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ALPELISIB Drug Record

  • Summary
  • Interactions
  • Claims
  • ALPELISIB chembl:CHEMBL2396661 ApprovedAntineoplastic

    Alternate Names:

    PIQRAY
    NVP-BYL719
    BYL-719
    ALPELISIB
    BYL719
    BYL 719
    chembl:CHEMBL2396661
    chemidplus:1217486-61-7
    pubchem.compound:56649450

    Drug Info:

    Pharmaceutical Developer Novartis
    Source Reported Drug Name(s) BYL719
    Drug Class PI3K/mTOR dual Inhibitor
    Drug Class Kinase Inhibitors
    (10 More Sources)

    Publications:

    Fritsch et al., 2014, Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials., Mol. Cancer Ther.
    André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
    Castel et al., 2016, PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition., Cancer Cell
    Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.
    Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
    Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov
    Fernandes MS et al., 2016 Oct 18, Specific inhibition of p110α subunit of PI3K: putative therapeutic strategy for KRAS mutant colorectal cancers., Oncotarget
    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.
    Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.
    Chen IC et al., 2017, Phosphatidylinositol-3 Kinase Inhibitors, Buparlisib and Alpelisib, Sensitize Estrogen Receptor-positive Breast Cancer Cells to Tamoxifen., Sci Rep
    Yang X et al., 2017, New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kα Complexed with a Potent Lead Compound., Sci Rep
    Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.
    Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
    Schwartz et al., 2015, Feedback suppression of PI3Kα signaling in PTEN-mutated tumors is relieved by selective inhibition of PI3Kβ., Cancer Cell
    Juric et al., 2015, Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor., Nature
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
    Costa et al., 2015, Discovery and functional characterization of a neomorphic PTEN mutation., Proc. Natl. Acad. Sci. U.S.A.
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
  • ALPELISIB   PI4KA

    Interaction Score: 1.87

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ALPELISIB   SGK1

    Interaction Score: 1.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27451907


    Sources:
    CIViC

  • ALPELISIB   PIK3CA

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type no benefit
    combination therapy Alpelisib + WEHI-539
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    24608574 31091374 27974663 27451907 27126994 28119489 27604488 27602501 26013318 26627007 28852212 29109464


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

  • ALPELISIB   PIK3R6

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   PIK3R4

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   PTEN

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type prostate cancer
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    25544636 25409150 27604488 26577700 28119489 26504226


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC

  • ALPELISIB   PIK3R1

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   RB1

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25002028


    Sources:
    CIViC

  • ALPELISIB   BRAF

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Alpelisib + PLX4720
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    27659046 27924459 28363909 26577700 27312529


    Sources:
    JAX-CKB CIViC

  • ALPELISIB   CDK4

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25002028


    Sources:
    CIViC

  • ALPELISIB   PIK3C3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • ALPELISIB   PIK3C2G

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • ALPELISIB   PIK3C2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • ALPELISIB   PIK3C2B

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • ALPELISIB   PIK3R5

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   PIK3R3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   PIK3R2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   PIK3CD

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   NRAS

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    24569456


    Sources:
    JAX-CKB

  • ALPELISIB   MAP2K1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • ALPELISIB   FGFR2

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    28119489


    Sources:
    JAX-CKB

  • ALPELISIB   PIK3CB

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   KRAS

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    27659046 27602501 24608574 27312529


    Sources:
    JAX-CKB

  • ALPELISIB   HRAS

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BYL719 + MEK162
    Indication/Tumor Type ovarian cancer
    Response Type predicted – sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • ALPELISIB   AKT1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type breast cancer
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    27604488


    Sources:
    JAX-CKB

  • ALPELISIB   FGFR1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Indication/Tumor Type estrogen-receptor positive breast cancer

    PMIDs:
    27126994


    Sources:
    JAX-CKB

  • ALPELISIB   PIK3CG

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • ALPELISIB   ESR2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ALPELISIB   FGFR3

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BGJ398 + BYL719
    Indication/Tumor Type transitional cell carcinoma
    Response Type predicted – sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • ALPELISIB   ERBB2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • ALPELISIB   ESR1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • ALPELISIB   MTOR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Lung

    PMIDs:
    None found


    Sources:
    CancerCommons

  • ALPELISIB   TP53

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ABT-263 + Alpelisib + CGM097 + Trametinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    27659046


    Sources:
    JAX-CKB

  • MyCancerGenome: BYL719

    • Version: 20-Jun-2017

    Alternate Names:
    BYL719 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors

    Publications:

  • CancerCommons: BYL719

    • Version: 25-July-2013

    Alternate Names:
    BYL719 PubChem Drug Name
    56649450 PubChem Drug ID
    BYL719 Drug Trade Name

    Drug Info:
    Drug Class PI3K/mTOR dual Inhibitor
    Source Reported Drug Name(s) BYL719
    Pharmaceutical Developer Novartis

    Publications:

  • JAX-CKB: BYL719

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

  • JAX-CKB: Alpelisib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
    Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.
    Castel et al., 2016, PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition., Cancer Cell

  • CIViC: ALPELISIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
    André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med
    Fritsch et al., 2014, Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials., Mol. Cancer Ther.

  • TTD: BYL719

    • Version: 2020.06.01

    Alternate Names:
    D0W7HE TTD Drug ID

    Drug Info:

    Publications:

  • FDA: Alpelisib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2396661

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: BYL719

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: BYL719

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: BYL719

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL2396661

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: alpelisib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Alpelisib

    • 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