINIB SRC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase SRC inhibitor Direct Interaction yes Notes

PMIDs: 27196758

Sources: TALC TdgClinicalTrial JAX-CKB ChemblInteractions TTD

BOSUTINIB HCK

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

BOSUTINIB LYN

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

BOSUTINIB EGFR

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Osimertinib + Bosutinib + PF-573328 Indication/Tumor Type lung cancer Response Type sensitive

PMIDs: 28416483

Sources: JAX-CKB

MyCancerGenome: BOSUTINIB

Alternate Names: SKI-606 Development Name BOSUTINIB Generic Name BOSULIF Trade Name

Drug Info: Drug Class Kinase Inhibitors FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive)

Publications:

TdgClinicalTrial: BOSUTINIB

Alternate Names:

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

Publications:

JAX-CKB: Bosutinib

Alternate Names:

Drug Info:

Publications: Nam et al., 2016, Src as a Therapeutic Target in Biliary Tract Cancer., Mol. Cancer Ther. Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.

DoCM: BOSUTINIB

Alternate Names:

Drug Info:

TALC: BOSUTINIB

Alternate Names: BOSUTINIB Primary Drug Name BOSUTINIB Drug Generic Name SKI-606 Drug Synonym

Drug Info:

Publications:

TTD: Bosutinib

Alternate Names: D0OB0F TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL288441

Alternate Names:

Drug Info:

Publications:

FDA: Bosutinib

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL288441

Alternate Names:

Drug Info:

Publications:

PharmGKB: bosutinib

Alternate Names:

Drug Info:

Publications:

OncoKB: Bosutinib

Alternate Names:

Drug Info:

Publications:

COSMIC: Bosutinib

Alternate Names:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status NCCN guidelines

PMIDs:
18828913 17114651 21605905 21489624 12623848 21895409 20367437 15381060 23676790 19466505 15256422 24456693 20697894 19652056 14745431 25157968 18615627 14559829 11853795 11964322 21505103 12399961 21562040

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions DoCM COSMIC PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Fusion protein BCR:ABL1

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase SRC inhibitor

Direct Interaction yes

Notes

PMIDs:
27196758

Sources:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase HCK inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase Lyn inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Osimertinib + Bosutinib + PF-573328

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
28416483

Sources:
JAX-CKB

Alternate Names:

SKI-606 Development Name

BOSUTINIB Generic Name

BOSULIF Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive)

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

Nam et al., 2016, Src as a Therapeutic Target in Biliary Tract Cancer., Mol. Cancer Ther.

Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.

Alternate Names:

BOSUTINIB Primary Drug Name

BOSUTINIB Drug Generic Name

SKI-606 Drug Synonym

Alternate Names:

D0OB0F TTD Drug ID