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    DRUG:

    uprosertib (LAE003)

    i
    Other names: UPB 795, GSK795, GSK 795, GSK-2141795, GSK2141795, UPB795, LAE-003, UPB-795, LAE 003, LAE003, GSK 2141795C, GSK-795, GSK 2141795
    Company:
    Laekna Therap, Novartis
    Drug class:
    AKT inhibitor
    Related drugs:
    1m
    SWOG-S1221: Uprosertib, Dabrafenib, and Trametinib in Treating Patients With Stage IIIC-IV Cancer (clinicaltrials.gov)
    P1/2, N=27, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Oct 2024 --> Oct 2025
    Trial completion date • Combination therapy
    |
    BRAF mutation • BRAF V600 • RAS mutation
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • uprosertib (LAE003)
    1year
    SWOG-S1221: Uprosertib, Dabrafenib, and Trametinib in Treating Patients With Stage IIIC-IV Cancer (clinicaltrials.gov)
    P1/2, N=27, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Oct 2023 --> Oct 2024
    Trial completion date • Combination therapy
    |
    BRAF mutation • BRAF V600 • RAS mutation
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • uprosertib (LAE003)
    over1year
    Comprehensive analysis of angiogenesis pattern and related immune landscape for individual treatment in osteosarcoma. (PubMed, NPJ Precis Oncol)
    OS patients with high ANGscore might be resistant to uprosertib, and be sensitive to VE821, AZD6738 and BMS.345541. In conclusion, we established a novel ANGscore system by comprehensively analysing the expression pattern of angiogenesis genes, which can accurately differentiate the prognosis and immune characteristics of OS populations. Additionally, the ANGscore can be used for patient stratification during immunotherapy, and guide individualized treatment strategies.
    Journal • IO biomarker
    |
    IFNG (Interferon, gamma)
    |
    ceralasertib (AZD6738) • VE-821 • uprosertib (LAE003)
    almost3years
    Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P2, N=25, Completed, National Cancer Institute (NCI) | Active, not recruiting --> Completed
    Trial completion
    |
    BRAF (B-raf proto-oncogene)
    |
    Mekinist (trametinib) • uprosertib (LAE003)
    over3years
    RNF43 and PWWP2B inhibit cancer cell proliferation and are predictive or prognostic biomarker for FDA-approved drugs in patients with advanced gastric cancer. (PubMed, J Cancer)
    Our data demonstrated that RNF43 and PWWP2B are a biomarker that predict recurrence of gastric cancer. Our findings suggest that docetaxel trihydrate, uprosertib and pelitinib could be used as novel therapeutic agents for the prevention and treatment of gastric cancer with a decrease in RNF43 and PWWP2B expression.
    Clinical • FDA event • Journal
    |
    RNF43 (Ring Finger Protein 43)
    |
    docetaxel • uprosertib (LAE003)
    4years
    Phase I dose-escalation trial of the oral AKT inhibitor uprosertib in combination with the oral MEK1/MEK2 inhibitor trametinib in patients with solid tumors. (PubMed, Cancer Chemother Pharmacol)
    Continuous and intermittent dosing of trametinib in combination with uprosertib was not tolerated, and minimal clinical activity was observed in all schedules tested.
    Clinical • P1 data • Journal • Combination therapy
    |
    BRAF (B-raf proto-oncogene) • MAP2K2 (Mitogen-activated protein kinase kinase 2)
    |
    Mekinist (trametinib) • uprosertib (LAE003)
    4years
    Trametinib With or Without GSK2141795 in Treating Patients With Recurrent or Persistent Endometrial Cancer (clinicaltrials.gov)
    P1, N=26, Completed, National Cancer Institute (NCI) | Active, not recruiting --> Completed
    Clinical • Trial completion • Combination therapy
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    Mekinist (trametinib) • uprosertib (LAE003)
    4years
    Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P2, N=25, Active, not recruiting, National Cancer Institute (NCI) | N=74 --> 25
    Clinical • Enrollment change
    |
    BRAF (B-raf proto-oncogene)
    |
    Mekinist (trametinib) • uprosertib (LAE003)
    over4years
    Akt-targeted therapy as a promising strategy to overcome drug resistance in breast cancer - A comprehensive review from chemotherapy to immunotherapy. (PubMed, Pharmacol Res)
    Atezolizumab targeting the protein programmed cell death-ligand (PD-L1) in combination with paclitaxel was recently approved by the Food and Drug Administration (FDA) for Triple-Negative Breast Cancer (TNBC), the most incurable type of breast cancer...In addition, resistance to chemotherapy with drugs such as lapatinib, geftinib, and tamoxifen can develop...The Akt inhibitors ipatasertib, capivasertib, uprosertib, and MK-2206 not only suppress cancer cell proliferation and metastasis, but may also inhibit cytokine regulation and PD-L1 expression. Ipatasertib and uprosertib are undergoing clinical investigation to treat TNBC. Inhibition of Akt and its regulators can be used to control breast cancer progression and also immunosuppression, while discovery of additional compounds that target Akt and its modulators could provide solutions to resistance to chemotherapy and immunotherapy.
    Review • Journal • PD(L)-1 Biomarker
    |
    PD-L1 (Programmed death ligand 1) • CTNNB1 (Catenin (cadherin-associated protein), beta 1)
    |
    PD-L1 expression
    |
    Tecentriq (atezolizumab) • paclitaxel • lapatinib • tamoxifen • Truqap (capivasertib) • MK-2206 • ipatasertib (RG7440) • uprosertib (LAE003)
    almost5years
    Trametinib With GSK2141795 in BRAF Wild-type Melanoma (clinicaltrials.gov)
    P2, N=20, Completed, Adil Daud | Active, not recruiting --> Completed
    Clinical • Trial completion
    |
    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    BRAF mutation • NRAS mutation
    |
    Mekinist (trametinib) • uprosertib (LAE003)
    almost5years
    Biospecimen Collection in Assessing the Effect of Trametinib With or Without Uprosertib on Biomarkers in Patients With Persistent or Recurrent Endometrial Cancer Enrolled on Trial GOG02290 (clinicaltrials.gov)
    P2, N=40, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed
    Clinical • Trial completion • Combination therapy
    |
    BRAF (B-raf proto-oncogene)
    |
    Mekinist (trametinib) • uprosertib (LAE003)
    almost5years
    Biospecimen Collection in Assessing the Effect of Trametinib With or Without Uprosertib on Biomarkers in Patients With Persistent or Recurrent Endometrial Cancer Enrolled on Trial GOG02290 (clinicaltrials.gov)
    P2, N=40, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Aug 2019 --> Jan 2020 | Trial primary completion date: Aug 2019 --> Jan 2020
    Clinical • Trial completion date • Trial primary completion date • Combination therapy
    |
    BRAF (B-raf proto-oncogene)
    |
    Mekinist (trametinib) • uprosertib (LAE003)