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    DRUG:

    ipatasertib (RG7440)

    i
    Other names: RG7440, GDC-0068 , GCD 0068, RG-7440, RO5532961
    Company:
    Pfizer, Roche
    Drug class:
    PI3K inhibitor, AKT inhibitor
    Related drugs:
    3d
    Phase I trial of Ipatasertib plus Atezolizumab enhances PI3K/AKT pathway immune responses in solid tumors and refractory glioblastoma. (PubMed, Clin Cancer Res)
    This is the first report in clinical samples showing that ipatasertib efficiently depletes FOXP3+ regulatory T cells and results in increased infiltration of effector CD8+ T cells in the tumor microenvironment. This was associated with preliminary efficacy in a subset of patients with treatment-refractory glioblastoma (GBM).
    P1 data • Journal
    |
    CD8 (cluster of differentiation 8) • FOXP3 (Forkhead Box P3)
    |
    Tecentriq (atezolizumab) • ipatasertib (RG7440)
    12d
    NCI-2021-13901: Testing the Addition of Ipatasertib to Usual Chemotherapy and Radiation for Head and Neck Cancer (clinicaltrials.gov)
    P1, N=46, Recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2026 --> Jul 2027 | Trial primary completion date: Jun 2026 --> Jul 2027
    Trial completion date • Trial primary completion date
    |
    cisplatin • ipatasertib (RG7440)
    15d
    FAIM: Fulvestrant, Ipatasertib and CDK4/6 Inhibition in Metastatic ER+/HER2- Breast Cancer Patients Without ctDNA Suppression (clinicaltrials.gov)
    P2, N=57, Active, not recruiting, Royal Marsden NHS Foundation Trust | Recruiting --> Active, not recruiting | N=324 --> 57 | Trial completion date: Sep 2026 --> Jun 2027 | Trial primary completion date: Sep 2026 --> Jun 2027
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Circulating tumor DNA
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 positive • ER positive • HER-2 negative • ER positive + HER-2 negative • HER-2 negative + ER positive
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • ipatasertib (RG7440) • Pegasys (pegylated interferon α -2a)
    16d
    UmbrellaMAX: A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study (clinicaltrials.gov)
    P3, N=100, Recruiting, Hoffmann-La Roche | N=23 --> 100
    Enrollment change
    |
    Avastin (bevacizumab) • Rozlytrek (entrectinib) • ipatasertib (RG7440) • divarasib (RG6330) • Itovebi (inavolisib) • tiragolumab (RG6058)
    27d
    Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study (clinicaltrials.gov)
    P2, N=920, Active, not recruiting, Hoffmann-La Roche | Recruiting --> Active, not recruiting
    Enrollment closed • Tumor mutational burden • IO biomarker • Pan tumor
    |
    BRAF (B-raf proto-oncogene)
    |
    Tecentriq (atezolizumab) • Rozlytrek (entrectinib) • Alecensa (alectinib) • Kadcyla (ado-trastuzumab emtansine) • Gavreto (pralsetinib) • ipatasertib (RG7440) • belvarafenib (RG6185) • divarasib (RG6330) • Itovebi (inavolisib) • camonsertib (RP-3500)
    1m
    Personalized Targeted IMMUNOtherapy-based Regimens in Recurrent GASTric Adenocarcinoma (IMMUNOGAST) (clinicaltrials.gov)
    P2, N=60, Active, not recruiting, Hospices Civils de Lyon | Recruiting --> Active, not recruiting
    Enrollment closed • Tumor mutational burden
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 overexpression
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • ipatasertib (RG7440)
    1m
    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
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor)
    |
    HER-2 positive • PIK3CA mutation
    |
    Herceptin (trastuzumab) • Perjeta (pertuzumab) • ipatasertib (RG7440)
    2ms
    EAY131-Z1K: Testing Ipatasertib as Potentially Targeted Treatment in Cancers With AKT Genetic Changes (MATCH - Subprotocol Z1K) (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Jan 2027
    Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
    |
    BRAF mutation • HRAS mutation
    |
    ipatasertib (RG7440)
    3ms
    Reactive Oxygen Species Drive Cell Migration and PD-L1 Expression via YB-1 Phosphorylation in Pleural Mesothelioma. (PubMed, Antioxidants (Basel))
    The pharmacological inhibition of AKT (ipatasertib), MEK (trametinib), and RSK (BI-D1870) resulted in the reversal of ROS-induced effects, with the strongest effects observed upon the inhibition of YB-1 phosphorylation by BI-D1870. The results suggest that ROS exposure has a strong impact on cell migration and immune evasion not only in PM cells but also in mesothelial cells, from which PM arises. Interfering with ROS-responsive kinase pathways, particularly YB-1 phosphorylation, could counteract pro-migratory and immune-evasive effects in PM.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • PD-L2 (Programmed Cell Death 1 Ligand 2)
    |
    PD-L1 expression
    |
    Mekinist (trametinib) • ipatasertib (RG7440)
    4ms
    UmbrellaMAX: A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study (clinicaltrials.gov)
    P3, N=100, Recruiting, Hoffmann-La Roche | N=60 --> 100
    Enrollment change
    |
    Avastin (bevacizumab) • Rozlytrek (entrectinib) • ipatasertib (RG7440) • divarasib (RG6330) • Itovebi (inavolisib) • tiragolumab (RG6058)
    4ms
    Study of Chemotherapy Plus Ipatasertib for People With Solid Tumors With PTEN/AKT Mutations, A ComboMATCH Treatment Trial (clinicaltrials.gov)
    P2, N=33, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension
    |
    AKT2 (V-akt murine thymoma viral oncogene homolog 2)
    |
    AKT1 mutation
    |
    paclitaxel • ipatasertib (RG7440)
    4ms
    MORPHEUS BC: A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer (clinicaltrials.gov)
    P1/2, N=316, Recruiting, Hoffmann-La Roche | Trial completion date: Nov 2027 --> May 2029 | Trial primary completion date: Nov 2027 --> May 2029
    Trial completion date • Trial primary completion date
    |
    ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
    |
    HER-2 positive • ER positive
    |
    Herceptin (trastuzumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • ipatasertib (RG7440) • Itovebi (inavolisib) • giredestrant (RG6171) • Pegasys (pegylated interferon α -2a) • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) • samuraciclib (CT7001)