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BUPARLISIB Drug Record

  • Summary
  • Interactions
  • Claims
  • BUPARLISIB chembl:CHEMBL2017974 Antineoplastic

    Alternate Names:

    NVP-BKM120
    BKM120-NX
    BKM-120NX
    BKM-120
    NVP-BKM-120
    BUPARLISIB
    BKM 120
    BKM120
    drugbank:11666
    chembl:CHEMBL2017974
    pubchem.compound:16654980
    chemidplus:944396-07-0

    Drug Info:

    Notes pan-PI3K inhibitor
    Drug Class Kinase Inhibitors
    Pharmaceutical Developer Novartis
    Source Reported Drug Name(s) BKM120
    Drug Class PI3K Inhibitor
    (6 More Sources)

    Publications:

    Roper et al., 2014, Combination PI3K/MEK inhibition promotes tumor apoptosis and regression in PIK3CA wild-type, KRAS mutant colorectal cancer., Cancer Lett.
    Vansteenkiste et al., 2015, Safety and Efficacy of Buparlisib (BKM120) in Patients with PI3K Pathway-Activated Non-Small Cell Lung Cancer: Results from the Phase II BASALT-1 Study., J Thorac Oncol
    Hong et al., 2016, Targeting the PI3K signaling pathway in KRAS mutant colon cancer., Cancer Med
    Park et al., 2012, NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations., Int. J. Oncol.
    Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
    Hanker et al., 2013, Mutant PIK3CA accelerates HER2-driven transgenic mammary tumors and induces resistance to combinations of anti-HER2 therapies., Proc. Natl. Acad. Sci. U.S.A.
    Saura et al., 2014, Phase Ib study of Buparlisib plus Trastuzumab in patients with HER2-positive advanced or metastatic breast cancer that has progressed on Trastuzumab-based therapy., Clin. Cancer Res.
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
    Bonelli et al., 2015, Inhibition of PI3K Pathway Reduces Invasiveness and Epithelial-to-Mesenchymal Transition in Squamous Lung Cancer Cell Lines Harboring PIK3CA Gene Alterations., Mol. Cancer Ther.
    Kodack et al., 2017, The brain microenvironment mediates resistance in luminal breast cancer to PI3K inhibition through HER3 activation., Sci Transl Med
    Wang et al., 2016, Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer., Oncotarget
    Wang et al., 2017, A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma., Eur. Urol.
    Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
    Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
    Hyman et al., 2015, Parallel phase Ib studies of two schedules of buparlisib (BKM120) plus carboplatin and paclitaxel (q21 days or q28 days) for patients with advanced solid tumors., Cancer Chemother. Pharmacol.
    Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., 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.
  • BUPARLISIB   PIK3CA

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma
    combination therapy Buparlisib + Fulvestrant
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    28119489 23940356 24470511 27974663 26013318 28539475 26715098 26909613 22159814 26098748


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CancerCommons TTD OncoKB

  • BUPARLISIB   PIK3CD

    Interaction Score: 0.22

    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 TTD

  • BUPARLISIB   PIK3C2B

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • BUPARLISIB   PIK3C2A

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • BUPARLISIB   PIK3C3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • BUPARLISIB   PIK3C2G

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • BUPARLISIB   PIK3R4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • BUPARLISIB   PIK3R5

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • BUPARLISIB   PIK3R6

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • BUPARLISIB   PIK3R3

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • BUPARLISIB   PTEN

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + Trastuzumab
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type predicted – sensitive

    PMIDs:
    26098748 28119489 24470511 25672916


    Sources:
    JAX-CKB CIViC

  • BUPARLISIB   PIK3R1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • BUPARLISIB   HRAS

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung squamous cell carcinoma
    Response Type no benefit
    Approval Status Preclinical - Cell culture

    PMIDs:
    26544513


    Sources:
    JAX-CKB

  • BUPARLISIB   PIK3CB

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions TTD

  • BUPARLISIB   PIK3R2

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • BUPARLISIB   NRAS

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Binimetinib + BKM120
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    27307593


    Sources:
    JAX-CKB

  • BUPARLISIB   FGFR2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BGJ398 + BKM120
    Indication/Tumor Type endometrial cancer
    Response Type sensitive

    PMIDs:
    28119489


    Sources:
    JAX-CKB

  • BUPARLISIB   KRAS

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + AG490
    Indication/Tumor Type stomach cancer
    Response Type sensitive

    PMIDs:
    24576621 26098748 26715098 22159814


    Sources:
    JAX-CKB

  • BUPARLISIB   PIK3CG

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions TTD

  • BUPARLISIB   ERBB2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + Bevacizumab
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive

    PMIDs:
    24470511 23948973 28539475 23940356


    Sources:
    JAX-CKB

  • BUPARLISIB   FGFR3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell line xenograft
    Response Type sensitive

    PMIDs:
    28108151


    Sources:
    JAX-CKB

  • BUPARLISIB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Binimetinib + BKM120
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    24265152 27307593


    Sources:
    JAX-CKB

  • BUPARLISIB   FGFR1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD4547 + BKM120
    Indication/Tumor Type transitional cell carcinoma
    Response Type sensitive

    PMIDs:
    28108151


    Sources:
    JAX-CKB

  • BUPARLISIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + Osimertinib
    Indication/Tumor Type lung cancer
    Response Type sensitive

    PMIDs:
    28416483


    Sources:
    JAX-CKB

  • CancerCommons: BKM120

    • Version: 25-July-2013

    Alternate Names:
    BKM120 PubChem Drug Name
    16654980 PubChem Drug ID
    BKM120 Drug Trade Name

    Drug Info:
    Drug Class PI3K Inhibitor
    Source Reported Drug Name(s) BKM120
    Pharmaceutical Developer Novartis

    Publications:

  • MyCancerGenome: BKM120

    • Version: 20-Jun-2017

    Alternate Names:
    BKM120 Development Name

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

    Publications:

  • JAX-CKB: BKM120

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Hong et al., 2016, Targeting the PI3K signaling pathway in KRAS mutant colon cancer., Cancer Med
    Park et al., 2012, NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations., Int. J. Oncol.
    Vansteenkiste et al., 2015, Safety and Efficacy of Buparlisib (BKM120) in Patients with PI3K Pathway-Activated Non-Small Cell Lung Cancer: Results from the Phase II BASALT-1 Study., J Thorac Oncol

  • CIViC: BUPARLISIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Hyman et al., 2015, Parallel phase Ib studies of two schedules of buparlisib (BKM120) plus carboplatin and paclitaxel (q21 days or q28 days) for patients with advanced solid tumors., Cancer Chemother. Pharmacol.

  • TTD: Buparlisib

    • Version: 2020.06.01

    Alternate Names:
    D01QSO TTD Drug ID

    Drug Info:

    Publications:

  • TALC: BUPARLISIB

    • Version: 12-May-2016

    Alternate Names:
    BUPARLISIB Primary Drug Name
    BUPARLISIB Drug Generic Name
    BKM120 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2017974

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2017974

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: BKM120

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Buparlisib

    • Version: 23-July-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