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CERITINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • CERITINIB chembl:CHEMBL2403108 ApprovedAntineoplastic

    Alternate Names:

    LDK378
    ZYKADIA
    NVP-LDK-378-NX
    CERITINIB
    LDK-378
    NVP-LDK378-NX
    ZYKADIA®
    N-{2-[(5-CHLORO-2-{[2-ISOPROPOXY-5-METHYL-4-(PIPERIDIN-4-YL)PHENYL]AMINO}PYRIMIDIN-4-YL)AMINO]PHENYL}PROPANE-2-SULFONAMIDE
    CÉRITINIB
    COMPOUND 15B [PMID 23742252]
    pubchem.compound:57379345
    rxcui:1535457
    drugbank:09063
    chembl:CHEMBL2403108
    chemidplus:1032900-25-6

    Drug Info:

    FDA Approval Non-small cell lung cancer (with ALK fusion)
    Drug Class Kinase Inhibitor
    Pharmaceutical Developer Novartis
    Source Reported Drug Name(s) LDK378
    Drug Class ALK Inhibitor
    Drug Class Kinase Inhibitors
    (12 More Sources)

    Publications:

    Chen J et al., 2013, LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor., J Med Chem
    Landi L et al., 2016, Ceritinib for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer., Expert Rev Clin Pharmacol
    Kanaan Z et al., 2015, Novel targeted therapies for resistant ALK-rearranged non-small-cell lung cancer: ceritinib and beyond., Onco Targets Ther
    Marsilje et al., 2013, Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials., J. Med. Chem.
    Galkin et al., 2007, Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK., Proc. Natl. Acad. Sci. U.S.A.
    Shaw et al., 2014, Ceritinib in ALK-rearranged non-small-cell lung cancer., N. Engl. J. Med.
    Morán et al., 2013, Targeting EML4-ALK driven non-small cell lung cancer (NSCLC)., Transl Lung Cancer Res
    Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget
    Kodityal et al., 2016, A novel acquired ALK F1245C mutation confers resistance to crizotinib in ALK-positive NSCLC but is sensitive to ceritinib., Lung Cancer
    Crystal et al., 2014, Patient-derived models of acquired resistance can identify effective drug combinations for cancer., Science
    Johung et al., 2016, Extended Survival and Prognostic Factors for Patients With ALK-Rearranged Non-Small-Cell Lung Cancer and Brain Metastasis., J. Clin. Oncol.
    Soria et al., 2017, First-line ceritinib versus platinum-based chemotherapy in advanced ALK-rearranged non-small-cell lung cancer (ASCEND-4): a randomised, open-label, phase 3 study., Lancet
    Crinò et al., 2016, Multicenter Phase II Study of Whole-Body and Intracranial Activity With Ceritinib in Patients With ALK-Rearranged Non-Small-Cell Lung Cancer Previously Treated With Chemotherapy and Crizotinib: Results From ASCEND-2., J. Clin. Oncol.
    Gainor et al., 2015, Progression-Free and Overall Survival in ALK-Positive NSCLC Patients Treated with Sequential Crizotinib and Ceritinib., Clin. Cancer Res.
    Friboulet et al., 2014, The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer., Cancer Discov
    Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.
    Gainor et al., 2016, Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer., Cancer Discov
    Ceccon et al., 2015, Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma., Mol. Cancer Res.
    Zhang et al., 2016, The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models., Clin. Cancer Res.
    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
    Katayama et al., 2014, Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib., Clin. Cancer Res.
    Sakamoto et al., 2011, CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant., Cancer Cell
    Choi et al., 2010, EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors., N. Engl. J. Med.
    Chen et al., 2014, Co-clinical trials demonstrate superiority of crizotinib to chemotherapy in ALK-rearranged non-small cell lung cancer and predict strategies to overcome resistance., Clin. Cancer Res.
    Kim et al., 2013, Heterogeneity of genetic changes associated with acquired crizotinib resistance in ALK-rearranged lung cancer., J Thorac Oncol
    Doebele et al., 2012, Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer., Clin. Cancer Res.
    Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med
    Mansfield et al., 2016, Chromoplectic TPM3-ALK rearrangement in a patient with inflammatory myofibroblastic tumor who responded to ceritinib after progression on crizotinib., Ann. Oncol.
    Yakirevich et al., 2016, Oncogenic ALK Fusion in Rare and Aggressive Subtype of Colorectal Adenocarcinoma as a Potential Therapeutic Target., Clin. Cancer Res.
    Amatu et al., 2015, Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer., Br. J. Cancer
    Ou et al., 2015, I1171 missense mutation (particularly I1171N) is a common resistance mutation in ALK-positive NSCLC patients who have progressive disease while on alectinib and is sensitive to ceritinib., Lung Cancer
    Kim et al., 2016, Activity and safety of ceritinib in patients with ALK-rearranged non-small-cell lung cancer (ASCEND-1): updated results from the multicentre, open-label, phase 1 trial., 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
    Shaw AT et al., 2017, Ceritinib versus chemotherapy in patients with ALK-rearranged non-small-cell lung cancer previously given chemotherapy and crizotinib (ASCEND-5): a randomised, controlled, open-label, phase 3 trial., Lancet Oncol
    Lovly et al., 2014, Rationale for co-targeting IGF-1R and ALK in ALK fusion-positive lung cancer., Nat. Med.
    Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.
    Lim et al., 2017, Open-Label, Multicenter, Phase II Study of Ceritinib in Patients With Non-Small-Cell Lung Cancer Harboring ROS1 Rearrangement., J. Clin. Oncol.
    Katayama R et al., 2015, P-glycoprotein Mediates Ceritinib Resistance in Anaplastic Lymphoma Kinase-rearranged Non-small Cell Lung Cancer., EBioMedicine
  • CERITINIB   EML4

    Interaction Score: 5.06

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26775591 25173427 24675041 27780853 25228534 27009859 27432227 26698910


    Sources:
    JAX-CKB

  • CERITINIB   ALK

    Interaction Score: 4.79

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Notes Specifically targets ALK translocations
    Reported Cancer Type Lung
    combination therapy Saracatinib + Ceritinib

    PMIDs:
    26582431 25945060 23742252 17185414 24670165 25806224 27009859 26775591 25394791 26438117 28126333 27432917 25724526 24675041 26698910 27432227 25421750 27780853 25749034 25228534 21575866 20979473 24327273 23344087 22235099 22277784 27742657 26933125 26633560 25736571 26973324 29650534 28602779


    Sources:
    TALC MyCancerGenome JAX-CKB ChemblInteractions DoCM COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

  • CERITINIB   NPM1

    Interaction Score: 1.61

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type anaplastic large cell lymphoma
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    27009859 25749034 25421750


    Sources:
    JAX-CKB

  • CERITINIB   TSSK1B

    Interaction Score: 1.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23837797


    Sources:
    DTC

  • CERITINIB   ROS1

    Interaction Score: 0.8

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26372962 28520527


    Sources:
    JAX-CKB CIViC

  • CERITINIB   IGF1R

    Interaction Score: 0.3

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23837797


    Sources:
    DTC

  • CERITINIB   MAP2K1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Ceritinib + Selumetinib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    25394791


    Sources:
    JAX-CKB

  • CERITINIB   SRC

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    25394791


    Sources:
    JAX-CKB

  • CERITINIB   INSR

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23837797


    Sources:
    DTC

  • CERITINIB   ABCB1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26870817


    Sources:
    CIViC

  • CERITINIB   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23837797


    Sources:
    DTC

  • MyCancerGenome: CERITINIB

    • Version: 20-Jun-2017

    Alternate Names:
    ZYKADIA Trade Name

    Drug Info:
    Drug Class Kinase Inhibitor
    FDA Approval Non-small cell lung cancer (with ALK fusion)

    Publications:

  • CancerCommons: LDK378

    • Version: 25-July-2013

    Alternate Names:
    LDK378 Drug Trade Name
    LDK378 Drug Development Name

    Drug Info:
    Drug Class ALK Inhibitor
    Source Reported Drug Name(s) LDK378
    Pharmaceutical Developer Novartis

    Publications:

  • MyCancerGenome: LDK378

    • Version: 20-Jun-2017

    Alternate Names:
    LDK378 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • DTC: CERITINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL2403108 ChEMBL Drug ID

    Drug Info:

    Publications:
    Chen J et al., 2013, LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor., J Med Chem

  • DoCM: CERITINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med
    Doebele et al., 2012, Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer., Clin. Cancer Res.
    Chen et al., 2014, Co-clinical trials demonstrate superiority of crizotinib to chemotherapy in ALK-rearranged non-small cell lung cancer and predict strategies to overcome resistance., Clin. Cancer Res.

  • JAX-CKB: Ceritinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget
    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
    Ceccon et al., 2015, Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma., Mol. Cancer Res.

  • PharmGKB: ceritinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Landi L et al., 2016, Ceritinib for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer., Expert Rev Clin Pharmacol
    Kanaan Z et al., 2015, Novel targeted therapies for resistant ALK-rearranged non-small-cell lung cancer: ceritinib and beyond., Onco Targets Ther

  • CIViC: CERITINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Kodityal et al., 2016, A novel acquired ALK F1245C mutation confers resistance to crizotinib in ALK-positive NSCLC but is sensitive to ceritinib., Lung Cancer
    Yakirevich et al., 2016, Oncogenic ALK Fusion in Rare and Aggressive Subtype of Colorectal Adenocarcinoma as a Potential Therapeutic Target., Clin. Cancer Res.
    Ou et al., 2015, I1171 missense mutation (particularly I1171N) is a common resistance mutation in ALK-positive NSCLC patients who have progressive disease while on alectinib and is sensitive to ceritinib., Lung Cancer

  • TTD: Ceritinib

    • Version: 2020.06.01

    Alternate Names:
    D04LVK TTD Drug ID

    Drug Info:

    Publications:

  • TALC: LDK378

    • Version: 12-May-2016

    Alternate Names:
    LDK378 Primary Drug Name
    LDK378 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2403108

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2403108

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: 1032900-25-6

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Ceritinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Ceritinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Ceritinib

    • 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