^
    1d
    PI3K inhibition in combination with tamoxifen in patients with metastatic HR+/HER2- breast cancer: clinical and circulating tumor DNA results. (PubMed, Clin Cancer Res)
    Our findings suggest efficacy of PI3K inhibition + tamoxifen beyond second-line treatment and after prior targeted therapies, including CDK4/6 inhibition in metastatic HR+/HER2- breast cancer although the magnitude of benefit did not outweigh the tolerability of this combination. Exploratory biomarker analysis indicates that tumor fraction determined in ctDNA differentiates patients based on prognosis and may help to optimize patient selection for targeted treatment strategies.
    Journal • Circulating tumor DNA
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    HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 negative
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    everolimus • tamoxifen • taselisib (GDC-0032)
    1d
    Ossifying fibromyxoid tumor with a novel PIK3CA mutation (c.1624G>A) unresponsive to alpelisib: A case report. (PubMed, Respir Med Case Rep)
    Based on the findings, the patient opted for off-label therapy with alpelisib, an α-specific PI3K inhibitor that selectively targets p110α and has shown promising efficacy in breast cancer patients harboring the identical PIK3CA mutations. However, no clinical response was observed in the patient, and the lack of response may be associated with the specific nature of the PIK3CA mutation, and/or other unfavorable tumor biological factors that override any benefit from alpelisib.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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    PIK3CA mutation
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    Piqray (alpelisib)
    2d
    EPIK-B2: Study of Alpelisib (BYL719) in Combination With Trastuzumab and Pertuzumab as Maintenance Therapy in Patients With HER2-positive Advanced Breast Cancer With a PIK3CA Mutation (clinicaltrials.gov)
    P3, N=19, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Jun 2026 --> Feb 2027 | Trial primary completion date: Jun 2026 --> Feb 2027
    Trial completion 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)
    |
    HER-2 positive • PIK3CA mutation
    |
    Herceptin (trastuzumab) • Perjeta (pertuzumab) • Piqray (alpelisib)
    3d
    A Study to Evaluate the Efficacy and Safety of CYH33 in Patients With Recurrent/Persistent Ovary Clear Cell Carcinoma (clinicaltrials.gov)
    P2, N=93, Active, not recruiting, Haihe Biopharma Co., Ltd. | Completed --> Active, not recruiting | Trial completion date: Jul 2024 --> Feb 2026
    Enrollment closed • Trial completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    risovalisib (CYH33)
    7d
    A Window of Opportunity Study to Assess the Modulation of Biomarkers in Head and Neck Squamous Cell Cancer (HNSCC) By Preoperative Treatment With BYL719 (clinicaltrials.gov)
    P=N/A, N=15, Completed, London Health Sciences Centre Research Institute OR Lawson Research Institute of St. Joseph's | Active, not recruiting --> Completed
    Trial completion
    |
    Piqray (alpelisib)
    8d
    optINAVO: To Study the Effect of Inavolisib in Combination With Fulvestrant in Participants With Breast Cancer (clinicaltrials.gov)
    P2, N=80, Not yet recruiting, Hoffmann-La Roche
    New P2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CDK4 (Cyclin-dependent kinase 4)
    |
    HER-2 negative • PIK3CA mutation
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    fulvestrant • Itovebi (inavolisib)
    12d
    reaINAVO: A Study to Evaluate the Effectiveness and Safety of Inavolisib in Participants With Endocrine-resistant, PIK3CA-mutated, Hormone Receptor-positive, HER2-negative Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P=N/A, N=500, Recruiting, Hoffmann-La Roche | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation
    |
    Ibrance (palbociclib) • fulvestrant • Itovebi (inavolisib)
    13d
    Umbrella Trial of Subtype-Targeted Therapies in ER+/HER2- Breast Cancer (clinicaltrials.gov)
    P2, N=19, Completed, Jennifer Lee Caswell-Jin | Suspended --> Completed
    Trial completion
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 negative • HER-2 negative + ER positive
    |
    Piqray (alpelisib) • fulvestrant • zotatifin (eFT226) • Soltamox (tamoxifen citrate)
    15d
    Cost-effectiveness analysis of inavolisib combined with palbociclib plus fulvestrant in PIK3CA-mutated HR+/Her2- advanced breast cancer in China. (PubMed, Front Pharmacol)
    While inavolisib plus palbociclib-fulvestrant significantly prolongs PFS and OS in PIK3CA-mutated HR+/HER2- ABC/MBC, it is not cost-effective at current prices in China. Strategic price adjustments or reimbursement negotiations are essential to improve economic feasibility and inform clinical and policy decisions.
    Journal • HEOR • Cost-effectiveness
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    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    EGFR mutation • HR positive • HER-2 negative • PIK3CA mutation • EGFR positive
    |
    Ibrance (palbociclib) • fulvestrant • Itovebi (inavolisib)
    16d
    Angiogenic switching in cerebral cavernous malformations driven by MAP3K3-PIK3CA synergy. (PubMed, Brain)
    Treatment with the PI3Kα-selective inhibitor alpelisib suppressed lesion formation and reversed pro-angiogenic signaling in both mouse models and patient-derived cerebral cavernous malformations organoids. These findings uncover a convergent mechanism involving MAPK and PI3K pathway activation in cerebral cavernous malformations pathogenesis and demonstrate that PI3Kα inhibition may offer a viable therapeutic strategy for a disease that currently lacks effective pharmacological treatment.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Piqray (alpelisib)
    19d
    reaINAVO: A Study to Evaluate the Effectiveness and Safety of Inavolisib in Participants With Endocrine-resistant, PIK3CA-mutated, Hormone Receptor-positive, HER2-negative Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P=N/A, N=500, Not yet recruiting, Hoffmann-La Roche
    New trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation
    |
    Ibrance (palbociclib) • fulvestrant • Itovebi (inavolisib)
    19d
    Targeting intrinsic and CAF-mediated signaling by PI3Kα inhibitor CYH33 attenuated metastasis in lung squamous cell carcinoma. (PubMed, Acta Pharmacol Sin)
    Furthermore, CYH33 possessed potent activity against the growth of LUSC with hyperactivated PI3K signaling. Collectively, the dual-targeting of CYH33 that directly blocked PI3Kα in tumor cells and disrupted CAF-mediated pro-metastatic signaling supported PI3Kα inhibitors as a potential therapeutic approach for advanced LUSC.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • HGF (Hepatocyte growth factor)
    |
    risovalisib (CYH33)