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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:
    1d
    Personalized Targeted IMMUNOtherapy-based Regimens in Recurrent GASTric Adenocarcinoma (IMMUNOGAST) (clinicaltrials.gov)
    P2, N=54, Completed, Hospices Civils de Lyon | Unknown status --> Completed | Trial completion date: Oct 2023 --> Jun 2026 | Trial primary completion date: Oct 2023 --> Jun 2026
    Trial completion • Trial completion date • Trial primary completion date • Tumor mutational burden
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 overexpression
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • ipatasertib (RG7440)
    2d
    From 2D to 3D Bioprinted In Vitro Breast Cancer Model: A Comparative Study of Proliferation, Tissue Structure, and mTOR Signaling. (PubMed, MedComm (2020))
    In addition, mTOR pathway activity and responsiveness to mTOR inhibitors (rapamycin and ipatasertib) and chemotherapeutic agents (cisplatin) were assessed. Compared with 2D monolayer cultures, 3D TMSs exhibited reduced mTOR signaling activity, which led to significantly decreased sensitivity to mTOR inhibition. These findings indicate that 3D bioprinted breast cancer models recapitulate key structural and signaling features of in situ tumors more accurately than 2D systems, highlighting their potential value for preclinical drug testing and mechanistic studies.
    Preclinical • Journal
    |
    CTNNB1 (Catenin (cadherin-associated protein), beta 1) • CDH1 (Cadherin 1) • CDH2 (Cadherin 2)
    |
    cisplatin • ipatasertib (RG7440)
    22d
    All Screens Lead to Polo-like kinase 1: A Central Node in Cancer Therapeutics and Resistance. (PubMed, Pharmacol Res)
    Emerging evidence supports synergistic potential of new-generation PLK1 inhibitors, such as Onvansertib, with chemo- and immune-therapies. This mini-review and perspective present current insights on PLK1 overexpression and its mechanistic impact on cancer aggressiveness and therapy resistance. We highlight the need for refined patient stratification and innovative combination regimens to exploit PLK1 inhibition in cancer treatment.
    Review • Journal
    |
    PLK1 (Polo Like Kinase 1)
    |
    Lynparza (olaparib) • cisplatin • carboplatin • gemcitabine • paclitaxel • 5-fluorouracil • Piqray (alpelisib) • irinotecan • ipatasertib (RG7440) • volasertib (NBL-001) • leucovorin calcium • onvansertib (PCM-075) • Estybon (rigosertib) • BI2536 • BAL0891 • GSK461364 • thiostrepton (RSO-021)
    29d
    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, Terminated, Hoffmann-La Roche | Completed --> Terminated; Study was closed early as the sponsor decided not to continue development of certain treatment combinations.
    Trial termination
    |
    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)
    1m
    BARBICAN: Investigate the Contribution of Ipatasertib to Neoadjuvant Chemotherapy Plus Atezolizumab in TNBC (clinicaltrials.gov)
    P2, N=146, Active, not recruiting, Queen Mary University of London | Trial completion date: Jan 2026 --> Aug 2026 | Trial primary completion date: Jan 2021 --> Aug 2026
    Trial completion date • Trial primary completion date
    |
    Tecentriq (atezolizumab) • paclitaxel • doxorubicin hydrochloride • cyclophosphamide • ipatasertib (RG7440)
    1m
    Safety and antitumour activity of ipatasertib combined with endocrine therapy and a CDK4/6 inhibitor in HR+/HER2- metastatic breast cancer (TAKTIC): a single-centre, open-label, phase 1b trial. (PubMed, Lancet Oncol)
    The combination of fulvestrant, ipatasertib, and palbociclib showed preliminary signs of clinical activity and showed expected adverse events in heavily pretreated patients with HR+/HER2- metastatic breast cancer, warranting further evaluation in those with CDK4/6 inhibitor-refractory disease.
    P1 data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • fulvestrant • letrozole • ipatasertib (RG7440) • anastrozole • exemestane
    1m
    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=56 --> 792
    Enrollment change
    |
    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • carboplatin • gemcitabine • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • Verzenio (abemaciclib) • albumin-bound paclitaxel • Kisqali (ribociclib) • fulvestrant • eribulin mesylate • letrozole • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Itovebi (inavolisib) • Actemra IV (tocilizumab) • atirmociclib (PF-07220060) • ladiratuzumab vedotin (SGN-LIV1A) • selicrelumab (RG7876)
    1m
    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)
    2ms
    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)
    2ms
    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)
    2ms
    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)
    2ms
    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)