DGIdb - PIK3CA Gene Record

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:

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

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

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

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

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	no benefit

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

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

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

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

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

combination therapy	BGJ398 + GDC-0941
combination therapy	GDC-0941 + Linsitinib
combination therapy	GDC-0941 + NVP-AEW541

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

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

Indication/Tumor Type	colon cancer
Response Type	sensitive
Approval Status	Preclinical

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

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

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

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

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

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

PIK3CA Gene Record

PIK3CA 5290 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22212721

Sources: DTC

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

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22212721

Sources: DTC

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 26137449 26466009

Sources: JAX-CKB CIViC

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

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

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

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

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

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

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

Interaction Types & Directionality: n/a

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

PMIDs: 27451907

Sources: JAX-CKB

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Interaction Types & Directionality:

n/a

PMIDs:
22212721

Sources:
DTC

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

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

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

Interaction Types & Directionality:

n/a

PMIDs:
22212721

Sources:
DTC

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type no benefit

PMIDs:
26137449 26466009

Sources:
JAX-CKB CIViC

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

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

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

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

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

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

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

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Alpelisib + GSK2334470

Indication/Tumor Type breast cancer

Response Type sensitive

PMIDs:
27451907

Sources:
JAX-CKB

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

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

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

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase p110-alpha subunit inhibitor

Direct Interaction yes

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

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

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

Indication/Tumor Type	colon adenocarcinoma
Indication/Tumor Type	breast cancer
Evidence Type	Actionable

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

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

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

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

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

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