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LORLATINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • LORLATINIB chembl:CHEMBL3286830 ApprovedAntineoplastic

    Alternate Names:

    LORBRENA
    LORLATINIB
    PF-06463922
    PF-6463922
    chemidplus:1454846-35-5
    pubchem.compound:71731823
    drugbank:12130
    chembl:CHEMBL3286830

    Drug Info:

    (5 More Sources)

    Publications:

    Ou et al., 2017, Dual occurrence of ALK G1202R solvent front mutation and small cell lung cancer transformation as resistance mechanisms to second generation ALK inhibitors without prior exposure to crizotinib. Pitfall of solely relying on liquid re-biopsy?, Lung Cancer
    Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.
    Infarinato et al., 2016, The ALK/ROS1 Inhibitor PF-06463922 Overcomes Primary Resistance to Crizotinib in ALK-Driven Neuroblastoma., Cancer Discov
    Mologni et al., 2015, NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922., Oncotarget
    Zou et al., 2015, PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models., Cancer Cell
    Gainor et al., 2016, Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer., Cancer Discov
    Solomon BJ et al., 2018, Lorlatinib in patients with ALK-positive non-small-cell lung cancer: results from a global phase 2 study., Lancet Oncol
    Yoda S et al., 2018, Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound <i>ALK</i> Mutations in ALK-Positive Lung Cancer., Cancer Discov
    Davare MA et al., 2018, Rare but Recurrent ROS1 Fusions Resulting From Chromosome 6q22 Microdeletions are Targetable Oncogenes in Glioma., Clin Cancer Res
    Zou et al., 2015, PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations., Proc. Natl. Acad. Sci. U.S.A.
    Facchinetti F et al., 2016, Crizotinib-Resistant ROS1 Mutations Reveal a Predictive Kinase Inhibitor Sensitivity Model for ROS1- and ALK-Rearranged Lung Cancers., Clin Cancer Res
  • LORLATINIB   EML4

    Interaction Score: 5.15

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26554404 26144315 27432227 26698910


    Sources:
    JAX-CKB

  • LORLATINIB   ROS1

    Interaction Score: 2.94

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    30171048 25733882 27401242


    Sources:
    JAX-CKB CIViC PharmGKB TTD FDA

  • LORLATINIB   ALK

    Interaction Score: 2.86

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Approval Status Preclinical - Cell line xenograft
    Response Type conflicting
    Indication/Tumor Type lung cancer

    PMIDs:
    28285684 26698910 26554404 25749034 26144315 27432227 30413378 29650534


    Sources:
    JAX-CKB COSMIC CIViC PharmGKB TTD FDA OncoKB

  • LORLATINIB   NPM1

    Interaction Score: 1.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    25749034


    Sources:
    JAX-CKB

  • LORLATINIB   RB1

    Interaction Score: 0.94

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung small cell carcinoma
    Response Type predicted – resistant
    Approval Status Clinical Study

    PMIDs:
    28285684


    Sources:
    JAX-CKB

  • LORLATINIB   TP53

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung small cell carcinoma
    Response Type predicted – resistant
    Approval Status Clinical Study

    PMIDs:
    28285684


    Sources:
    JAX-CKB

  • JAX-CKB: PF-06463922

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Ou et al., 2017, Dual occurrence of ALK G1202R solvent front mutation and small cell lung cancer transformation as resistance mechanisms to second generation ALK inhibitors without prior exposure to crizotinib. Pitfall of solely relying on liquid re-biopsy?, Lung Cancer
    Gainor et al., 2016, Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer., Cancer Discov
    Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.

  • CIViC: LORLATINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Solomon BJ et al., 2018, Lorlatinib in patients with ALK-positive non-small-cell lung cancer: results from a global phase 2 study., Lancet Oncol
    Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.
    Yoda S et al., 2018, Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound <i>ALK</i> Mutations in ALK-Positive Lung Cancer., Cancer Discov

  • TTD: Lorlatinib

    • Version: 2020.06.01

    Alternate Names:
    D0AF6O TTD Drug ID

    Drug Info:

    Publications:

  • TTD: PF-06463922

    • Version: 2020.06.01

    Alternate Names:
    D04DYC TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3286830

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Lorlatinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: lorlatinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Lorlatinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Lorlatinib

    • 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