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OMIPALISIB Drug Record

  • Summary
  • Interactions
  • Claims
  • OMIPALISIB chembl:CHEMBL1236962 Antineoplastic

    Alternate Names:

    OMIPALISIB
    GSK2126458

    Drug Info:

    (4 More Sources)

    Publications:

    Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
    Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.
    Munster et al., 2016, First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies., Clin. Cancer Res.
    Khalili et al., 2012, Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner., Clin. Cancer Res.
  • OMIPALISIB   GNAQ

    Interaction Score: 0.5

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GSK2126458 + Trametinib
    Indication/Tumor Type uveal melanoma
    Response Type sensitive

    PMIDs:
    22733540


    Sources:
    JAX-CKB

  • OMIPALISIB   PIK3R1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   NRAS

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type decreased response
    Approval Status Preclinical

    PMIDs:
    23431193 22389471


    Sources:
    JAX-CKB CIViC

  • OMIPALISIB   PIK3CD

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3R6

    Interaction Score: 0.2

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3R4

    Interaction Score: 0.2

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3R3

    Interaction Score: 0.2

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3R5

    Interaction Score: 0.2

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction PI3-kinase class I inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3R2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   AKT2

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • OMIPALISIB   AKT3

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • OMIPALISIB   MAP2K1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type conflicting
    Response Type no benefit
    combination therapy GSK2126458 + Trametinib

    PMIDs:
    22389471


    Sources:
    JAX-CKB

  • OMIPALISIB   PIK3CB

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3CA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Phase I
    Response Type no benefit

    PMIDs:
    26603258


    Sources:
    ClearityFoundationBiomarkers JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

  • OMIPALISIB   PIK3CG

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial TTD

  • OMIPALISIB   BRAF

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + GSK2126458
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    22389471


    Sources:
    JAX-CKB

  • OMIPALISIB   AKT1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • OMIPALISIB   PTEN

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers

  • OMIPALISIB   MTOR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • JAX-CKB: GSK2126458

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
    Khalili et al., 2012, Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner., Clin. Cancer Res.
    Munster et al., 2016, First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies., Clin. Cancer Res.

  • CIViC: OMIPALISIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.

  • TTD: GSK2126458

    • Version: 2020.06.01

    Alternate Names:
    D03EZE TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1236962

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: GSK2126458

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: GSK2126458

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1236962

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: GSK2126458

    • Version: 26-July-2013

    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