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PIK3CA Gene Record

  • Summary
  • Interactions
  • Claims
  • PIK3CA 5290 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    5290
    PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT ALPHA
    PIK3CA
    CLOVE
    CWS5
    MCAP
    MCM
    MCMTC
    PI3K
    PI3K-alpha
    p110-alpha
    171834
    8975
    ENSG00000121879
    OTTHUMG00000157311
    5289
    P42336
    PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT, ALPHA ISOFORM (EC 2.7.1.153) (PI3-KINASE P110 SUBUNIT ALPHA) (PTDINS- 3-KINASE P110) (PI3K). [SOURCE:UNIPROT/SWISSPROT;ACC:P42336]
    37
    PA33308
    Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
    Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha
    Phosphoinositide-3-kinase catalytic alpha polypeptide
    Serine/threonine protein kinase PIK3CA
    PI3-kinase subunit alpha
    PI3Kalpha
    PtdIns-3-kinase subunit alpha
    PtdIns-3-kinase subunit p110-alpha
    p110alpha
    PK3CA_HUMAN
    PI3-kinase alpha
    T80276
    CLAPO
    CCM4

    Gene Info:

    CancerCommons Reported Gene Name PI3K
    CancerCommons Reported Gene Name PI3K/mTOR
    Human Readable Name DRUGGABLE GENOME
    Target Class Enzymes
    Target Subclass EC:2.7.1.153
    Interpro Short Name PI3/4_kinase_cat_dom
    Human Readable Name PHOSPHATIDYLINOSITOL 3 KINASE
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR000403
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Interpro Name Phosphatidylinositol 3-/4-kinase, catalytic domain
    Gene Biotype PROTEIN_CODING
    (22 More Sources)

    Gene Categories: Category Details

    KINASE
    SERINE THREONINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    PHOSPHATIDYLINOSITOL 3 KINASE
    CLINICALLY ACTIONABLE

    Publications:

    Wang et al., 2016, Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer., Oncotarget
    Sabbah DA et al., 2012, Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases., Bioorg Med Chem Lett
    de Lint et al., 2016, Sensitizing Triple-Negative Breast Cancer to PI3K Inhibition by Cotargeting IGF1R., Mol. Cancer Ther.
    Juric et al., 2017, A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies., Clin. Cancer Res.
    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
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol
    Shiver et al., 2015, Response to Idelalisib in a Patient with Stage IV Merkel-Cell Carcinoma., N. Engl. J. Med.
    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.
    Kodack et al., 2017, The brain microenvironment mediates resistance in luminal breast cancer to PI3K inhibition through HER3 activation., Sci Transl Med
    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
    Potter et al., 2016, Inhibition of PI3K/BMX Cell Survival Pathway Sensitizes to BH3 Mimetics in SCLC., Mol. Cancer Ther.
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
    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.
    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.
    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.
    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
    Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov
    Lopez et al., 2015, Dual HER2/PIK3CA Targeting Overcomes Single-Agent Acquired Resistance in HER2-Amplified Uterine Serous Carcinoma Cell Lines In Vitro and In Vivo., Mol. Cancer Ther.
    Kashiyama et al., 2014, Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423., PLoS ONE
    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.
    Gökmen-Polar et al., 2012, Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models., Breast Cancer Res. Treat.
    Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget
    De Roock et al., 2010, Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis., Lancet Oncol.
    Sartore-Bianchi et al., 2009, PIK3CA mutations in colorectal cancer are associated with clinical resistance to EGFR-targeted monoclonal antibodies., Cancer Res.
    Xu et al., 2017, PIK3CA Mutations Contribute to Acquired Cetuximab Resistance in Patients with Metastatic Colorectal Cancer., Clin. Cancer Res.
    Souglakos J et al., 2009, Prognostic and predictive value of common mutations for treatment response and survival in patients with metastatic colorectal cancer., Br J Cancer
    Swick et al., 2017, Cotargeting mTORC and EGFR Signaling as a Therapeutic Strategy in HNSCC., Mol. Cancer Ther.
    Ciardiello et al., 2016, Cetuximab continuation after first progression in metastatic colorectal cancer (CAPRI-GOIM): a randomized phase II trial of FOLFOX plus cetuximab versus FOLFOX., Ann. Oncol.
    Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
    de la Rochefordiere et al., 2015, PIK3CA Pathway Mutations Predictive of Poor Response Following Standard Radiochemotherapy ± Cetuximab in Cervical Cancer Patients., Clin. Cancer Res.
    Hechtman et al., 2015, AKT1 E17K in Colorectal Carcinoma Is Associated with BRAF V600E but Not MSI-H Status: A Clinicopathologic Comparison to PIK3CA Helical and Kinase Domain Mutants., Mol. Cancer Res.
    Hong et al., 2012, A multicenter phase I trial of PX-866, an oral irreversible phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
    Ziemke et al., 2016, Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6., Clin. Cancer Res.
    Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
    Powles et al., 2016, Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma., J. Clin. Oncol.
    Dolly et al., 2016, Phase I Study of Apitolisib (GDC-0980), Dual Phosphatidylinositol-3-Kinase and Mammalian Target of Rapamycin Kinase Inhibitor, in Patients with Advanced Solid Tumors., Clin. Cancer Res.
    Wallin et al., 2011, GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway., Mol. Cancer Ther.
    Ribas et al., 2015, AKT Antagonist AZD5363 Influences Estrogen Receptor Function in Endocrine-Resistant Breast Cancer and Synergizes with Fulvestrant (ICI182780) In Vivo., Mol. Cancer Ther.
    Li et al., 2013, The AKT inhibitor AZD5363 is selectively active in PI3KCA mutant gastric cancer, and sensitizes a patient-derived gastric cancer xenograft model with PTEN loss to Taxotere., J Transl Med
    Yoon et al., 2009, Combination of EGFR and MEK1/2 inhibitor shows synergistic effects by suppressing EGFR/HER3-dependent AKT activation in human gastric cancer cells., Mol. Cancer Ther.
    Davies et al., 2012, Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background., Mol. Cancer Ther.
    Hyman et al., 2017, AKT Inhibition in Solid Tumors With AKT1 Mutations., J. Clin. Oncol.
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
    Baselga et al., 2016, Relationship between Tumor Biomarkers and Efficacy in EMILIA, a Phase III Study of Trastuzumab Emtansine in HER2-Positive Metastatic Breast Cancer., Clin. Cancer Res.
    Guarneri et al., 2015, Prospective Biomarker Analysis of the Randomized CHER-LOB Study Evaluating the Dual Anti-HER2 Treatment With Trastuzumab and Lapatinib Plus Chemotherapy as Neoadjuvant Therapy for HER2-Positive Breast Cancer., Oncologist
    Loibl S et al., 2014, PIK3CA mutations are associated with lower rates of pathologic complete response to anti-human epidermal growth factor receptor 2 (her2) therapy in primary HER2-overexpressing breast cancer., J Clin Oncol
    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
    Yamaguchi et al., 2016, A synthetic-lethality RNAi screen reveals an ERK-mTOR co-targeting pro-apoptotic switch in PIK3CA+ oral cancers., Oncotarget
    Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
    Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE
    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.
    Smith et al., 2016, Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth., Mol. Cancer Ther.
    Lopez et al., 2014, Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo., Gynecol. Oncol.
    Ndubaku et al., 2013, Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity., J. Med. Chem.
    Zumsteg et al., 2016, Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations., Clin. Cancer Res.
    Juric et al., 2017, Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors., Cancer Discov
    Avellino et al., 2005, Rapamycin stimulates apoptosis of childhood acute lymphoblastic leukemia cells., Blood
    Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
    Engelman et al., 2008, Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers., Nat. Med.
    Kang et al., 2005, Phosphatidylinositol 3-kinase mutations identified in human cancer are oncogenic., Proc. Natl. Acad. Sci. U.S.A.
    Gymnopoulos et al., 2007, Rare cancer-specific mutations in PIK3CA show gain of function., Proc. Natl. Acad. Sci. U.S.A.
    Hart et al., 2013, VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer., Mol. Cancer Ther.
    Janakiraman et al., 2010, Genomic and biological characterization of exon 4 KRAS mutations in human cancer., Cancer Res.
    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.
    Munster et al., 2016, First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies., Clin. Cancer Res.
    Ludovini V et al., 2011, Phosphoinositide-3-kinase catalytic alpha and KRAS mutations are important predictors of resistance to therapy with epidermal growth factor receptor tyrosine kinase inhibitors in patients with advanced non-small cell lung cancer., J Thorac Oncol
    Depreeuw et al., 2015, Characterization of patient-derived tumor xenograft models of endometrial cancer for preclinical evaluation of targeted therapies., Gynecol. Oncol.
    Weigelt et al., 2011, PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs., Oncogene
    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.
    Holt et al., 2012, Enhanced apoptosis and tumor growth suppression elicited by combination of MEK (selumetinib) and mTOR kinase inhibitors (AZD8055)., Cancer Res.
    Blagden et al., 2014, First-in-human study of CH5132799, an oral class I PI3K inhibitor, studying toxicity, pharmacokinetics, and pharmacodynamics, in patients with metastatic cancer., Clin. Cancer Res.
    Tanaka et al., 2011, The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations., Clin. Cancer Res.
    Liu et al., 2009, Genetic alterations in the phosphoinositide 3-kinase/Akt signaling pathway confer sensitivity of thyroid cancer cells to therapeutic targeting of Akt and mammalian target of rapamycin., Cancer Res.
    Athuluri-Divakar et al., 2016, A Small Molecule RAS-Mimetic Disrupts RAS Association with Effector Proteins to Block Signaling., Cell
    Anderson et al., 2013, The dual pathway inhibitor rigosertib is effective in direct patient tumor xenografts of head and neck squamous cell carcinomas., Mol. Cancer Ther.
    Patnaik et al., 2016, First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas., Ann. Oncol.
    Liu et al., 2013, BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models., Mol. Cancer Ther.
    Venkatesan et al., 2010, PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor., Bioorg. Med. Chem. Lett.
    Yuan et al., 2011, PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity., Mol. Cancer Ther.
    Westfall et al., 2005, Inhibition of phosphatidylinositol 3-kinase sensitizes ovarian cancer cells to carboplatin and allows adjunct chemotherapy treatment., Mol. Cancer Ther.
    Tenzer et al., 2001, The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C., Cancer Res.
    Angeloni et al., 2007, Role of quercetin and its in vivo metabolites in protecting H9c2 cells against oxidative stress., Biochimie
    Jalota-Badhwar et al., 2015, P7170: A Novel Molecule with Unique Profile of mTORC1/C2 and Activin Receptor-like Kinase 1 Inhibition Leading to Antitumor and Antiangiogenic Activity., Mol. Cancer Ther.
    Ambrogio et al., 2016, Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma., Nat. Med.
    Witters et al., 2004, Combining flavopiridol with various signal transduction inhibitors., Oncol. Rep.
    Ciprés et al., 1999, An IL-2 receptor beta subdomain that controls Bcl-X(L) expression and cell survival., Eur. J. Immunol.
    Liao X et al., 2012, Aspirin use, tumor PIK3CA mutation, and colorectal-cancer survival., N Engl J Med
    Hedberg ML et al., 2019, Use of nonsteroidal anti-inflammatory drugs predicts improved patient survival for <i>PIK3CA</i>-altered head and neck cancer., J Exp Med
    Basho et al., 2017, Targeting the PI3K/AKT/mTOR Pathway for the Treatment of Mesenchymal Triple-Negative Breast Cancer: Evidence From a Phase 1 Trial of mTOR Inhibition in Combination With Liposomal Doxorubicin and Bevacizumab., JAMA Oncol
    Falchook et al., 2015, Dual antiangiogenic inhibition: a phase I dose escalation and expansion trial targeting VEGF-A and VEGFR in patients with advanced solid tumors., Invest New Drugs
    Razis E et al., 2011, Evaluation of the association of PIK3CA mutations and PTEN loss with efficacy of trastuzumab therapy in metastatic breast cancer., Breast Cancer Res Treat
    O'Brien et al., 2010, Predictive biomarkers of sensitivity to the phosphatidylinositol 3' kinase inhibitor GDC-0941 in breast cancer preclinical models., Clin. Cancer Res.
    Chuang et al., 2017, ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies., J Thorac Oncol
    Wang et al., 2011, PI3K pathway activation results in low efficacy of both trastuzumab and lapatinib., BMC Cancer
    Berns et al., 2007, A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer., Cancer Cell
    Ballou et al., 2007, Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one., J. Biol. Chem.
    Mohan et al., 2015, MEK Inhibitor PD-0325901 Overcomes Resistance to PI3K/mTOR Inhibitor PF-5212384 and Potentiates Antitumor Effects in Human Head and Neck Squamous Cell Carcinoma., Clin. Cancer Res.
    D'Amato et al., 2014, The dual PI3K/mTOR inhibitor PKI-587 enhances sensitivity to cetuximab in EGFR-resistant human head and neck cancer models., Br. J. Cancer
    Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis
    Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
    Hollestelle et al., 2007, Phosphatidylinositol-3-OH kinase or RAS pathway mutations in human breast cancer cell lines., Mol. Cancer Res.
    Song et al., 2015, Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1-Rearranged Non-Small Cell Lung Cancer., Clin. Cancer Res.
    Lui et al., 2013, Frequent mutation of the PI3K pathway in head and neck cancer defines predictive biomarkers., Cancer Discov
    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
    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
    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.
    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
    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
    Simoncini et al., 2002, Nongenomic mechanisms of endothelial nitric oxide synthase activation by the selective estrogen receptor modulator raloxifene., Circulation
    André et al., 2016, Molecular Alterations and Everolimus Efficacy in Human Epidermal Growth Factor Receptor 2-Overexpressing Metastatic Breast Cancers: Combined Exploratory Biomarker Analysis From BOLERO-1 and BOLERO-3., J. Clin. Oncol.
    Di Nicolantonio et al., 2010, Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus., J. Clin. Invest.
    Mohseni et al., 2010, PIK3CA and KRAS mutations predict for response to everolimus therapy: now that's RAD001., J. Clin. Invest.
    Bhattacharya et al., 2012, Pharmacologic synergy between dual phosphoinositide-3-kinase and mammalian target of rapamycin inhibition and 5-fluorouracil in PIK3CA mutant gastric cancer cells., Cancer Biol. Ther.
    Grünwald et al., 2015, TEMHEAD: a single-arm multicentre phase II study of temsirolimus in platin- and cetuximab refractory recurrent and/or metastatic squamous cell carcinoma of the head and neck (SCCHN) of the German SCCHN Group (AIO)., Ann. Oncol.
    Liu et al., 2011, The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathway., J. Clin. Endocrinol. Metab.
    Janku et al., 2012, PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations., J. Clin. Oncol.
    Fleming et al., 2012, Phase II trial of temsirolimus in patients with metastatic breast cancer., Breast Cancer Res. Treat.
    Myers et al., 2016, Tumor mutational analysis of GOG248, a phase II study of temsirolimus or temsirolimus and alternating megestrol acetate and tamoxifen for advanced endometrial cancer (EC): An NRG Oncology/Gynecologic Oncology Group study., Gynecol. Oncol.
    Lee et al., 2006, Interplay between PI3K/Akt and MAPK signaling pathways in DNA-damaging drug-induced apoptosis., Biochim. Biophys. Acta
    Knuefermann et al., 2003, HER2/PI-3K/Akt activation leads to a multidrug resistance in human breast adenocarcinoma cells., Oncogene
    Yip-Schneider et al., Inhibition of the phosphatidylinositol 3'-kinase signaling pathway increases the responsiveness of pancreatic carcinoma cells to sulindac., J. Gastrointest. Surg.
    Muscarella et al., 2003, Cross-linking of surface IgM in the Burkitt's lymphoma cell line ST486 provides protection against arsenite- and stress-induced apoptosis that is mediated by ERK and phosphoinositide 3-kinase signaling pathways., J. Biol. Chem.
    Mallon et al., 2010, Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor., Mol. Cancer Ther.
    Yousif et al., Phosphoinositide 3-kinase mediated signalling contributes to development of diabetes-induced abnormal vascular reactivity of rat carotid artery., Cell Biochem. Funct.
    Gallia et al., 2009, Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells., Mol. Cancer Ther.
    Gálvez-Peralta et al., 2014, Context-dependent antagonism between Akt inhibitors and topoisomerase poisons., Mol. Pharmacol.
    Dumble et al., 2014, Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor., PLoS ONE
    Papadopoulos et al., 2014, Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245409 (XL765), a novel, orally administered PI3K/mTOR inhibitor in patients with advanced solid tumors., Clin. Cancer Res.
    Yu et al., 2014, Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway., Mol. Cancer Ther.
    Bhagwat et al., 2011, Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin., Mol. Cancer Ther.
    Hudson et al., 2016, Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers., Mol. Cancer Ther.
    Poolman et al., 2005, Inhibition of the respiratory burst by resveratrol in human monocytes: correlation with inhibition of PI3K signaling., Free Radic. Biol. Med.
    Song et al., 2015, Potent antitumor activity of cabozantinib, a c-MET and VEGFR2 inhibitor, in a colorectal cancer patient-derived tumor explant model., Int. J. Cancer
    Campbell et al., 2004, The phosphatidylinositol/AKT/atypical PKC pathway is involved in the improved insulin sensitivity by DHEA in muscle and liver of rats in vivo., Life Sci.
    Gupta et al., 2015, A Phase I Trial of Combined Ridaforolimus and MK-2206 in Patients with Advanced Malignancies., Clin. Cancer Res.
    Darieva et al., 2004, Activation of phosphatidylinositol 3-kinase and c-Jun-N-terminal kinase cascades enhances NF-kappaB-dependent gene transcription in BCG-stimulated macrophages through promotion of p65/p300 binding., J. Leukoc. Biol.
    Premkumar et al., 2006, Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells., Mol. Carcinog.
    Lee et al., 2010, Deguelin promotes apoptosis and inhibits angiogenesis of gastric cancer., Oncol. Rep.
    Angevin et al., 2017, Safety, tolerability and antitumour activity of LY2780301 (p70S6K/AKT inhibitor) in combination with gemcitabine in molecularly selected patients with advanced or metastatic cancer: a phase IB dose escalation study., Eur. J. Cancer
    Yap et al., 2011, Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930., Mol. Cancer Ther.
    Fuhler et al., 2004, Disturbed granulocyte macrophage-colony stimulating factor priming of phosphatidylinositol 3,4,5-trisphosphate accumulation and Rac activation in fMLP-stimulated neutrophils from patients with myelodysplasia., J. Leukoc. Biol.
    Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov
    Shingu et al., 2003, Synergistic augmentation of antimicrotubule agent-induced cytotoxicity by a phosphoinositide 3-kinase inhibitor in human malignant glioma cells., Cancer Res.
    Ma et al., 2015, Multicenter phase II study of the AKT inhibitor MK-2206 in recurrent or metastatic nasopharyngeal carcinoma from patients in the mayo phase II consortium and the cancer therapeutics research group (MC1079)., Invest New Drugs
    Sangai et al., 2012, Biomarkers of response to Akt inhibitor MK-2206 in breast cancer., Clin. Cancer Res.
    Cufí et al., 2013, Dietary restriction-resistant human tumors harboring the PIK3CA-activating mutation H1047R are sensitive to metformin., Oncotarget
    Zhuang et al., 2005, Suramin promotes proliferation and scattering of renal epithelial cells., J. Pharmacol. Exp. Ther.
    Verma et al., 2006, The anti-leishmanial drug miltefosine causes insulin resistance in skeletal muscle cells in vitro., Diabetologia
    Yap et al., 2012, AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity., Clin. Cancer Res.
    Smakman et al., 2006, KRAS(D13) Promotes apoptosis of human colorectal tumor cells by ReovirusT3D and oxaliplatin but not by tumor necrosis factor-related apoptosis-inducing ligand., Cancer Res.
    Koizumi et al., 2005, Blocking of PI3K/Akt pathway enhances apoptosis induced by SN-38, an active form of CPT-11, in human hepatoma cells., Int. J. Oncol.
    Mortensen et al., 2015, CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization., Mol. Cancer Ther.
    Bendell et al., 2015, A phase I dose-escalation study to assess safety, tolerability, pharmacokinetics, and preliminary efficacy of the dual mTORC1/mTORC2 kinase inhibitor CC-223 in patients with advanced solid tumors or multiple myeloma., Cancer
    Machl et al., 2016, M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier., Am J Cancer Res
    Lieu et al., 2015, Antitumor activity of a potent MEK inhibitor, TAK-733, against colorectal cancer cell lines and patient derived xenografts., Oncotarget
    Fuhrer et al., 1996, Activation of Src-family protein tyrosine kinases and phosphatidylinositol 3-kinase in 3T3-L1 mouse preadipocytes by interleukin-11., Exp. Hematol.
    Yan et al., 2013, Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068., Clin. Cancer Res.
    Edvardsen H et al., 2010, SNPs in genes coding for ROS metabolism and signalling in association with docetaxel clearance., Pharmacogenomics J
  • SERABELISIB   PIK3CA

    Interaction Score: 1.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    28490463


    Sources:
    JAX-CKB ChemblInteractions TTD OncoKB

  • CHEMBL1939433   PIK3CA

    Interaction Score: 0.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22212721


    Sources:
    DTC

  • INK-1117   PIK3CA

    Interaction Score: 0.66

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase p110-alpha subunit inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions TTD

  • CC-223   PIK3CA

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    24978597 25855786 26177599


    Sources:
    JAX-CKB

  • CHEMBL263664   PIK3CA

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    21191045


    Sources:
    JAX-CKB

  • CHEMBL1379243   PIK3CA

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22212721


    Sources:
    DTC

  • TASELISIB   PIK3CA

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    25172762 23662903 26589432 26333383 28331003


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CIViC TTD OncoKB

  • IDELALISIB   PIK3CA

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type no benefit

    PMIDs:
    26137449 26466009


    Sources:
    JAX-CKB CIViC

  • TRASTUZUMAB   PIK3CA

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Trastuzumab + Lapatinib
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type decreased response

    PMIDs:
    21594665 20453058 22294718 25199759 28167203 21558396 23940356 21676217 17936563 24470511 26469692 26245675 19010894 26920887


    Sources:
    JAX-CKB CIViC PharmGKB

  • CAPIVASERTIB   PIK3CA

    Interaction Score: 0.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical - Pdx
    Approval Status Preclinical - Cell culture
    Response Type predicted – sensitive

    PMIDs:
    26116361 24088382 19755509 22294718 28489509


    Sources:
    JAX-CKB CIViC

  • PKI-179   PIK3CA

    Interaction Score: 0.33

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase p110-alpha subunit inhibitor
    Direct Interaction yes
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    20797855


    Sources:
    JAX-CKB ChemblInteractions

  • TEMSIROLIMUS   PIK3CA

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    19706758 27893038 25527417 21289267 22271473 22245973 27016228 21216929


    Sources:
    ClearityFoundationBiomarkers JAX-CKB 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

  • RIDAFOROLIMUS   PIK3CA

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Ridaforolimus + MK2206
    Indication/Tumor Type breast cancer
    Response Type predicted – sensitive

    PMIDs:
    26187616


    Sources:
    JAX-CKB

  • AZD-8835   PIK3CA

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type estrogen-receptor positive breast cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    26839307


    Sources:
    JAX-CKB

  • CHEMBL1765740   PIK3CA

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Alpelisib + GSK2334470
    Indication/Tumor Type breast cancer
    Response Type sensitive

    PMIDs:
    27451907


    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

  • 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

  • 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

  • COPANLISIB   PIK3CA

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    27672108 24170767


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial OncoKB

  • PWT-33579   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase p110-alpha subunit inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BAY-1082439   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase p110-alpha subunit inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AFURESERTIB   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    24978597


    Sources:
    JAX-CKB

  • CHEMBL589258   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    20371716


    Sources:
    JAX-CKB

  • DOXIL   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Temsirolimus + Doxil
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    21216929


    Sources:
    JAX-CKB

  • DEMCIZUMAB   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26855149


    Sources:
    JAX-CKB

  • GDC-0077   PIK3CA

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    OncoKB

  • A-443654   PIK3CA

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    19208828 24569089 24978597


    Sources:
    JAX-CKB

  • RIGOSERTIB   PIK3CA

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Novel Target
    Trial Name ON 01910.Na,Estybon
    Indication/Tumor Type head and neck squamous cell carcinoma

    PMIDs:
    27104980 23873848


    Sources:
    TdgClinicalTrial JAX-CKB

  • DEGUELIN   PIK3CA

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type stomach cancer
    Response Type predicted – sensitive
    Approval Status Preclinical

    PMIDs:
    24978597 20811676


    Sources:
    JAX-CKB

  • PA-799   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    25231405 21558396


    Sources:
    JAX-CKB ChemblInteractions TTD

  • LAPATINIB   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    Approval Status Preclinical - Pdx
    Indication/Tumor Type urinary bladder cancer

    PMIDs:
    22294718 26270481 23940356 26920887 26245675 26627007 25199759 19010894


    Sources:
    JAX-CKB CIViC PharmGKB

  • MILTEFOSINE   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16752184


    Sources:
    NCI

  • ABT 737   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ABT-737 + BEZ235
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type predicted – sensitive

    PMIDs:
    27974663


    Sources:
    JAX-CKB

  • PERIFOSINE   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19706758


    Sources:
    CIViC

  • SAMOTOLISIB   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction PI3-kinase class I inhibitor
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    27439478


    Sources:
    JAX-CKB ChemblInteractions TTD

  • SONOLISIB   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    22693357


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial

  • FULVESTRANT   PIK3CA

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Fulvestrant + GDC-0941
    Indication/Tumor Type estrogen-receptor positive breast cancer
    Response Type no benefit

    PMIDs:
    27174596 31091374


    Sources:
    JAX-CKB CIViC OncoKB

  • GEDATOLISIB   PIK3CA

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    25977343 24823695 24042735 21325073 17314276 25688157


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

  • PD-0325901   PIK3CA

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    combination therapy MLN0128 + PD-0325901
    Indication/Tumor Type colorectal cancer

    PMIDs:
    21325073 24339963 26272063


    Sources:
    JAX-CKB

  • NERATINIB   PIK3CA

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26243863 26333383 26627007


    Sources:
    JAX-CKB

  • MK-2206   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26084990 22932669 26187616 21289267 26627007


    Sources:
    JAX-CKB

  • 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

  • OPRELVEKIN   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8641341


    Sources:
    NCI

  • MSC-2363318A   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27186432


    Sources:
    JAX-CKB

  • CGM-097   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27659046


    Sources:
    JAX-CKB

  • ACALISIB   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Indication/Tumor Type breast adenocarcinoma
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • AEW-541   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + NVP-AEW541
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type sensitive

    PMIDs:
    27196766


    Sources:
    JAX-CKB

  • LUCITANIB   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Alpelisib + Lucitanib
    Indication/Tumor Type estrogen-receptor positive breast cancer
    Response Type sensitive

    PMIDs:
    27126994


    Sources:
    JAX-CKB

  • VOXTALISIB   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 colorectal cancer

    PMIDs:
    24583798 24634413


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions CancerCommons

  • LY-294002   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22212721 17562705


    Sources:
    DTC

  • DS-7423   PIK3CA

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type ovarian clear cell adenocarcinoma
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    24504419


    Sources:
    ClearityFoundationBiomarkers JAX-CKB ChemblInteractions

  • EVEROLIMUS   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    21358673 27091708 27797976 26951309 27893038 22662154 23629727 20664172 20664174


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC

  • PF-04691502   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction PI3-kinase class I inhibitor
    Direct Interaction yes
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    21750219


    Sources:
    ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions

  • IPATASERTIB   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    24141624


    Sources:
    JAX-CKB

  • IRINOTECAN HYDROCHLORIDE   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15809721


    Sources:
    NCI

  • AT-13148   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    22781553


    Sources:
    JAX-CKB

  • APITOLISIB   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type no benefit
    Indication/Tumor Type renal cell carcinoma
    Indication/Tumor Type malignant pleural mesothelioma

    PMIDs:
    26951309 26787751 21998291


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions

  • LINSITINIB   PIK3CA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + Linsitinib
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type sensitive

    PMIDs:
    27196766


    Sources:
    JAX-CKB

  • CETUXIMAB   PIK3CA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Cetuximab
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    20619739 19223544 28424201 19603024 28446642 27002107 26715098 25838391 25724520 25714871


    Sources:
    JAX-CKB CIViC

  • OMIPALISIB   PIK3CA

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Phase I
    Response Type no benefit

    PMIDs:
    26603258


    Sources:
    ClearityFoundationBiomarkers JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

  • TAK-733   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type predicted – sensitive
    Approval Status Preclinical - Pdx & cell culture

    PMIDs:
    26439693


    Sources:
    JAX-CKB

  • PERTUZUMAB   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23940356


    Sources:
    JAX-CKB

  • VISTUSERTIB   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27974663


    Sources:
    JAX-CKB

  • SAR-260301   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma

    PMIDs:
    None found


    Sources:
    CancerCommons

  • PANULISIB   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    25700704


    Sources:
    JAX-CKB ChemblInteractions

  • GSK-1059615   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    JAX-CKB ChemblInteractions

  • VS-5584   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type colon adenocarcinoma
    Indication/Tumor Type breast cancer
    Evidence Type Actionable

    PMIDs:
    23270925


    Sources:
    JAX-CKB ChemblInteractions

  • NAVITOCLAX   PIK3CA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27197306 27659046


    Sources:
    JAX-CKB

  • SAPANISERTIB   PIK3CA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy MLN0128 + PD-0325901
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    27974663 26272063 23085766 25261369


    Sources:
    JAX-CKB

  • PIMASERTIB   PIK3CA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Everolimus + Pimasertib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    23629727


    Sources:
    JAX-CKB

  • SULINDAC   PIK3CA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12654560 30683736


    Sources:
    NCI CIViC

  • FIMEPINOSTAT   PIK3CA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type hematologic cancer
    Approval Status Preclinical - Cell line xenograft
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    20570890 22693356


    Sources:
    JAX-CKB ChemblInteractions

  • VEMURAFENIB   PIK3CA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    22180495 24265153 26137449 24265155


    Sources:
    JAX-CKB CIViC

  • OSI-027   PIK3CA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    21673091


    Sources:
    JAX-CKB

  • AZD-8055   PIK3CA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD8055 + Selumetinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    28446642 22271687


    Sources:
    JAX-CKB

  • SELUMETINIB   PIK3CA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type predicted – sensitive
    Indication/Tumor Type endometrial cancer
    combination therapy Selumetinib + ZSTK474

    PMIDs:
    26232337 26137449 21358673 26272063 24939055 22271687


    Sources:
    JAX-CKB

  • VENETOCLAX   PIK3CA

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Venetoclax
    Indication/Tumor Type breast cancer
    Response Type no benefit

    PMIDs:
    27974663


    Sources:
    JAX-CKB

  • TANESPIMYCIN   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16267832


    Sources:
    NCI

  • BCG VACCINE   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14742634


    Sources:
    NCI

  • UPROSERTIB   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type predicted – sensitive
    Approval Status Phase I

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • TRAMETINIB   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Palbociclib + Trametinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    26882569 27797976 26469692 27659046 26627007 26369631


    Sources:
    JAX-CKB

  • AZD-6482   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy AZD6482 + BYL719
    Indication/Tumor Type breast cancer
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB ChemblInteractions

  • BEVACIZUMAB   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type resistant
    Approval Status Preclinical
    Indication/Tumor Type Her2-receptor positive breast cancer

    PMIDs:
    23940356 27893038 21216929 25363205


    Sources:
    JAX-CKB

  • SIROLIMUS   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    15878982 28514312 26882569 19029981 15647370 17376864


    Sources:
    JAX-CKB NCI CIViC

  • PI-103   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy PI-103 + 5-FU
    Indication/Tumor Type gastric adenocarcinoma
    Response Type sensitive

    PMIDs:
    22336586


    Sources:
    MyCancerGenome JAX-CKB

  • COBIMETINIB   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + cobimetinib
    Indication/Tumor Type colorectal adenocarcinoma
    Response Type sensitive

    PMIDs:
    22084396


    Sources:
    JAX-CKB

  • FLOXURIDINE   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Fluorouracil + Irinotecan + Floxuridine
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    25714871


    Sources:
    JAX-CKB

  • CABOZANTINIB   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25242168


    Sources:
    CIViC

  • LETROZOLE   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    Indication/Tumor Type estrogen-receptor positive breast cancer
    combination therapy Letrozole + BYL719

    PMIDs:
    27126994


    Sources:
    JAX-CKB

  • CAMPTOTHECIN   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Gedatolisib + Camptothecin
    Indication/Tumor Type colon cancer
    Response Type sensitive

    PMIDs:
    12464623 24042735 25688157


    Sources:
    JAX-CKB NCI

  • INFIGRATINIB   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy BGJ398 + BKM120
    combination therapy BGJ398 + BYL719
    Evidence Type Actionable

    PMIDs:
    28119489


    Sources:
    MyCancerGenome JAX-CKB

  • TOPOTECAN   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bortezomib + Temsirolimus + Topotecan
    Indication/Tumor Type small intestine adenocarcinoma
    Response Type resistant

    PMIDs:
    21216929


    Sources:
    JAX-CKB

  • REGRAMOSTIM   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15107457


    Sources:
    NCI

  • WX-037   PIK3CA

    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:
    ChemblInteractions

  • ZSTK-474   PIK3CA

    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:
    ChemblInteractions

  • RIBOCICLIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25002028


    Sources:
    CIViC

  • RECILISIB   PIK3CA

    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:
    ChemblInteractions

  • PRASTERONE   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15501480


    Sources:
    NCI

  • BGT-226   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RG-7666   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ALVOCIDIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14767524


    Sources:
    NCI

  • PWT-33587   PIK3CA

    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:
    ChemblInteractions

  • SF-1126   PIK3CA

    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:
    ChemblInteractions

  • PALBOCICLIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    27020857 26369631 25002028


    Sources:
    JAX-CKB CIViC

  • REGORAFENIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23629727 25838391


    Sources:
    JAX-CKB

  • DABRAFENIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + Everolimus + Trametinib
    Indication/Tumor Type thyroid carcinoma
    Response Type sensitive

    PMIDs:
    27797976


    Sources:
    JAX-CKB

  • PANITUMUMAB   PIK3CA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19223544


    Sources:
    CIViC

  • IRINOTECAN   PIK3CA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Irinotecan
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    24042735 16707468 21325073 25714871


    Sources:
    JAX-CKB

  • PUQUITINIB   PIK3CA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PONATINIB   PIK3CA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type urinary bladder cancer
    Response Type no benefit
    Approval Status Preclinical - Pdx

    PMIDs:
    26270481


    Sources:
    JAX-CKB

  • CAPECITABINE   PIK3CA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Lapatinib + Capecitabine
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type decreased response

    PMIDs:
    26920887


    Sources:
    JAX-CKB CIViC

  • MIDOSTAURIN   PIK3CA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11719451


    Sources:
    NCI

  • EMODIN   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22212721


    Sources:
    DTC

  • ALDESLEUKIN   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10229082


    Sources:
    NCI

  • OLAPARIB   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + Olaparib
    Indication/Tumor Type ovarian cancer
    Response Type sensitive

    PMIDs:
    26909613


    Sources:
    JAX-CKB

  • PACLITAXEL   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Clinical Study
    Response Type resistant
    Indication/Tumor Type colorectal cancer

    PMIDs:
    21216929 26245675 24170767 26469692 12761490


    Sources:
    JAX-CKB NCI

  • RALOXIFENE   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11901050


    Sources:
    NCI

  • SURAMIN   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15833899


    Sources:
    NCI

  • QUERCETIN   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22212721 17045724


    Sources:
    DTC MyCancerGenome NCI

  • CARBOPLATIN   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy XL147 + Carboplatin + Paclitaxel
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    16275998 21216929


    Sources:
    JAX-CKB NCI PharmGKB

  • IBUPROFEN   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30683736


    Sources:
    CIViC

  • GSK-2636771   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • DOXORUBICIN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Doxorubicin + Temsirolimus
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type predicted – sensitive

    PMIDs:
    27893038 16905201 12761490


    Sources:
    JAX-CKB NCI

  • METFORMIN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23986086


    Sources:
    JAX-CKB

  • MYRICETIN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22212721


    Sources:
    DTC

  • RESVERATROL   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15925284


    Sources:
    NCI

  • STREPTOZOCIN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16130182


    Sources:
    NCI

  • ASPIRIN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23094721 30683736


    Sources:
    CIViC

  • ERLOTINIB   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21258250


    Sources:
    CIViC

  • FLUOROURACIL   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Cetuximab
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    25714871 28424201 22336586


    Sources:
    JAX-CKB

  • SORAFENIB   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Sorafenib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    23629727 25363205


    Sources:
    JAX-CKB

  • VINCRISTINE   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12874004


    Sources:
    NCI

  • TAMOXIFEN   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD5363 + Tamoxifen
    Indication/Tumor Type estrogen-receptor positive breast cancer
    Response Type predicted – sensitive

    PMIDs:
    26116361


    Sources:
    JAX-CKB

  • CELECOXIB   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30683736


    Sources:
    CIViC

  • GEFITINIB   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21258250


    Sources:
    CIViC

  • DASATINIB   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dasatinib + Demcizumab
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    26855149


    Sources:
    JAX-CKB

  • CISPLATIN   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Phase II
    Response Type predicted – resistant

    PMIDs:
    27489350


    Sources:
    JAX-CKB CIViC PharmGKB

  • DOCETAXEL   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20157331


    Sources:
    PharmGKB

  • GEMCITABINE   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cisplatin + Gemcitabine + Sorafenib
    Indication/Tumor Type invasive bladder transitional cell carcinoma
    Response Type predicted – resistant

    PMIDs:
    28750271


    Sources:
    JAX-CKB

  • BORTEZOMIB   PIK3CA

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bortezomib + Temsirolimus + Topotecan
    Indication/Tumor Type small intestine adenocarcinoma
    Response Type resistant

    PMIDs:
    21216929


    Sources:
    JAX-CKB

  • Ensembl: ENSG00000121879

    • Version: 101_38

    Alternate Names:
    PIK3CA Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: P42336

    • Version: January-2014

    Alternate Names:
    PIK3CA Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:2.7.1.153

    Publications:

  • HopkinsGroom: P42336

    • Version: 11-September-2012

    Alternate Names:
    PIK3CA Uniprot Gene Name
    ENSG00000121879 Ensembl Gene Id
    PK3CA_HUMAN Uniprot Id

    Gene Info:
    Interpro Short Name PI3/4_kinase_cat_dom
    Human Readable Name PHOSPHATIDYLINOSITOL 3 KINASE
    Uniprot Evidence 1: Evidence at protein level

    Gene Categories:
    DRUGGABLE GENOME, PHOSPHATIDYLINOSITOL 3 KINASE

    Publications:

  • CancerCommons: PIK3CA

    • Version: 25-July-2013

    Alternate Names:
    5290 Entrez Gene ID
    5289 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name PI3K
    CancerCommons Reported Gene Name PI3K/mTOR

    Publications:

  • RussLampel: ENSG00000121879

    • Version: 26-July-2011

    Alternate Names:
    PIK3CA Display Id
    PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT, ALPHA ISOFORM (EC 2.7.1.153) (PI3-KINASE P110 SUBUNIT ALPHA) (PTDINS- 3-KINASE P110) (PI3K). [SOURCE:UNIPROT/SWISSPROT;ACC:P42336] Description
    ENSG00000121879 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • JAX-CKB: PIK3CA

    • Version: 27-September-2017

    Alternate Names:
    5290 CKB Entrez Id
    PIK3CA CKB Gene Synonym
    CLOVE CKB Gene Synonym

    Gene Info:

    Publications:
    Wang et al., 2016, Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer., Oncotarget
    de Lint et al., 2016, Sensitizing Triple-Negative Breast Cancer to PI3K Inhibition by Cotargeting IGF1R., Mol. Cancer Ther.
    Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.

  • PharmGKB: PIK3CA

    • Version: 18-August-2020

    Alternate Names:
    PA33308 PharmGKB ID

    Gene Info:

    Publications:
    Edvardsen H et al., 2010, SNPs in genes coding for ROS metabolism and signalling in association with docetaxel clearance., Pharmacogenomics J
    Loibl S et al., 2014, PIK3CA mutations are associated with lower rates of pathologic complete response to anti-human epidermal growth factor receptor 2 (her2) therapy in primary HER2-overexpressing breast cancer., J Clin Oncol

  • CIViC: PIK3CA

    • Version: 14-September-2020

    Alternate Names:
    5290 Entrez Gene ID
    37 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE, CLINICALLY ACTIONABLE

    Publications:
    Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
    Weigelt et al., 2011, PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs., Oncogene
    Tanaka et al., 2011, The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations., Clin. Cancer Res.

  • NCI: PIK3CA

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Ciprés et al., 1999, An IL-2 receptor beta subdomain that controls Bcl-X(L) expression and cell survival., Eur. J. Immunol.
    Yousif et al., Phosphoinositide 3-kinase mediated signalling contributes to development of diabetes-induced abnormal vascular reactivity of rat carotid artery., Cell Biochem. Funct.
    Premkumar et al., 2006, Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells., Mol. Carcinog.

  • DTC: PIK3CA

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Sabbah DA et al., 2012, Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases., Bioorg Med Chem Lett
    Nacht M et al., 2013, Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα., J Med Chem
    Ballou et al., 2007, Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one., J. Biol. Chem.

  • MyCancerGenome: PIK3CA

    • Version: 20-Jun-2017

    Alternate Names:
    5290 Entrez Gene Id
    PIK3CA MyCancerGenome Gene Symbol
    PI3K MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • ChemblInteractions: PIK3CA

    • Version: chembl_23

    Alternate Names:
    PIK3CA GENE_SYMBOL
    Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform UNIPROT
    Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha UNIPROT

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000121879

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000121879 Gene Symbol
    PIK3CA Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • OncoKB: PIK3CA

    • Version: 23-July-2020

    Alternate Names:
    5290 OncoKB Entrez Id
    MCAP OncoKB Gene Synonym
    p110-alpha OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Tempus: PIK3CA

    • Version: 11-November-2018

    Alternate Names:
    PIK3CA Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: PIK3CA

    • Version: 27-Jun-2013

    Alternate Names:
    5290 Gene ID
    PI3K dGene Synonym
    p110-alpha dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, PHOSPHATIDYLINOSITOL 3 KINASE

    Publications:

  • TTD: PI3-kinase alpha

    • Version: 2020.06.01

    Alternate Names:
    PIK3CA TTD Gene Abbreviation
    T80276 TTD Target ID

    Gene Info:

    Publications:

  • Pharos: PIK3CA

    • Version: 01-February-2022

    Alternate Names:
    Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Gene Name
    P42336 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • MskImpact: PIK3CA

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • MyCancerGenomeClinicalTrial: PIK3CA

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • ClearityFoundationBiomarkers: PIK3CA

    • Version: 26-July-2013

    Alternate Names:

    Gene Info:

    Publications:

  • FoundationOneGenes: PIK3CA

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: PIK3CA

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FDA: PIK3CA

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Publications:

  • GO: PIK3CA

    • Version: 01-February-2022

    Alternate Names:

    Gene Info:

    Gene Categories:
    KINASE, SERINE THREONINE KINASE

    Publications:

  • Oncomine: PIK3CA

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    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