^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    PP2A inhibitor

    Related drugs:
    17d
    The protein phosphatase 2A-B56α complex regulates N-Myc degradation in neuroblastoma. (PubMed, J Biol Chem)
    Treatment with DT-061 combined with its inactive competitive antagonist, DT-766, and the proteasome inhibitor, MG-132, reversed this effect on the loss of N-Myc protein expression, suggesting that PP2A-B56α modulation affects N-Myc stability via the proteasomal degradation pathway. In a xenograft model, we observed tumor growth inhibition upon DT-061 treatment, along with a reduction in N-Myc protein expression in vivo. Combined, these results highlight the importance of the PP2A tumor suppressor in regulating MYCN oncogenic signaling and open new potential treatment regimens for high-risk neuroblastoma patients.
    Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor)
    |
    MYCN amplification
    |
    DT-061 • MG132
    1m
    First-in-human Phase I to Evaluate PEP-010 as Single Agent and in Combination With Paclitaxel or With Gemcitabine (CleverPeptide) (clinicaltrials.gov)
    P1, N=57, Active, not recruiting, Institut Curie | Recruiting --> Active, not recruiting | N=101 --> 57 | Trial completion date: Dec 2025 --> Jan 2027 | Trial primary completion date: Nov 2025 --> Dec 2026
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • First-in-human
    |
    gemcitabine • paclitaxel • PEP-010
    2ms
    Safety and Efficacy of Targeting PP2A in Ovarian Clear Cell Carcinoma Using Dostarlimab and LB-100 (clinicaltrials.gov)
    P1/2, N=21, Recruiting, M.D. Anderson Cancer Center | Trial completion date: Jan 2026 --> Oct 2027 | Trial primary completion date: Jan 2026 --> Oct 2027
    Trial completion date • Trial primary completion date
    |
    CD4 (CD4 Molecule)
    |
    Jemperli (dostarlimab-gxly) • LB-100
    5ms
    First-in-human Phase I to Evaluate PEP-010 as Single Agent and in Combination With Paclitaxel or With Gemcitabine (CleverPeptide) (clinicaltrials.gov)
    P1, N=101, Recruiting, Institut Curie | Trial primary completion date: Jul 2025 --> Nov 2025
    Trial primary completion date • First-in-human
    |
    gemcitabine • paclitaxel • PEP-010
    6ms
    Synergistic Efficacy of Chidamide and LB100 in Sézary Syndrome via TNC Downregulation and PI3K/AKT/mTOR Dephosphorylation. (PubMed, Cancer Sci)
    This study also preliminarily validated the effect of the combination of the two drugs on other subtypes of CTCL. Overall, these findings provide potential new therapeutic strategies for CTCL (especially SS), although further clinical evaluation is required to validate these results.
    Journal
    |
    ANXA5 (Annexin A5)
    |
    Epidaza (chidamide) • LB-100
    7ms
    Canagliflozin inhibits hepatic stellate cells activation and proliferation by inhibiting PP2A-mediated β-catenin dephosphorylation to attenuate hepatic fibrosis. (PubMed, Int Immunopharmacol)
    In conclusion, our study indicates that Canagliflozin ameliorate HF via inhibiting PP2A-mediated dephosphorylation of β-catenin in HSCs. The inhibition of PP2A in HSCs may represent a potential therapeutic target not only for cancer treatment but also for the management of HF.
    Journal
    |
    CTNNB1 (Catenin (cadherin-associated protein), beta 1)
    10ms
    A PP2A-mtATR-tBid axis links DNA damage-induced CIP2A degradation to apoptotic dormancy and therapeutic resistance in PDAC. (PubMed, Cancer Lett)
    We found that in gemcitabine-resistant pancreatic ductal adenocarcinoma (PDAC) cells, CIP2A degradation via ubiquitination enhanced PP2A phosphatase activity, leading to the dephosphorylation of ATR at Ser428 in the cytoplasm...These findings reveal a novel mechanism of resistance to DNA damage-based cancer drugs and introduce a new action mechanism of LB-100, which works through mtATR-tBid complex-mediated apoptotic dormancy triggered by CIP2A degradation-mediated PP2A activation. Disrupting the mtATR-tBid complex may represent a promising strategy to restore or sensitize resistant cancer cells to apoptosis.
    Journal
    |
    CIP2A (Cellular Inhibitor Of PP2A)
    |
    gemcitabine • LB-100
    12ms
    Enhancer: Phase I/II of LB-100 Plus Doxorubicin Vs. Doxorubicin Alone in First Line of Advanced Soft Tissue Sarcomas (clinicaltrials.gov)
    P1/2, N=152, Active, not recruiting, Grupo Espanol de Investigacion en Sarcomas | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    doxorubicin hydrochloride • LB-100
    12ms
    NLRP4 unlocks an NK/macrophages-centered ecosystem to suppress non-small cell lung cancer. (PubMed, Biomark Res)
    Altogether, we delineated NLRP4's unexplored facets and discovered an NLRP4-driven anti-tumor ecosystem composed of TIGIT+TNFA+ NK and iNOS+ M1. Finally, targeting PP2A by its inhibitor successfully mimicked the anti-tumor capacity of the overexpression of NLRP4.
    Journal • IO biomarker
    |
    TNFA (Tumor Necrosis Factor-Alpha) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2) • CXCR2 (Chemokine (C-X-C motif) receptor 2) • LRP4 (LDL Receptor Related Protein 4)
    |
    LB-100
    1year
    Exploratory Study on the Sensitization Effect of PP2A Inhibitor (Norcantharidin) Combined with PD-1 Inhibitor in the Treatment of Solid Tumors (ChiCTR2400094682)
    P=N/A, N=46, Shanghai Tongren Hospital; Shanghai Tongren Hospital
    New trial
    |
    PD-L1 (Programmed death ligand 1) • TMB (Tumor Mutational Burden)
    |
    PD-L1 expression
    1year
    First-in-human Phase I to Evaluate PEP-010 As Single Agent and in Combination with Paclitaxel or with Gemcitabine (CleverPeptide) (clinicaltrials.gov)
    P1, N=101, Recruiting, Institut Curie | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Jul 2025
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    gemcitabine • paclitaxel • PEP-010