^
    3d
    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
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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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    HER-2 negative • PIK3CA mutation
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    Ibrance (palbociclib) • fulvestrant • Itovebi (inavolisib)
    4d
    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)
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    risovalisib (CYH33)
    4d
    Discovery of a novel PI3Kα inhibitor for breast cancer therapy via virtual screening method, molecular dynamics simulation and biological evaluation. (PubMed, J Mol Graph Model)
    In vitro cytotoxicity assays were then performed in MCF-7 and MDA-MB-231 breast cancer cell lines, with alpelisib as a reference compound. Hit 2 reduced cell viability in both cell lines, but its effect was particularly pronounced in MDA-MB-231 cells, a model of triple-negative breast cancer (TNBC). These results suggest that Hit 2 represents a promising natural scaffold for further design and development in breast cancer therapy, with particular relevance for aggressive TNBC.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    Piqray (alpelisib)
    4d
    InavoPC: A Study to Test Inavolisib Treatment in Participants With Metastatic Castration-Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=100, Recruiting, Hoffmann-La Roche | Not yet recruiting --> Recruiting
    Enrollment open
    |
    FoundationOne® CDx
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • Itovebi (inavolisib)
    7d
    EPIK-B6: Study Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant in Japanese Men and Postmenopausal Women With Advanced Breast Cancer (clinicaltrials.gov)
    P2, N=24, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Jul 2026 --> Jan 2027 | Trial primary completion date: Jun 2026 --> Jan 2027
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 negative • PIK3CA mutation
    |
    Piqray (alpelisib) • fulvestrant
    11d
    Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations (clinicaltrials.gov)
    P2, N=7, Terminated, M.D. Anderson Cancer Center | Trial completion date: Feb 2027 --> Dec 2025 | Active, not recruiting --> Terminated; Copanlisib development was discontinued by Bayer following withdrawal of copanlisib in relapsed follicular lymphoma in November 2023.
    Trial completion date • Trial termination
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • PI3K (Phosphoinositide 3-kinases)
    |
    PIK3CA mutation • PTEN deletion
    |
    fulvestrant • Aliqopa (copanlisib)
    12d
    INAVO-CRC: A Study to Evaluate the Efficacy and Safety of Inavolisib When Administered in Combination With Bevacizumab and FOLFOX or FOLFIRI as First Line Therapy in Participants With Colorectal Cancer (clinicaltrials.gov)
    P2, N=164, Not yet recruiting, Hoffmann-La Roche
    New P2 trial
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Avastin (bevacizumab) • 5-fluorouracil • irinotecan • leucovorin calcium • Itovebi (inavolisib)
    13d
    Copanlisib Plus Venetoclax in R/R DLBCL (clinicaltrials.gov)
    P1/2, N=48, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Apr 2026 --> Jul 2026 | Trial primary completion date: Apr 2026 --> Jul 2025
    Trial completion date • Trial primary completion date
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
    |
    Venclexta (venetoclax) • Aliqopa (copanlisib)
    13d
    Cost-effectiveness of inavolisib plus palbociclib-fulvestrant versus palbociclib plus fulvestrant as first-line treatment in HR+/HER2-advanced breast cancer. (PubMed, Breast)
    Compared with palbociclib-fulvestrant, the inavolisib triple regimen is not cost-effective at its current price. A substantial price reduction or careful selection of the target patient may be required for the regimen to be economically viable.
    Journal • HEOR • Cost-effectiveness
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation
    |
    Ibrance (palbociclib) • fulvestrant • Itovebi (inavolisib)
    15d
    Design and Synthesis of Thiadiazole Derivatives as Dual EGFR/COX‑2 Inhibitors with Anticancer and Anti-inflammatory Activities. (PubMed, ACS Omega)
    In this study, 20 new compounds with thiadiazole structures were synthesized based on Alpelisib...For compounds 3j and 3o, further activity studies, molecular docking, and molecular dynamics studies were performed. The compounds' EGFR and COX-2 inhibitory potential was investigated.
    Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    Piqray (alpelisib)
    17d
    BTCRC-BRE19-409: Alpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=44, Active, not recruiting, Marina N Sharifi | Trial completion date: Jan 2026 --> May 2026 | Recruiting --> Active, not recruiting
    Enrollment closed • Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HER-2 amplification • HER-2 negative • PIK3CA mutation
    |
    Piqray (alpelisib) • fulvestrant
    18d
    Inavolisib-Based Therapy for PIK3CA-Mutated Advanced Male Breast Cancer: A Cost-Effectiveness Analysis. (PubMed, Breast Cancer (Dove Med Press))
    A lifetime Markov model was developed from a US payer perspective to evaluate the cost-effectiveness of inavolisib plus palbociclib and fulvestrant versus placebo plus palbociclib and fulvestrant in men with PIK3CA-mutated advanced breast cancer. Inavolisib-based therapy is not cost-effective for treating PIK3CA-mutated advanced male breast cancer at its current price. Significant price reductions or adjustments to value assessment frameworks are required to ensure equitable access for this underserved population.
    Journal • HEOR • Cost-effectiveness
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HR positive • HER-2 negative • PIK3CA mutation
    |
    Ibrance (palbociclib) • fulvestrant • Itovebi (inavolisib)