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DACTOLISIB Drug Record

  • Summary
  • Interactions
  • Claims
  • DACTOLISIB chembl:CHEMBL1879463 Antineoplastic

    Alternate Names:

    NVP-BEZ235
    DACTOLISIB
    BEZ-235
    NVP-BEZ235-NX
    BEZ235

    Drug Info:

    Notes catalytic, dual PI3K/mTOR inhibitor
    Drug Class Kinase Inhibitors
    Pharmaceutical Developer Novartis
    Source Reported Drug Name(s) BEZ235
    Drug Class PI3K/mTOR dual Inhibitor
    (8 More Sources)

    Publications:

    Morales GA et al., 2013, Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors., J Med Chem
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol
    Wang et al., 2014, Activation of AR sensitizes breast carcinomas to NVP-BEZ235's therapeutic effect mediated by PTEN and KLLN upregulation., Mol. Cancer Ther.
    García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
    Lui et al., 2013, Frequent mutation of the PI3K pathway in head and neck cancer defines predictive biomarkers., Cancer Discov
    Engelman et al., 2008, Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers., Nat. Med.
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
    Depreeuw et al., 2015, Characterization of patient-derived tumor xenograft models of endometrial cancer for preclinical evaluation of targeted therapies., Gynecol. Oncol.
    Swick et al., 2017, Cotargeting mTORC and EGFR Signaling as a Therapeutic Strategy in HNSCC., Mol. Cancer Ther.
    Oishi et al., 2014, The PI3K/mTOR dual inhibitor NVP-BEZ235 reduces the growth of ovarian clear cell carcinoma., Oncol. Rep.
    Roper et al., 2011, The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer., PLoS ONE
    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.
    Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
    Mueller et al., 2012, Selective PI3K inhibition by BKM120 and BEZ235 alone or in combination with chemotherapy in wild-type and mutated human gastrointestinal cancer cell lines., Cancer Chemother. Pharmacol.
    Qu et al., 2014, Antitumor activity of selective MEK1/2 inhibitor AZD6244 in combination with PI3K/mTOR inhibitor BEZ235 in gefitinib-resistant NSCLC xenograft models., J. Exp. Clin. Cancer Res.
    Kim et al., 2013, Coexistent mutations of KRAS and PIK3CA affect the efficacy of NVP-BEZ235, a dual PI3K/MTOR inhibitor, in regulating the PI3K/MTOR pathway in colorectal cancer., Int. J. Cancer
    Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.
    Shoji et al., 2012, Genotype-dependent efficacy of a dual PI3K/mTOR inhibitor, NVP-BEZ235, and an mTOR inhibitor, RAD001, in endometrial carcinomas., PLoS ONE
    Eichhorn PJ et al., 2008, Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235., Cancer Res
    Migliardi et al., 2012, Inhibition of MEK and PI3K/mTOR suppresses tumor growth but does not cause tumor regression in patient-derived xenografts of RAS-mutant colorectal carcinomas., Clin. Cancer Res.
    Soares et al., 2015, Dual PI3K/mTOR Inhibitors Induce Rapid Overactivation of the MEK/ERK Pathway in Human Pancreatic Cancer Cells through Suppression of mTORC2., Mol. Cancer Ther.
    Raja et al., 2015, Assessment of the In Vivo Activity of PI3K and MEK Inhibitors in Genetically Defined Models of Colorectal Cancer., Mol. Cancer Ther.
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Jin et al., 2011, Synergistic action of a RAF inhibitor and a dual PI3K/mTOR inhibitor in thyroid cancer., Clin. Cancer Res.
  • DACTOLISIB   CRTC1

    Interaction Score: 0.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial

  • DACTOLISIB   CRTC2

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial

  • DACTOLISIB   MPL

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Ruxolitinib
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • DACTOLISIB   PIK3CA

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes
    Reported Cancer Type Melanoma

    PMIDs:
    23619167 19029981 26270481 26232337 28446642 24927217 26137449 21966435 26013318 26272063 23629727 27974663 22543857 24939055 23475782 26627007 22662154 19010894


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial

  • DACTOLISIB   PIK3R4

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • DACTOLISIB   PIK3R6

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome MyCancerGenomeClinicalTrial

  • DACTOLISIB   PIK3R1

    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:
    ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • DACTOLISIB   APC

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Binimetinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    26206338


    Sources:
    JAX-CKB

  • DACTOLISIB   PIK3R5

    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:
    MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • DACTOLISIB   PIK3R3

    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:
    MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • DACTOLISIB   KRAS

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    22392911 19029981 23629727 25673820 24939055 23475782 22662154 26272063 26232337 26206338


    Sources:
    JAX-CKB CIViC

  • DACTOLISIB   PIK3R2

    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 MyCancerGenomeClinicalTrial

  • DACTOLISIB   PTEN

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Selumetinib + BEZ235
    Indication/Tumor Type endometrial cancer
    Response Type sensitive

    PMIDs:
    28446642 27974663 26206338 22662154 26232337


    Sources:
    ClearityFoundationBiomarkers JAX-CKB

  • DACTOLISIB   PIK3C2A

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • DACTOLISIB   PIK3C3

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • DACTOLISIB   NEK2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   PIK3C2B

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • DACTOLISIB   PIK3C2G

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • DACTOLISIB   PIK3CD

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • DACTOLISIB   HRAS

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    21831957


    Sources:
    JAX-CKB

  • DACTOLISIB   PIK3CB

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

  • DACTOLISIB   MTOR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma
    Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor
    Direct Interaction yes

    PMIDs:
    23410005


    Sources:
    DTC MyCancerGenome ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial TTD

  • DACTOLISIB   ACVR1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   LIMK1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   PIK3CG

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial TTD

  • DACTOLISIB   CDK7

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   LTK

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   NRAS

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22392911


    Sources:
    CIViC

  • DACTOLISIB   LRRK2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Vemurafenib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    23549875 26137449


    Sources:
    JAX-CKB CIViC

  • DACTOLISIB   MAP4K2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   JAK2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Ruxolitinib
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • DACTOLISIB   FGFR3

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sorafenib + BEZ235
    Indication/Tumor Type urinary bladder cancer
    Response Type sensitive

    PMIDs:
    26270481


    Sources:
    JAX-CKB

  • DACTOLISIB   MAP4K5

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   CHEK1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   MET

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    24939055


    Sources:
    DTC JAX-CKB

  • DACTOLISIB   CSF1R

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   CLK4

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   ALK

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + BEZ235
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    24939055 23629727


    Sources:
    JAX-CKB

  • DACTOLISIB   AURKB

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   TP53

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type resistant
    Response Type decreased response
    Response Type sensitive

    PMIDs:
    26272063


    Sources:
    JAX-CKB

  • DACTOLISIB   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24356815


    Sources:
    CIViC

  • DACTOLISIB   NFE2L2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CancerCommons: BEZ235

    • Version: 25-July-2013

    Alternate Names:
    Dactolisib PubChem Drug Name
    11977753 PubChem Drug ID
    BEZ235 Drug Trade Name

    Drug Info:
    Drug Class PI3K/mTOR dual Inhibitor
    Source Reported Drug Name(s) BEZ235
    Pharmaceutical Developer Novartis

    Publications:

  • MyCancerGenome: BEZ235

    • Version: 20-Jun-2017

    Alternate Names:
    BEZ235 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors
    Notes catalytic, dual PI3K/mTOR inhibitor

    Publications:

  • DTC: DACTOLISIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1879463 ChEMBL Drug ID

    Drug Info:

    Publications:
    Morales GA et al., 2013, Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors., J Med Chem

  • JAX-CKB: BEZ235

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Jin et al., 2011, Synergistic action of a RAF inhibitor and a dual PI3K/mTOR inhibitor in thyroid cancer., Clin. Cancer Res.
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Qu et al., 2014, Antitumor activity of selective MEK1/2 inhibitor AZD6244 in combination with PI3K/mTOR inhibitor BEZ235 in gefitinib-resistant NSCLC xenograft models., J. Exp. Clin. Cancer Res.

  • CIViC: DACTOLISIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
    Wang et al., 2014, Activation of AR sensitizes breast carcinomas to NVP-BEZ235's therapeutic effect mediated by PTEN and KLLN upregulation., Mol. Cancer Ther.
    Migliardi et al., 2012, Inhibition of MEK and PI3K/mTOR suppresses tumor growth but does not cause tumor regression in patient-derived xenografts of RAS-mutant colorectal carcinomas., Clin. Cancer Res.

  • TALC: BEZ235

    • Version: 12-May-2016

    Alternate Names:
    BEZ235 Primary Drug Name
    BEZ235 Drug Synonym

    Drug Info:

    Publications:

  • TTD: BEZ235

    • Version: 2020.06.01

    Alternate Names:
    D0VG0D TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1879463

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: DACTOLISIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: NVP-BEZ235

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: NVP-BEZ235

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1879463

    • Version: chembl_23

    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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21