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PILARALISIB Drug Record

  • Summary
  • Interactions
  • Claims
  • PILARALISIB chembl:CHEMBL3360203 Antineoplastic

    Alternate Names:

    PILARALISIB
    SAR-245408
    XL147
    XL-147

    Drug Info:

    Notes pan-PI3K inhibitor
    Drug Class Kinase Inhibitors
    (5 More Sources)

    Publications:

    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
    Foster et al., 2015, The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models., Mol. Cancer Ther.
    Shapiro et al., 2014, Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
    Rexer et al., 2013, Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2., Clin. Cancer Res.
    Chakrabarty et al., 2013, Trastuzumab-resistant cells rely on a HER2-PI3K-FoxO-survivin axis and are sensitive to PI3K inhibitors., Cancer Res.
  • PILARALISIB   PIK3R1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions

  • PILARALISIB   STK11

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    25637314


    Sources:
    JAX-CKB

  • PILARALISIB   PIK3C2B

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PILARALISIB   PIK3C3

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PILARALISIB   PIK3C2G

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PILARALISIB   PIK3C2A

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PILARALISIB   PIK3CD

    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:
    MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions

  • PILARALISIB   PIK3R4

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PILARALISIB   PIK3R5

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • PILARALISIB   PIK3R6

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PILARALISIB   PIK3R3

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • PILARALISIB   PIK3R2

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • PILARALISIB   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    21216929 25637314 24166903


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions

  • PILARALISIB   PIK3CB

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • PILARALISIB   PIK3CG

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions TTD

  • PILARALISIB   PTEN

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type glioblastoma multiforme
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    25637314


    Sources:
    ClearityFoundationBiomarkers JAX-CKB

  • PILARALISIB   ERBB2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Trastuzumab + XL147
    Evidence Type Actionable
    Approval Status Preclinical

    PMIDs:
    23948973 23204226


    Sources:
    JAX-CKB CIViC

  • PILARALISIB   KRAS

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy XL147 + Carboplatin
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    21216929 25637314


    Sources:
    JAX-CKB

  • PILARALISIB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    25637314


    Sources:
    JAX-CKB

  • PILARALISIB   MET

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    25637314


    Sources:
    JAX-CKB

  • MyCancerGenome: XL147

    • Version: 20-Jun-2017

    Alternate Names:
    SAR245408 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors
    Notes pan-PI3K inhibitor

    Publications:

  • JAX-CKB: XL147

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Shapiro et al., 2014, Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
    Foster et al., 2015, The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models., Mol. Cancer Ther.
    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.

  • CIViC: PILARALISIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Chakrabarty et al., 2013, Trastuzumab-resistant cells rely on a HER2-PI3K-FoxO-survivin axis and are sensitive to PI3K inhibitors., Cancer Res.

  • TTD: XL147

    • Version: 2020.06.01

    Alternate Names:
    D03KAC TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL3360203

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL3360203

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: XL-147

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • TALC: XL147

    • Version: 12-May-2016

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: XL147

    • Version: 15-June-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