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DACOMITINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • DACOMITINIB chembl:CHEMBL2105719 ApprovedAntineoplastic

    Alternate Names:

    PF-00299804
    VIZIMPRO
    DACOMITINIB
    PF-00299804-03

    Drug Info:

    Pharmaceutical Developer Pfizer
    Source Reported Drug Name(s) PF-00299804/Dacomitinib
    Drug Class EGFR Inhibitor
    Drug Class Kinase Inhibitors
    FDA Approval not approved
    Drug Class small molecule
    Drug Indications antineoplastic agent
    (11 More Sources)

    Publications:

    Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem
    Yasuda et al., 2012, EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications., Lancet Oncol.
    Engelman et al., 2007, PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib., Cancer Res.
    Jänne et al., 2014, Dacomitinib as first-line treatment in patients with clinically or molecularly selected advanced non-small-cell lung cancer: a multicentre, open-label, phase 2 trial., Lancet Oncol.
    Zahonero et al., 2015, Preclinical Test of Dacomitinib, an Irreversible EGFR Inhibitor, Confirms Its Effectiveness for Glioblastoma., Mol. Cancer Ther.
    Ma et al., 2016, InsR/IGF1R Pathway Mediates Resistance to EGFR Inhibitors in Glioblastoma., Clin. Cancer Res.
    Kobayashi et al., 2015, EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs., Clin. Cancer Res.
    Kobayashi et al., 2017, Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer., Mol. Cancer Ther.
    Kosaka et al., 2017, Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors., Cancer Res.
    Gerber et al., 2014, Management and future directions in non-small cell lung cancer with known activating mutations., Am Soc Clin Oncol Educ Book
    Wu YL et al., 2017, Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial., Lancet Oncol
    Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med
    Ramalingam et al., 2016, Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials., Ann. Oncol.
    Brzezniak C et al., 2013, Dacomitinib, a new therapy for the treatment of non-small cell lung cancer., Expert Opin Pharmacother
    Fry et al., 1998, Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor., Proc. Natl. Acad. Sci. U.S.A.
    Gonzales et al., 2008, Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor., Mol. Cancer Ther.
    Kalous et al., 2012, Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib., Mol. Cancer Ther.
    Kris et al., 2015, Targeting HER2 aberrations as actionable drivers in lung cancers: phase II trial of the pan-HER tyrosine kinase inhibitor dacomitinib in patients with HER2-mutant or amplified tumors., Ann. Oncol.
    Nam et al., 2012, Evaluation of the antitumor effects and mechanisms of PF00299804, a pan-HER inhibitor, alone or in combination with chemotherapy or targeted agents in gastric cancer., Mol. Cancer Ther.
  • DACOMITINIB   EGFR

    Interaction Score: 2.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name PF-299804
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    23930994 21764376 18089823 25456362 25939761 26561558 26206867 27913578 28363995 24857124 28958502 21430269 26768165 23294134 9751783


    Sources:
    TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

  • DACOMITINIB   ERBB4

    Interaction Score: 1.87

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name PF-299804
    Novel drug target Novel Target
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome TdgClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

  • DACOMITINIB   ERBB2

    Interaction Score: 1.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    18606718 22761403 25899785 22135232 28363995


    Sources:
    TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC MyCancerGenomeClinicalTrial TTD

  • DACOMITINIB   ERBB3

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Epidermal growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • DACOMITINIB   PTEN

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BMS-754807 + Dacomitinib
    Indication/Tumor Type glioblastoma multiforme
    Response Type sensitive

    PMIDs:
    25939761 26561558


    Sources:
    JAX-CKB

  • CancerCommons: PF-00299804

    • Version: 25-July-2013

    Alternate Names:
    11511120 PubChem Drug ID
    Dacomitinib Drug Trade Name

    Drug Info:
    Drug Class EGFR Inhibitor
    Source Reported Drug Name(s) PF-00299804/Dacomitinib
    Pharmaceutical Developer Pfizer

    Publications:

  • MyCancerGenome: DACOMITINIB

    • Version: 20-Jun-2017

    Alternate Names:
    DACOMITINIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • TdgClinicalTrial: DACOMITINIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • DTC: DACOMITINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL2110732 ChEMBL Drug ID

    Drug Info:

    Publications:
    Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem

  • JAX-CKB: Dacomitinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Nam et al., 2012, Evaluation of the antitumor effects and mechanisms of PF00299804, a pan-HER inhibitor, alone or in combination with chemotherapy or targeted agents in gastric cancer., Mol. Cancer Ther.
    Gonzales et al., 2008, Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor., Mol. Cancer Ther.
    Kris et al., 2015, Targeting HER2 aberrations as actionable drivers in lung cancers: phase II trial of the pan-HER tyrosine kinase inhibitor dacomitinib in patients with HER2-mutant or amplified tumors., Ann. Oncol.

  • CIViC: DACOMITINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Ramalingam et al., 2016, Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials., Ann. Oncol.
    Wu YL et al., 2017, Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial., Lancet Oncol
    Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med

  • TTD: Dacomitinib

    • Version: 2020.06.01

    Alternate Names:
    D06XXH TTD Drug ID

    Drug Info:

    Publications:

  • TALC: DACOMITINIB

    • Version: 12-May-2016

    Alternate Names:
    DACOMITINIB Drug Generic Name
    DACOMITINIB Primary Drug Name
    PF299804 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2105719

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2105719

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: DACOMITINIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2110732

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Dacomitinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: dacomitinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Dacomitinib

    • Version: 04-September-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