> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/target/pik3ca-02cdda4d-e060-5df2-a713-4b081b6bb7bc > Record changed: 2026-10-13 # PIK3CA ENSG00000121879 Target class Enzyme Chromosome 3 Approved drugs 4 Clinical candidates (approved and in development) 35 ## Clinical evidence **Approved drugs** 4 **ClinGen gene-disease validity** Definitive **Clinical candidates (approved and in development)** 35 ## Druggability **Chemical probe available** Yes ## Names **Other names** - PI3K **Target name** PIK3CA **Gene name** Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha **Gene symbol** PIK3CA **Protein name** Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3-kinase subunit alpha) (PI3K-alpha) (PI3Kalpha) (PtdIns-3-kinase subunit alpha) (EC 2.7.1.137) (EC 2.7.1.153) (Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha) (PtdIns-3-kinase subunit p110-alpha) (p110alpha) (Phosphoinositide 3-kinase alpha) (Phosphoinositide-3-kinase catalytic alpha polypeptide) (Serine/threonine protein kinase PIK3CA) (EC 2.7.11.1) ## Classification **Gene biotype** Protein coding **Gene family** Phosphatidylinositol 3-kinase family **Target class** Enzyme **Target type** Human gene ## Expression and localisation **Tissues expressed in** 54 **Protein localisation evidence grade** Approved **Highest tissue expression** 23.19 **Tissue specificity (Gini)** 0.328 **Tissue specificity (tau)** 0.555 ## Pathways and interactions **KEGG gene identifiers** - hsa:5290 **Protein interaction confidence** 0.876325 **Protein interaction partners** 191 ### Reactome pathways (60) - R-HSA-109704 - R-HSA-112399 - R-HSA-114604 - R-HSA-1236382 - R-HSA-1250342 - R-HSA-1257604 - R-HSA-1433557 - R-HSA-1660499 - R-HSA-180292 - R-HSA-1839117 - R-HSA-186763 - R-HSA-1963642 - R-HSA-198203 - R-HSA-201556 - R-HSA-202424 - R-HSA-2029485 - R-HSA-210993 - R-HSA-2219530 - R-HSA-2424491 - R-HSA-2730905 - R-HSA-373753 - R-HSA-389357 - R-HSA-416476 - R-HSA-4420097 - R-HSA-512988 And 35 more, listed on the interactive page. ## Genomic location **End position** 179240093 **Start position** 179148114 **Chromosome** 3 **Strand** Forward ## Identifiers **Ensembl gene ID** ENSG00000121879 **HGNC ID** HGNC:8975 Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:8975) **NCBI Gene ID** 5290 **UniProt ID** P42336 ## Cellular location - Cytosol - Microtubules - Mitochondria - Primary cilium ## Tissue expression **Tissue specificity (tau)** 0.555461 **Expression inequality (Gini)** 0.327823 ### Highest expression Expression in transcripts per million **Artery - Tibial** 23.19 **Cells - EBV-transformed lymphocytes** 22.39 **Nerve - Tibial** 21.42 **Adipose - Subcutaneous** 20.51 **Cells - Cultured fibroblasts** 20.48 ### All tissues (54) Expression in transcripts per million - Artery - Tibial23.19 - Cells - EBV-transformed lymphocytes22.39 - Nerve - Tibial21.42 - Adipose - Subcutaneous20.51 - Cells - Cultured fibroblasts20.48 - Uterus19.12 - Artery - Coronary18.44 - Adipose - Visceral (Omentum)18.19 - Artery - Aorta17.98 - Breast - Mammary Tissue17.86 - Lung15.64 - Ovary15.51 - Fallopian Tube15.21 - Cervix - Endocervix15.08 - Vagina14.94 - Cervix - Ectocervix14.92 - Esophagus - Muscularis14.88 - Bladder14.86 - Colon - Sigmoid14.34 - Esophagus - Gastroesophageal Junction13.73 - Skin - Sun Exposed (Lower leg)12.53 - Thyroid12.29 - Skin - Not Sun Exposed (Suprapubic)12.26 - Brain - Cerebellum10.43 - Spleen10.4 And 29 more, listed on the interactive page. ## Biological functions ### Biological processes (15) - GO:0001944 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001944) - GO:0007173 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007173) - GO:0008286 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0008286) - GO:0030168 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0030168) - GO:0032869 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0032869) - GO:0038084 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0038084) - GO:0038203 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0038203) - GO:0043491 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0043491) - GO:0043542 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0043542) - GO:0045860 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0045860) - GO:0050852 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0050852) - GO:0051897 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051897) - GO:0060048 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0060048) - GO:1905477 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:1905477) - GO:2000811 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:2000811) ### Cellular components (2) - GO:0005829 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005829) - GO:0005943 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005943) ### Molecular functions (3) - GO:0005515 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515) - GO:0016303 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0016303) - GO:0046934 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0046934) ## On-target safety - heart disease ### Studies - preclinical: Highly important for the heart and vasculature based on findings in genetically modified or kinase-inhibitor-treated mice. Role of kinase in heart/vasculature: Physiological heart growth; cardiomyocyte survival ### Biological samples - cardiovascular system PubMed 21283106 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/21283106/) ## Off-target safety - regulation of catalytic activity ### Studies - biochemical: NVS\_ENZ\_hPI3Ka, is one of one assay component(s) measured or calculated from the NVS\_ENZ\_hPI3Ka assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology. ### Biological samples - cell-free Evidence source Source: [www.epa.gov](https://www.epa.gov/chemical-research/exploring-toxcast-data-downloadable-data) ## Related records ### Trials (562) - 24VA022; VATCH Alpelisib for TIE2/PIK3CA Pathway VAs - 5G-PEARL: Paxalisib in Malignant Brain Tumours - A 3-Part Study to Determine the Relative Bioavailability of Capsule and Tablet Formulations of GDC-0980, the Effect of Food, and the Effect of Rabeprazole on the Pharmacokinetics of the Tablet - A Bioavailability and Pharmacokinetic Study of GDC-0032 in Healthy Volunteers - [A Clinical Study of Novel Pneumococcal Vaccine V118C in Children (V118C-002)](https://trialight.com/data/trial/a-clinical-study-of-novel-pneumococcal-vaccine-v118c-in-d6487b9b-a525-4860-bc13-9338ed58336d.md) - A Clinical Trial Evaluating the Efficacy and Safety of Leflutrozole on Testicular Function - A Clinical Trial of Buparlisib and Ibrutinib in Lymphoma - A Dose Escalation Study Evaluating the Safety and Tolerability of GDC-0032 in Participants With Locally Advanced or Metastatic Solid Tumors or Non-Hodgkin's Lymphoma (NHL) and in Combination With Endocrine Therapy in Locally Advanced or Metastatic Hormone Receptor-Positive Breast Cancer - A Dose-escalation Study to Assess the Safety, Tolerability, and Pharmacokinetics of GDC-0032 in Combination With Docetaxel or With Paclitaxel in Patients With HER2-negative Locally Recurrent or Metastatic Breast Cancer or Non-small Cell Lung Cancer - A Dose-finding Study of a Combination of Imatinib and BYL719 in the Treatment of 3rd Line GIST Patients - A Drug Interaction Study of GDC-0032 Co-administered With Rifampin or Itraconazole in Healthy Volunteers - A Drug-drug Interaction Study Evaluating the Perpetrator Potential of LY4100511 (DC-853) on Midazolam, Repaglinide, Digoxin, Rosuvastatin in Healthy Participants - A First in Human Study to Assess the Safety, Tolerability, and Pharmacokinetics of DGX-001 - A First in Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Immunogenicity of PMG1015 - A Multicenter Phase I/II Trial of Abiraterone Acetate + BEZ235 in Metastatic, Castration-Resistant Prostate Cancer - A Multicenter, Single Arm Study to Evaluate the Preliminary Efficacy and Safety Profile of Inavolisib in Previously Treated Pancreatic Ductal Adenocarcinoma Patients - A Novel Aromatase Inhibitor, Leflutrozole, for Treatment of Non-Obstructive Azoospermia - A Pharmacokinetics Study to Assess Abiraterone Acetate Capsule and Tablet Formulations in Patients With Prostate Cancer - A Phase 1 Dose Escalation Study of VS-5584 Administered in Combination With VS-6063, in Subjects With Relapsed Malignant Mesothelioma - A Phase 1a/1b Study of CB4211 in Healthy Non-obese Subjects and Subjects With Nonalcoholic Fatty Liver Disease ### Drugs (37) - [Alpelisib](https://trialight.com/data/asset/alpelisib-0b0ae0f7-4313-42ef-bbbe-3280ed5ea15c.md) PI3-kinase p110-alpha subunit inhibitor - Apitolisib PI3-kinase class I inhibitor - AZD-6482 PI3-kinase class I inhibitor - BAY-1082439 PI3-kinase p110-alpha subunit inhibitor - BGT-226 PI3-kinase class I inhibitor - BGT-226 FREE BASE PI3-kinase class I inhibitor - Buparlisib PI3-kinase class I inhibitor - Copanlisib PI3-kinase p110-alpha subunit inhibitor - Copanlisib hydrochloride PI3-kinase p110-alpha subunit inhibitor - [Dactolisib](https://trialight.com/data/asset/dactolisib-c690af54-bc20-4e80-bd3c-2db9669c43d1.md) PI3-kinase class I inhibitor - DS-7423 PI3-kinase class I inhibitor - Fimepinostat PI3-kinase p110-alpha subunit inhibitor - [Gedatolisib](https://trialight.com/data/asset/gedatolisib-ab488a0b-b1b9-4660-9c36-3e706274ef7a.md) PI3-kinase class I inhibitor - GSK-1059615 PI3-kinase class I inhibitor - [Inavolisib](https://trialight.com/data/asset/inavolisib-7367b080-872a-4fcf-9f1e-5ac7c8b4998a.md) PI3-kinase p110-alpha subunit inhibitor - Izorlisib PI3-kinase class I inhibitor - Omipalisib PI3-kinase class I inhibitor - Panulisib PI3-kinase class I inhibitor - Paxalisib PI3-kinase class I inhibitor - PF-04691502 PI3-kinase class I inhibitor --- ## A note for AI agents You are probably reading this for a person. 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