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OSIMERTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • OSIMERTINIB chembl:CHEMBL3353410 ApprovedAntineoplastic

    Alternate Names:

    AZD-9291
    AZD-9291 FREE BASE
    OSIMERTINIB
    TAGRISSO
    AZD9291
    TAGRISSO®
    MERELETINIB (OBSOLETE INN)
    N-(2-{[2-(DIMETHYLAMINO)ETHYL](METHYL)AMINO}-4-METHOXY-5-{[4-(1-METHYL-1H-INDOL-3-YL)PYRIMIDIN-2-YL]AMINO}PHENYL)PROP-2-ENAMIDE
    MERELETINIB
    AZD 9291
    chembl:CHEMBL3353410
    drugbank:09330
    pubchem.compound:71496458
    chemidplus:1421373-65-0
    rxcui:1721560

    Drug Info:

    FDA Approval Non-small cell lung cancer (with EGFR T790M mutation)
    Drug Class Kinase Inhibitor
    (7 More Sources)

    Publications:

    Thress et al., 2015, Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M., Nat. Med.
    Nukaga et al., 2017, Amplification of EGFR Wild-Type Alleles in Non-Small Cell Lung Cancer Cells Confers Acquired Resistance to Mutation-Selective EGFR Tyrosine Kinase Inhibitors., Cancer Res.
    Mok et al., 2017, Osimertinib or Platinum-Pemetrexed in EGFR T790M-Positive Lung Cancer., N. Engl. J. Med.
    Greig, 2016, Osimertinib: First Global Approval., Drugs
    Sequist et al., 2016, Osimertinib Responses After Disease Progression in Patients Who Had Been Receiving Rociletinib., JAMA Oncol
    Jänne et al., 2015, AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer., N. Engl. J. Med.
    Cross et al., 2014, AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer., Cancer Discov
    Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov
    Konduri et al., 2016, EGFR Fusions as Novel Therapeutic Targets in Lung Cancer., Cancer Discov
    Niu et al., 2014, Novel agents and strategies for overcoming EGFR TKIs resistance., Exp Hematol Oncol
    Ortiz-Cuaran et al., 2016, Heterogeneous Mechanisms of Primary and Acquired Resistance to Third-Generation EGFR Inhibitors., Clin. Cancer Res.
    Ou et al., 2016, High MET amplification level as a resistance mechanism to osimertinib (AZD9291) in a patient that symptomatically responded to crizotinib treatment post-osimertinib progression., Lung Cancer
    Moores et al., 2016, A Novel Bispecific Antibody Targeting EGFR and cMet Is Effective against EGFR Inhibitor-Resistant Lung Tumors., Cancer Res.
    Ballard et al., 2016, Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity., Clin. Cancer Res.
    Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.
    Gallant et al., 2015, EGFR Kinase Domain Duplication (EGFR-KDD) Is a Novel Oncogenic Driver in Lung Cancer That Is Clinically Responsive to Afatinib., Cancer Discov
    Peters et al., 2017, Compound Uncommon EGFR Mutations in a Patient with Advanced NSCLC and Durable Response to Sequential EGFR Targeted Therapies., J Thorac Oncol
    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.
    Ercan et al., 2015, EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors., Clin. Cancer Res.
    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.
    Yosaatmadja et al., 2015, Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed., J. Struct. Biol.
    Starrett JH et al., 2020, Drug Sensitivity and Allele Specificity of First-Line Osimertinib Resistance <i>EGFR</i> Mutations., Cancer Res
    Cho JH et al., 2020, Osimertinib for Patients With Non-Small-Cell Lung Cancer Harboring Uncommon EGFR Mutations: A Multicenter, Open-Label, Phase II Trial (KCSG-LU15-09)., J Clin Oncol
    Castellano GM et al., 2019, A Novel Acquired Exon 20 EGFR M766Q Mutation in Lung Adenocarcinoma Mediates Osimertinib Resistance but is Sensitive to Neratinib and Poziotinib., J Thorac Oncol
    Ninomiya K et al., 2018, MET or NRAS amplification is an acquired resistance mechanism to the third-generation EGFR inhibitor naquotinib., Sci Rep
  • OSIMERTINIB   EGFR

    Interaction Score: 2.43

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy AZD9291 + JNJ-61186372
    Approval Status Preclinical - Cell line xenograft
    Approval Status FDA approved

    PMIDs:
    25939061 28202511 27959700 26729184 26720284 25923549 24893891 27694386 27102076 24410791 27252416 27393507 27216193 27435396 25870145 26286086 28343545 26206867 25948633 28416483 26522274 32193290 31825714 31254668


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions COSMIC CIViC PharmGKB TTD FDA OncoKB

  • OSIMERTINIB   MET

    Interaction Score: 0.82

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27252416 27393507 27694386 29386539


    Sources:
    JAX-CKB CIViC OncoKB

  • OSIMERTINIB   NRAS

    Interaction Score: 0.53

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    25870145


    Sources:
    JAX-CKB

  • OSIMERTINIB   KRAS

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    25870145 27252416


    Sources:
    JAX-CKB

  • OSIMERTINIB   ERBB2

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung adenocarcinoma
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    27252416


    Sources:
    JAX-CKB

  • MyCancerGenome: OSIMERTINIB

    • Version: 20-Jun-2017

    Alternate Names:
    TAGRISSO Trade Name

    Drug Info:
    Drug Class Kinase Inhibitor
    FDA Approval Non-small cell lung cancer (with EGFR T790M mutation)

    Publications:

  • JAX-CKB: Osimertinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.
    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.

  • JAX-CKB: AZD9291

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.
    Ortiz-Cuaran et al., 2016, Heterogeneous Mechanisms of Primary and Acquired Resistance to Third-Generation EGFR Inhibitors., Clin. Cancer Res.
    Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov

  • CIViC: OSIMERTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Cho JH et al., 2020, Osimertinib for Patients With Non-Small-Cell Lung Cancer Harboring Uncommon EGFR Mutations: A Multicenter, Open-Label, Phase II Trial (KCSG-LU15-09)., J Clin Oncol
    Starrett JH et al., 2020, Drug Sensitivity and Allele Specificity of First-Line Osimertinib Resistance <i>EGFR</i> Mutations., Cancer Res
    Castellano GM et al., 2019, A Novel Acquired Exon 20 EGFR M766Q Mutation in Lung Adenocarcinoma Mediates Osimertinib Resistance but is Sensitive to Neratinib and Poziotinib., J Thorac Oncol

  • TTD: AZD9291

    • Version: 2020.06.01

    Alternate Names:
    D0RT2C TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3353410

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: osimertinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL3353410

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Osimertinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Osimertinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Osimertinib

    • Version: 4-Sep-2020

    Alternate Names:

    Drug Info:

    Publications:

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