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GENE:

PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)

i
Other names: PIK3CA, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha, Phosphoinositide-3-kinase, catalytic, alpha polypeptide, Serine/threonine protein kinase PIK3CA, PtdIns-3-kinase subunit P110-alpha, PI3K-alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase 110 KDa catalytic subunit alpha, Phosphatidylinositol 3-kinase, Catalytic, 110-KD, alpha, PI3-kinase P110 subunit alpha, PI3-kinase subunit alpha, PtdIns-3-kinase subunit alpha, PI3Kalpha, P110alpha, PI3K
1d
Clinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer. (clinicaltrials.gov)
P1/2, N=40, Active, not recruiting, Criterium, Inc. | Recruiting --> Active, not recruiting | Trial completion date: Jun 2025 --> Jun 2026 | Trial primary completion date: Aug 2024 --> Mar 2026
Enrollment closed • Trial completion date • Trial primary completion date
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CD4 (CD4 Molecule)
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HER-2 positive • PIK3CA mutation
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Guardant360® CDx • FoundationOne® Liquid CDx • therascreen® PIK3CA RGQ PCR Kit
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Piqray (alpelisib) • fulvestrant • Tukysa (tucatinib)
1d
IPATHER: Ipatasertib + Pertuzumab +Trastuzumab in Advanced HER2+ PI3KCA-mutant Breast Cancer Patients (clinicaltrials.gov)
P1, N=17, Completed, SOLTI Breast Cancer Research Group | Recruiting --> Completed
Trial completion
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor)
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HER-2 positive • PIK3CA mutation
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Herceptin (trastuzumab) • Perjeta (pertuzumab) • ipatasertib (RG7440)
1d
Trial initiation date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CDK4 (Cyclin-dependent kinase 4)
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HER-2 negative • PIK3CA mutation
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fulvestrant • Itovebi (inavolisib)
3d
Landscape of somatic genetic alterations and PAM50 intrinsic subtypes in breast cancer associated with germline pathogenic variants in DNA-repair genes. (PubMed, J Natl Cancer Inst)
GPVs in BRCA1, BRCA2, ATM, CHEK2, and PALB2 are associated with distinct intrinsic breast cancer subtypes and somatic genomic alterations. These findings may enhance precision in risk stratification and guide personalized treatment strategies.
Journal • BRCA Biomarker
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HER-2 (Human epidermal growth factor receptor 2) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • FGFR1 (Fibroblast growth factor receptor 1) • PALB2 (Partner and localizer of BRCA2) • CHEK2 (Checkpoint kinase 2)
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HER-2 negative
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Prosigna™ Breast Cancer Prognostic Gene Signature Assay
4d
GPS1 Exon 9 Mutations Represent a Rare Genetic Event in Penile Squamous Cell Carcinoma Pathogenesis. (PubMed, Int J Mol Sci)
This observation suggests that GPS1 exon 9 sequence is a target of genetic alteration during PSCC pathogenesis. However, the non-recurrent nature of these alterations indicates that they are unlikely to represent oncogenic drivers in this disease.
Journal
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TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • NOTCH1 (Notch 1) • FAT1 (FAT atypical cadherin 1) • GPS1 (G Protein Pathway Suppressor 1)
4d
Integrated Molecular and Functional Characterization of Cervical Small-Cell Neuroendocrine Carcinoma Using a 3D Organoid Model. (PubMed, Int J Mol Sci)
This study presents the first integrated molecular and functional analyses of patient tumors and matched organoid and xenograft models in cervical SCNEC. These models offer robust resources for mechanistic studies and may enable precision therapeutic strategies for this rare malignancy.
Journal
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TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • NCAM1 (Neural cell adhesion molecule 1) • SYP (Synaptophysin)
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PIK3CA mutation
4d
GARD: Genomic Data-Based Drug Repurposing in Head and Neck Cancer with Large Language Model Validation. (PubMed, Cancers (Basel))
Drug-gene mapping revealed candidates spanning those already in clinical trials for HNC (e.g., Afatinib, Cabozantinib, Dasatinib, Brigatinib, Lenvatinib, Capivasertib, and Erdafitinib) and emerging or repurposing candidates (Amuvatinib, XL765 (Voxtalisib), Golotimod, Artenimol, Quercetin, and Acetylsalicylic Acid), offering opportunities for precision repurposing...HPV stratification enhances precision, literature-based validation strengthens confidence, and integrated drug mapping enables refinement of existing therapies and discovery of novel candidates for personalized treatment strategies. Code Availability: The full implementation of the GARD pipeline, including preprocessing scripts, statistical analysis modules, and visualization tools, is publicly available on GitHub.
Journal • IO biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • SOX2 • CLDN1 (Claudin 1) • TLR7 (Toll Like Receptor 7) • EIF4G1 (Eukaryotic translation initiation factor 4 gamma, 1)
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Gilotrif (afatinib) • dasatinib • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet) • Balversa (erdafitinib) • Alunbrig (brigatinib) • Truqap (capivasertib) • amuvatinib (MP470) • aspirin • voxtalisib (SAR245409)
4d
The features and prognostic value of ARID1A mutation and protein expression in endometrial cancer of no specific molecular profile (NSMP) subtype: a retrospective study in a large Chinese cohort. (PubMed, J Cancer Res Clin Oncol)
ARID1A mutation was associated with worse PFS for patients with NSMP. ARID1A protein expression was significantly associated with ARID1A mutation. ARID1A mutation, with ER/PR expression and PIK3CA mutation status, could serve as the potential biomarkers to subclassify NSMP subtype and provide more precise therapeutic target.
Retrospective data • Journal
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ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • ARID1A (AT-rich interaction domain 1A)
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PIK3CA mutation • ARID1A mutation • ER negative
4d
Autophagy-centered regulation of PI3K/Akt/mTOR and MAPK signaling by traditional Chinese medicine in gastric cancer. (PubMed, Tissue Cell)
Future directions emphasize high-quality trials, omics integration, and precision TCM for clinical translation. TCM offers low-toxicity, holistic options for integrative GC management, potentially improving survival and quality of life.
Review • Journal • IO biomarker
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KRAS (KRAS proto-oncogene GTPase) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
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KRAS mutation • PIK3CA mutation
5d
Genomic profiling and HER2-targeted therapy: a case series of Chinese salivary duct carcinoma patients and its clinical implications. (PubMed, Front Oncol)
Two metastatic SDC patients with HER2 amplification responded to HER2 tyrosine kinase inhibitor (TKI) pyrotinib and the combination of trastuzumab and pertuzumab, respectively. Our work underscores the potential of genomic profiling to guide precision therapy in SDC, with HER2-targeted treatments offering promising therapeutic avenues.
Journal
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TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • HRAS (Harvey rat sarcoma viral oncogene homolog) • NF1 (Neurofibromin 1)
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TP53 mutation • HER-2 amplification • PIK3CA mutation
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Herceptin (trastuzumab) • Perjeta (pertuzumab) • Irene (pyrotinib)
5d
Design of novel PI3Kα and PI3Kγ inhibitors for cancer treatment using pharmacophore, protein-ligand contacts, and machine learning methods. (PubMed, J Comput Aided Mol Des)
Pharmacophore mapping, molecular docking-assisted structural analysis suggested certain criteria in the chemical compound, such as number of heavy atoms (> 25), number of rotatable bonds (> 4), molecular weight (> 400 Da), log P (> 2), to be favorable for better binding to the receptor. The role of non-bonding interactions measured with the number of atomic contacts within a 10.5 Å cutoff at the binding site of protein ligand complex, such as CC (> 2000), CO (> 800), CX (> 30), and the number of NN contacts (< 200), also favored the binding affinity of inhibitors.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
5d
Rare but Distinct: A Systematic Review of Primary Neuroendocrine Tumors of the Breast According to WHO 2019 Guidelines. (PubMed, Crit Rev Oncol Hematol)
BNETs represent a biologically distinct subset of breast cancers with favorable prognostic features and a consistent luminal-like phenotype. However, evidence on optimal treatment remains limited. Further large-scale, prospective studies are needed to define clinical management and validate molecular findings.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • KMT2C (Lysine Methyltransferase 2C) • SSTR (Somatostatin Receptor) • FOXA1 (Forkhead Box A1) • SSTR2 (Somatostatin Receptor 2)
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TP53 mutation • HR positive • HER-2 overexpression • PIK3CA mutation • HER-2 overexpression + HR positive