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PICTILISIB Drug Record

  • Summary
  • Interactions
  • Claims
  • PICTILISIB chembl:CHEMBL521851 Antineoplastic

    Alternate Names:

    GDC 0941
    CDC-0941
    PICTILISIB
    RG-7321
    GDC-0941

    Drug Info:

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

    Publications:

    Packer et al., 2017, PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers., Mol. Cancer Ther.
    Spoerke et al., 2012, Phosphoinositide 3-kinase (PI3K) pathway alterations are associated with histologic subtypes and are predictive of sensitivity to PI3K inhibitors in lung cancer preclinical models., Clin. Cancer Res.
    Potter et al., 2016, Inhibition of PI3K/BMX Cell Survival Pathway Sensitizes to BH3 Mimetics in SCLC., Mol. Cancer Ther.
    Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.
    Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov
    Haagensen et al., 2013, The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice., PLoS ONE
    Herrera-Abreu et al., 2016, Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor-Positive Breast Cancer., Cancer Res.
    de Lint et al., 2016, Sensitizing Triple-Negative Breast Cancer to PI3K Inhibition by Cotargeting IGF1R., Mol. Cancer Ther.
    Zheng et al., 2014, More antitumor efficacy of the PI3K inhibitor GDC-0941 in breast cancer with PIK3CA mutation or HER2 amplification status in vitro., Pharmazie
    Weigelt et al., 2013, PI3K pathway dependencies in endometrioid endometrial cancer cell lines., Clin. Cancer Res.
    Stratikopoulos et al., 2015, Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy., Cancer Cell
    Spoerke et al., 2016, Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant., Nat Commun
    Arjumand et al., 2016, Phosphatidyl inositol-3 kinase (PIK3CA) E545K mutation confers cisplatin resistance and a migratory phenotype in cervical cancer cells., Oncotarget
    Beaver et al., 2013, PIK3CA and AKT1 mutations have distinct effects on sensitivity to targeted pathway inhibitors in an isogenic luminal breast cancer model system., Clin. Cancer Res.
    Nacht M et al., 2013, Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα., J Med Chem
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Hoeflich et al., 2009, Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression., Cancer Res.
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Mahoney et al., 2009, LKB1/KRAS mutant lung cancers constitute a genetic subset of NSCLC with increased sensitivity to MAPK and mTOR signalling inhibition., Br. J. Cancer
    Qian et al., 2012, Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling., Clin. Cancer Res.
    Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
    Hofmann et al., 2012, K-RAS mutant pancreatic tumors show higher sensitivity to MEK than to PI3K inhibition in vivo., PLoS ONE
    Utermark et al., 2012, The p110α and p110β isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis., Genes Dev.
    Berger et al., 2014, Oncogenic RIT1 mutations in lung adenocarcinoma., Oncogene
    Cheng et al., 2014, A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition., Cancer Res.
    Vlietstra et al., 1998, Frequent inactivation of PTEN in prostate cancer cell lines and xenografts., Cancer Res.
    Yang et al., 2016, Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer., Clin. Cancer Res.
  • PICTILISIB   RIT1

    Interaction Score: 2.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24469055


    Sources:
    CIViC

  • PICTILISIB   MPL

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type sensitive
    combination therapy GDC-0941 + Ruxolitinib
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • PICTILISIB   PIK3CA

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy BGJ398 + GDC-0941
    combination therapy GDC-0941 + Linsitinib
    combination therapy GDC-0941 + NVP-AEW541

    PMIDs:
    28119489 23136191 27197306 22084396 27604488 24339963 27020857 27196766 24601221 23674493 26058079 27174596 27489350 23888070 23360348


    Sources:
    DTC MyCancerGenome JAX-CKB ChemblInteractions CIViC

  • PICTILISIB   PTEN

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + MS417
    Indication/Tumor Type breast cancer
    Response Type predicted – sensitive

    PMIDs:
    9661880 22693356 19276360 24265153 23136191 24322983 27020857 26577700 26733612 28119489 26058079


    Sources:
    JAX-CKB

  • PICTILISIB   RB1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Palbociclib + GDC-0941
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type no benefit

    PMIDs:
    27020857


    Sources:
    JAX-CKB

  • PICTILISIB   STK11

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    24322983


    Sources:
    JAX-CKB

  • PICTILISIB   PIK3C2G

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PICTILISIB   PIK3C2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PICTILISIB   PIK3C3

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PICTILISIB   PIK3C2B

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PICTILISIB   PIK3R6

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PICTILISIB   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

  • PICTILISIB   PIK3R4

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • PICTILISIB   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

  • PICTILISIB   PIK3R1

    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

  • PICTILISIB   PIK3R2

    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:
    MyCancerGenome ChemblInteractions

  • PICTILISIB   KRAS

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type myelodysplastic/myeloproliferative neoplasm
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    19165201 22693356 22084396 26725216 22952903


    Sources:
    JAX-CKB

  • PICTILISIB   CDK7

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PICTILISIB   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

  • PICTILISIB   LRRK2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PICTILISIB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC0879 + GDC-0941
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    26577700 24265153 19276360


    Sources:
    JAX-CKB

  • PICTILISIB   FGFR2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    28119489


    Sources:
    JAX-CKB

  • PICTILISIB   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

  • PICTILISIB   JAK2

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + Ruxolitinib
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • PICTILISIB   AKT1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27604488


    Sources:
    JAX-CKB

  • PICTILISIB   ERBB2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Palbociclib + GDC-0941
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive

    PMIDs:
    27020857 22802530


    Sources:
    JAX-CKB CIViC

  • PICTILISIB   MAPK8

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PICTILISIB   PIK3CG

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • PICTILISIB   CLK4

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PICTILISIB   YES1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MyCancerGenome: GDC-0941

    • Version: 20-Jun-2017

    Alternate Names:
    GDC-0941 Development Name

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

    Publications:

  • DTC: PICTILISIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL521851 ChEMBL Drug ID

    Drug Info:

    Publications:
    Nacht M et al., 2013, Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα., J Med Chem

  • JAX-CKB: GDC-0941

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Le et al., 2016, Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer., Cancer Discov
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Weigelt et al., 2013, PI3K pathway dependencies in endometrioid endometrial cancer cell lines., Clin. Cancer Res.

  • CIViC: PICTILISIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Utermark et al., 2012, The p110α and p110β isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis., Genes Dev.
    Berger et al., 2014, Oncogenic RIT1 mutations in lung adenocarcinoma., Oncogene
    Arjumand et al., 2016, Phosphatidyl inositol-3 kinase (PIK3CA) E545K mutation confers cisplatin resistance and a migratory phenotype in cervical cancer cells., Oncotarget

  • TALC: GDC-0941

    • Version: 12-May-2016

    Alternate Names:
    GDC-0941 Primary Drug Name
    GDC-0941 Drug Synonym

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL521851

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: GDC-0941

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL521851

    • 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.

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