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    1m
    EPIK-RO: Roll-Over Study of Alpelisib (BYL719) for Continued Access and Long-Term Safety. (clinicaltrials.gov)
    P2, N=51, Not yet recruiting, Novartis Pharmaceuticals
    New P2 trial
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    Herceptin (trastuzumab) • Perjeta (pertuzumab) • Piqray (alpelisib) • fulvestrant • letrozole
    1m
    A phase II study of alpelisib and capecitabine in patients with previously treated metastatic colorectal cancer (KCSG-CO21-04). (PubMed, Sci Rep)
    Overall, alpelisib combined with capecitabine demonstrated modest antitumor activity in a molecularly selected subset of patients with metastatic colorectal cancer. However, frequent treatment-limiting toxicities may limit the future clinical applicability of this regimen and highlight the need for improved toxicity management and optimized patient selection.
    P2 data • Journal
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    HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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    PIK3CA mutation
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    capecitabine • Piqray (alpelisib)
    1m
    Phase IB/II study of alpelisib combined with paclitaxel in patients with PIK3CA-altered metastatic or recurrent gastric cancer. (PubMed, Oncologist)
    Alpelisib plus paclitaxel was tolerable and pharmacologically feasible with a defined RP2D but showed limited efficacy in PIK3CA-altered GC.
    P1/2 data • Journal
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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    paclitaxel • Piqray (alpelisib)
    2ms
    Functional characterization of PIK3CA E545A mutation in MCF-7 breast cancer cells reveals enhanced proliferation and resistance to Alpelisib. (PubMed, Biochem Biophys Res Commun)
    Collectively, these findings identify E545A as a functionally active and therapeutically consequential PIK3CA variant. Our study expands the current understanding of PIK3CA-driven oncogenic diversity beyond canonical hotspot mutations and underscores the need for variant-resolved stratification to improve the efficacy of PI3K-targeted therapies.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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    HR positive • HER-2 negative • PIK3CA mutation • HR positive + HER-2 negative
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    Piqray (alpelisib)
    2ms
    Alpelisib enhances cisplatin mediated cytotoxicity in non-mutated, PIK3CA-dependent high-grade serous ovarian cancer. (PubMed, J Ovarian Res)
    Our findings highlight the potential of cisplatin-alpelisib treatment in a subset of HGSOC patients with PIK3CA overexpression, mediated either through gene amplification or transcriptional modulation, reflecting the wider application of alpelisib in PIK3CA-non-mutated ovarian cancer.
    Journal • BRCA Biomarker
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • BRCA2 (Breast cancer 2, early onset)
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    TP53 mutation • BRCA2 mutation • PIK3CA mutation
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    cisplatin • Piqray (alpelisib)
    2ms
    Niraparib and Copanlisib in Treating Patients With Recurrent Endometrial, Ovarian, Primary Peritoneal, or Fallopian Tube Cancer (clinicaltrials.gov)
    P1, N=31, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed | Trial completion date: Dec 2026 --> Jun 2026 | Trial primary completion date: Dec 2026 --> Jun 2026
    Trial completion • Trial completion date • Trial primary completion date
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    BRCA (Breast cancer early onset) • MUC16 (Mucin 16, Cell Surface Associated)
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    BRCA mutation
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    Zejula (niraparib) • Aliqopa (copanlisib)
    2ms
    Combined inhibition of CDK4/6 and PI3K pathways exhibit highly synergistic activity and translational potential in Ewing sarcoma. (PubMed, Transl Oncol)
    The results of the screen revealed that a PI3K inhibitor, copanlisib, combined with a CDK4/6 inhibitor, ribociclib, exhibited strong synergistic anti-Ewing sarcoma activity. In two xenograft models of Ewing sarcoma, we demonstrated that the combination significantly prolonged survival compared to treatment with either vehicle or single-agent therapy alone. Our findings identify a new candidate therapy combination for Ewing sarcoma and provide a resource of additional potential synergistic combinations for future validation.
    Journal
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    CDK4 (Cyclin-dependent kinase 4) • EWSR1 (EWS RNA Binding Protein 1) • FLI1 (Fli-1 Proto-Oncogene ETS Transcription Factor)
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    Kisqali (ribociclib) • Aliqopa (copanlisib)
    2ms
    Body mass index in postmenopausal women with estrogen receptor-positive, HER2-negative early breast cancer: An exploratory analysis of the LORELEI trial. (PubMed, Eur J Cancer)
    Obesity was associated with lower ORR with letrozole alone, whereas this association was not observed in patients treated with taselisib.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • IL6 (Interleukin 6)
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    HER-2 positive • ER positive • HER-2 negative • ER positive + HER-2 negative • HER-2 negative + ER positive
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    letrozole • taselisib (GDC-0032)
    2ms
    In vitro study of TSC1 deficiency in preadipocytes: insights into development and treatment options for tuberous sclerosis related lipomatosis. (PubMed, Orphanet J Rare Dis)
    This study highlights the need for further investigation into the efficacy of pathway inhibitors in managing TSC-related lipomas in vivo and offers a potential treatment avenue for patients suffering from recurrent lipomatosis.
    Preclinical • Journal
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    TSC2 (TSC complex subunit 2) • TSC1 (TSC complex subunit 1)
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    Piqray (alpelisib) • sirolimus
    2ms
    Identification of PI3K alpha inhibitors through large-scale virtual screening and integrated molecular modeling, biophysical characterization, and ADMET profiling. (PubMed, Sci Rep)
    ADMET profiling demonstrated satisfactory drug-likeness for all candidates. Five promising PI3K p110α inhibitor candidates with potential anti-lung cancer activity were identified; experimental validation is required to confirm these computational results.
    Journal
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    2ms
    In silico analysis of driver genes in squamous cell carcinoma of the cervix: insights into their biological functions, prognosis, immune infiltration, and therapy. (PubMed, World J Surg Oncol)
    Collectively, our analysis describes the driver genes and mutation characteristics in SCC. The multi-cohort and network-based framework employed in this study identifies candidate hub genes that warrant further clinical investigation in cervical cancer.
    Journal
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    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • STK11 (Serine/threonine kinase 11) • ARID1A (AT-rich interaction domain 1A) • NOTCH1 (Notch 1) • KMT2D (Lysine Methyltransferase 2D) • FBXW7 (F-Box And WD Repeat Domain Containing 7) • KMT2C (Lysine Methyltransferase 2C) • FAT1 (FAT atypical cadherin 1) • EP300 (E1A binding protein p300) • CASP8 (Caspase 8)
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    TP53 mutation • KRAS mutation • PIK3CA mutation • ARID1A mutation • STK11 mutation
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    Herceptin (trastuzumab) • everolimus • Piqray (alpelisib)
    2ms
    A Phase ll, Interventional, Single-arm Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib and Fulvestrant in Chinese Patients With PIK3CA-mutant, HR-positive, HER2-negative Locally Advanced or Metastatic Breast Cancer. (clinicaltrials.gov)
    P2, N=160, Not yet recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University
    New P2 trial
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor)
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    ER positive • HER-2 negative • PIK3CA mutation
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    Kisqali (ribociclib) • fulvestrant • Itovebi (inavolisib)