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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:

    Drug Categories acrylates
    FDA Approval Non-small cell lung cancer (with EGFR T790M mutation)
    Drug Class Kinase Inhibitor
    Drug Categories antineoplastic and immunomodulating agents
    Drug Categories breast cancer resistance protein inhibitors
    Drug Categories cytochrome p-450 cyp1a2 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp3a inhibitors
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp3a4 substrates
    Drug Categories cytochrome p-450 cyp3a4 substrates (strength unknown)
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories kinase inhibitor
    Drug Categories narrow therapeutic index drugs
    Drug Categories p-glycoprotein substrates
    Drug Categories tyrosine kinase inhibitors
    (10 More Sources)

    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
    Yosaatmadja et al., 2015, Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed., J. Struct. Biol.
    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
    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
    Niu et al., 2014, Novel agents and strategies for overcoming EGFR TKIs resistance., Exp Hematol Oncol
    Cross et al., 2014, AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer., Cancer Discov
    Mok et al., 2017, Osimertinib or Platinum-Pemetrexed in EGFR T790M-Positive Lung Cancer., N. Engl. J. Med.
    Jänne et al., 2015, AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer., N. Engl. J. Med.
    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.
    Greig, 2016, Osimertinib: First Global Approval., Drugs
    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.
    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.
    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
    Ercan et al., 2015, EGFR Mutations and Resistance to Irreversible Pyrimidine-Based 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
    Ortiz-Cuaran et al., 2016, Heterogeneous Mechanisms of Primary and Acquired Resistance to Third-Generation EGFR Inhibitors., Clin. Cancer Res.
    Thress et al., 2015, Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M., Nat. Med.
    Sequist et al., 2016, Osimertinib Responses After Disease Progression in Patients Who Had Been Receiving Rociletinib., JAMA 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.
    Moores et al., 2016, A Novel Bispecific Antibody Targeting EGFR and cMet Is Effective against EGFR Inhibitor-Resistant Lung Tumors., Cancer Res.
    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
    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.
    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: 2.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

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


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

  • OSIMERTINIB   MET

    Interaction Score: 0.77

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27694386 29386539 27393507 27252416


    Sources:
    OncoKB JAX-CKB CIViC CGI

  • OSIMERTINIB   NRAS

    Interaction Score: 0.47

    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: 0.25

    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: 0.22

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27252416


    Sources:
    JAX-CKB CGI

  • DrugBank: DB09330

    • Version: 5.1.7

    Alternate Names:
    OSIMERTINIB DrugBank Drug Name
    1421373-65-0 CAS Number
    Tagrisso Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories acids, acyclic

    Publications:
    Yosaatmadja et al., 2015, Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed., J. Struct. Biol.

  • 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

  • GuideToPharmacology: 223366052

    • Version: 29-September-2020

    Alternate Names:
    OSIMERTINIB GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • 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:

  • CGI: Osimertinib

    • Version: 27-September-2017

    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:

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