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BOSUTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • 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
    Drug Categories cytochrome p-450 cyp2c8 inhibitors
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a inhibitors
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories immunosuppressive agents
    Drug Categories kinase inhibitor
    Drug Categories p-glycoprotein inhibitors
    Drug Categories p-glycoprotein substrates
    Drug Categories p-glycoprotein substrates with narrow therapeutic index
    Drug Categories tyrosine kinase inhibitors
    (11 More Sources)

    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
    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
    Qin et al., 2011, Characteristics of BCR-ABL kinase domain point mutations in Chinese imatinib-resistant chronic myeloid leukemia patients., Ann. Hematol.
    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
    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.
    Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma
    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.
    Cang et al., 2008, P-loop mutations and novel therapeutic approaches for imatinib failures in chronic myeloid leukemia., J Hematol Oncol
    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.
    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
    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., 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
    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.
    Jones et al., 2008, Kinase domain point mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia emerge after therapy with BCR-ABL kinase inhibitors., Cancer
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    von Bubnoff et al., 2003, Inhibition of wild-type and mutant Bcr-Abl by pyrido-pyrimidine-type small molecule kinase inhibitors., Cancer Res.
    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.
    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
    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.
    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.
    Hochhaus et al., 2002, Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy., Leukemia
    Remsing Rix et al., 2009, Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells., Leukemia
    Nam et al., 2016, Src as a Therapeutic Target in Biliary Tract Cancer., Mol. Cancer Ther.
    Ahmad et al., 2013, Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors., J Biomol Screen
    Amsberg et al., 2013, Profile of bosutinib and its clinical potential in the treatment of chronic myeloid leukemia., Onco Targets 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   MAP3K2

    Interaction Score: 1.65

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23134735


    Sources:
    DrugBank

  • BOSUTINIB   STK24

    Interaction Score: 1.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   ABL1

    Interaction Score: 1.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

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


    Sources:
    OncoKB FDA PharmGKB DoCM TdgClinicalTrial TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

  • BOSUTINIB   STK10

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   STK4

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   SIK3

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   BCR

    Interaction Score: 0.62

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Fusion protein BCR:ABL1

    PMIDs:
    None found


    Sources:
    FDA PharmGKB DrugBank

  • BOSUTINIB   SIK1

    Interaction Score: 0.62

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   TXK

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   CAMK2G

    Interaction Score: 0.35

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    23493838


    Sources:
    DrugBank GuideToPharmacology

  • BOSUTINIB   CAMK1D

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   SIK2

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   SRC

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    27196758


    Sources:
    JAX-CKB TdgClinicalTrial TTD DrugBank TALC GuideToPharmacology ChemblInteractions

  • BOSUTINIB   HCK

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    DrugBank ChemblInteractions

  • BOSUTINIB   LYN

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase Lyn inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    DrugBank GuideToPharmacology ChemblInteractions

  • BOSUTINIB   MAP2K2

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19039322


    Sources:
    DrugBank

  • BOSUTINIB   TNK2

    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

  • BOSUTINIB   MAP2K1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19039322


    Sources:
    DrugBank

  • BOSUTINIB   FRK

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   MAP4K5

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BOSUTINIB   FYN

    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

  • BOSUTINIB   CDK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19039322


    Sources:
    DrugBank

  • BOSUTINIB   EGFR

    Interaction Score: 0.03

    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

  • DrugBank: DB06616

    • Version: 5.1.7

    Alternate Names:
    BOSUTINIB DrugBank Drug Name
    380843-75-4 CAS Number
    Bosulif Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories amines

    Publications:
    Remsing Rix et al., 2009, Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells., Leukemia
    Amsberg et al., 2013, Profile of bosutinib and its clinical potential in the treatment of chronic myeloid leukemia., Onco Targets Ther
    Ahmad et al., 2013, Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors., J Biomol Screen

  • 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:

  • GuideToPharmacology: 178102336

    • Version: 29-September-2020

    Alternate Names:
    BOSUTINIB GuideToPharmacology Ligand Name

    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:

  • CGI: Bosutinib

    • Version: 27-September-2017

    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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21