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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:
    5d
    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)
    13d
    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)
    22d
    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)
    1m
    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)
    2ms
    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)
    3ms
    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)
    4ms
    MYBL2 regulates the expression of CENPF in lung adenocarcinoma and promotes tumor development and metastasis through AKT pathway activation. (PubMed, Eur J Med Res)
    The expression of MYBL2 and CENPF in lung adenocarcinoma increases with LUAD progression. MYBL2 regulates the expression of CENPF in LUAD, and the elevated CENPF promotes the proliferation and migration of LUAD cells. Both MYBL2 and CENPF regulate the proliferation and migration of LUAD through AKT pathway activation.
    Journal
    |
    MYBL2 (MYB Proto-Oncogene Like 2) • CENPF (Centromere Protein F)
    |
    ipatasertib (RG7440)
    4ms
    Morpheus Lung: A Study Of Multiple Immunotherapy-Based Treatment Combinations In Participants With Metastatic Non-Small Cell Lung Cancer (Morpheus- Non-Small Cell Lung Cancer) (clinicaltrials.gov)
    P1/2, N=314, Completed, Hoffmann-La Roche | Active, not recruiting --> Completed
    Trial completion
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • carboplatin • gemcitabine • docetaxel • Cotellic (cobimetinib) • pemetrexed • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • Repatha (evolocumab) • camonsertib (RP-3500) • cibisatamab (RG7802) • ciforadenant (CPI-444) • zanzalintinib (XL092)
    4ms
    Addition of ipatasertib to dual anti-HER2 maintenance therapy in HER2-positive metastatic breast tumors with PIK3CA mutations: the phase 1b SOLTI-1507 IPATHER trial. (PubMed, Clin Cancer Res)
    These results support ipatasertib plus HP as a safe and promising maintenance strategy for HER2-positive breast tumors harboring PIK3CAmut.
    P1 data • Journal
    |
    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) • ipatasertib (RG7440)
    4ms
    Morpheus-TNBC: A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer (clinicaltrials.gov)
    P1/2, N=792, Recruiting, Hoffmann-La Roche | N=580 --> 792 | Trial completion date: May 2028 --> Sep 2030 | Trial primary completion date: May 2028 --> Sep 2030
    Enrollment change • Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression • PIK3CA mutation
    |
    VENTANA PD-L1 (SP142) Assay
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • carboplatin • gemcitabine • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • Verzenio (abemaciclib) • albumin-bound paclitaxel • Kisqali (ribociclib) • fulvestrant • Halaven (eribulin mesylate) • letrozole • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Itovebi (inavolisib) • Actemra IV (tocilizumab) • atirmociclib (PF-07220060) • ladiratuzumab vedotin (SGN-LIV1A) • selicrelumab (RG7876)