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ALECTINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • ALECTINIB chembl:CHEMBL1738797 ApprovedAntineoplastic

    Alternate Names:

    CH-5424802
    ALECENSA
    AF-802
    RO-5424802
    RO5424802
    ALECTINIB
    AF802
    CH5424802
    CH 5424802
    AF 802
    9-ETHYL-6,6-DIMETHYL-8-[4-(MORPHOLIN-4-YL)PIPERIDIN-1-YL]-11-OXO-6,11-DIHYDRO-5H-BENZO[B]CARBAZOLE-3-CARBONITRILE
    ALECENSA®
    pubchem.compound:49806720
    rxcui:1727455
    chemidplus:1256580-46-7
    chembl:CHEMBL1738797
    drugbank:11363

    Drug Info:

    Drug Class Kinase Inhibitors
    FDA Approval Non-small cell lung cancer (with ALK fusion)
    (7 More Sources)

    Publications:

    Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol
    Ou et al., 2014, Identification of a novel HIP1-ALK fusion variant in Non-Small-Cell Lung Cancer (NSCLC) and discovery of ALK I1171 (I1171N/S) mutations in two ALK-rearranged NSCLC patients with resistance to Alectinib., J Thorac Oncol
    Morán et al., 2013, Targeting EML4-ALK driven non-small cell lung cancer (NSCLC)., Transl Lung Cancer Res
    Sakamoto et al., 2011, CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant., Cancer Cell
    Lu et al., 2017, The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model., Cancer Lett.
    Kim et al., 2013, Heterogeneity of genetic changes associated with acquired crizotinib resistance in ALK-rearranged lung cancer., J Thorac Oncol
    Yoshimura et al., 2016, Antitumor activity of alectinib, a selective ALK inhibitor, in an ALK-positive NSCLC cell line harboring G1269A mutation: Efficacy of alectinib against ALK G1269A mutated cells., Cancer Chemother. Pharmacol.
    Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget
    Peters et al., 2017, Alectinib versus Crizotinib in Untreated ALK-Positive Non-Small-Cell Lung Cancer., N. Engl. J. Med.
    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
    Ou et al., 2016, Alectinib in Crizotinib-Refractory ALK-Rearranged Non-Small-Cell Lung Cancer: A Phase II Global Study., J. Clin. Oncol.
    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.
    Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.
    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.
    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
    Johnson et al., 2016, Identification of I1171N resistance mutation in ALK-positive non-small-cell lung cancer tumor sample and circulating tumor DNA., Lung Cancer
    Gainor et al., 2016, Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer., Cancer Discov
    Katayama et al., 2014, Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib., Clin. Cancer Res.
    Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med
    Yoshida et al., 2016, Rapid and dramatic response to alectinib in an anaplastic lymphoma kinase rearranged non-small-cell lung cancer patient who is critically ill., Anticancer Drugs
    Shaw et al., 2016, Alectinib in ALK-positive, crizotinib-resistant, non-small-cell lung cancer: a single-group, multicentre, phase 2 trial., Lancet Oncol.
    Seto et al., 2013, CH5424802 (RO5424802) for patients with ALK-rearranged advanced non-small-cell lung cancer (AF-001JP study): a single-arm, open-label, phase 1-2 study., Lancet Oncol.
    Gadgeel et al., 2014, Safety and activity of alectinib against systemic disease and brain metastases in patients with crizotinib-resistant ALK-rearranged non-small-cell lung cancer (AF-002JG): results from the dose-finding portion of a phase 1/2 study., Lancet Oncol.
    Fontana et al., 2015, Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK., Cancer 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
    Hida T et al., 2017, Alectinib versus crizotinib in patients with ALK-positive non-small-cell lung cancer (J-ALEX): an open-label, randomised phase 3 trial., Lancet
    Paik J et al., 2018, Alectinib: A Review in Advanced, ALK-Positive NSCLC., Drugs
    Tani et al., 2016, Activation of EGFR Bypass Signaling by TGFα Overexpression Induces Acquired Resistance to Alectinib in ALK-Translocated Lung Cancer Cells., Mol. Cancer Ther.
    Singhi et al., 2017, Identification of Targetable ALK Rearrangements in Pancreatic Ductal Adenocarcinoma., J Natl Compr Canc Netw
    Lin et al., 2016, Clinical Activity of Alectinib in Advanced RET-Rearranged Non-Small Cell Lung Cancer., J Thorac Oncol
  • ALECTINIB   EML4

    Interaction Score: 9.72

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23344087 26849637 26682573 25393796 21575866 28476735 25228534 27009859 27432227 26698910


    Sources:
    JAX-CKB

  • ALECTINIB   ALK

    Interaction Score: 5.89

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    25588040 25393796 25806224 21575866 28455243 23344087 26849637 27009859 28586279 28285684 26598747 26438117 26698910 25421750 25749034 27565911 27432227 25228534 22277784 26938871 26708155 23639470 25153538 25727400 29650534 28501140 30030733


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

  • ALECTINIB   NPM1

    Interaction Score: 2.52

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27009859 25749034 25421750


    Sources:
    JAX-CKB

  • ALECTINIB   SMAD4

    Interaction Score: 1.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type predicted – sensitive
    Approval Status Clinical Study

    PMIDs:
    28476735


    Sources:
    JAX-CKB

  • ALECTINIB   CDKN2A

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type predicted – sensitive
    Approval Status Clinical Study

    PMIDs:
    28476735


    Sources:
    JAX-CKB

  • ALECTINIB   RET

    Interaction Score: 0.43

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27544060


    Sources:
    JAX-CKB CIViC

  • ALECTINIB   FGFR1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type predicted – sensitive
    Approval Status Clinical Study

    PMIDs:
    28476735


    Sources:
    JAX-CKB

  • MyCancerGenome: CH5424802

    • Version: 20-Jun-2017

    Alternate Names:
    CH5424802 Development Name
    AF802 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • MyCancerGenome: ALECTINIB

    • Version: 20-Jun-2017

    Alternate Names:
    ALECENSA Trade Name

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

    Publications:

  • JAX-CKB: Alectinib

    • 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: alectinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

  • CIViC: ALECTINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Paik J et al., 2018, Alectinib: A Review in Advanced, ALK-Positive NSCLC., Drugs
    Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med
    Yoshida et al., 2016, Rapid and dramatic response to alectinib in an anaplastic lymphoma kinase rearranged non-small-cell lung cancer patient who is critically ill., Anticancer Drugs

  • TTD: Alectinib

    • Version: 2020.06.01

    Alternate Names:
    D0U3SY TTD Drug ID

    Drug Info:

    Publications:

  • TALC: CHS424802

    • Version: 12-May-2016

    Alternate Names:
    CHS424802 Primary Drug Name
    CHS424802 Drug Synonym
    AF802 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1738797

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Alectinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Alectinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Alectinib

    • 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