^
    2d
    A Study to Compare the Blood Levels and Safety of Tazemetostat in Participants With Advanced Cancer and Moderate/Severe Liver Impairment to Participants With Advanced Cancer and Normal Liver Function (clinicaltrials.gov)
    P1, N=24, Recruiting, Epizyme, Inc. | Trial primary completion date: Dec 2025 --> Mar 2026
    Trial primary completion date
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    Tazverik (tazemetostat)
    2d
    Evaluate the Safety and Clinical Activity of HH2853 (clinicaltrials.gov)
    P1/2, N=254, Recruiting, Haihe Biopharma Co., Ltd. | Trial completion date: Dec 2025 --> Dec 2028 | Trial primary completion date: Dec 2025 --> Dec 2027
    Trial completion date • Trial primary completion date • First-in-human
    |
    ARID1A (AT-rich interaction domain 1A) • BAP1 (BRCA1 Associated Protein 1)
    |
    ARID1A mutation • EZH2 mutation
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    HH2853
    2d
    Mandolin: A Study to Assess Efficacy and Safety of Oral Tazemetostat in Adult Participants With Relapsed/Refractory Follicular Lymphoma That Does Not Have an "EZH2 Gain-of-function" Genetic Mutation (clinicaltrials.gov)
    P2, N=0, Withdrawn, Epizyme, Inc. | N=55 --> 0 | Not yet recruiting --> Withdrawn
    Enrollment change • Trial withdrawal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
    |
    EZH2 mutation
    |
    Tazverik (tazemetostat)
    3d
    Clinical Study on the Efficacy and Safety of Zeprumetostat, Azacitidine Combined with Lipo-MIT in Relapsed/Refractory Peripheral T-Cell Lymphoma. (ChiCTR2600116686)
    P2, N=26, Not yet recruiting, The First Affiliated Hospital of Soochow University; The First Affiliated Hospital of Soochow University
    New P2 trial
    |
    azacitidine • zeprumetostat (SHR-2554) • Duoenda (mitoxantrone liposomal)
    4d
    The Therapeutic Effect of EZH2 Inhibitors in Targeting Human Papillomavirus Associated Cervical Cancer. (PubMed, Curr Issues Mol Biol)
    In summary, both EZH2 inhibitors showed therapeutic potential in comparison to cisplatin based on cellular and molecular readouts. Additionally, EPZ6438 showed a greater efficacy and higher sensitivity towards HPV+ cells, which was further supported by preliminary in vivo results from the chorioallantoic membrane assay.
    Journal
    |
    TP53 (Tumor protein P53) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
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    cisplatin • Tazverik (tazemetostat)
    6d
    OLFML2A mediates cell cycle regulation in triple-negative breast cancer via EZH2. (PubMed, Front Oncol)
    Rescue experiments using the EZH2 inhibitor GSK126 assessed the functional output of the OLFML2A-EZH2 axis via CCK-8, EdU assays...Comprehensive proteomic and molecular biology analyses further indicated that OLFML2A may play a role in cell cycle regulation through the modulation of EZH2. Our findings suggest that OLFML2A may facilitate cell cycle progression by regulating EZH2, implicating it as a potential therapeutic target for triple-negative breast cancer.
    Journal
    |
    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
    |
    GSK2816126
    6d
    Zeprumetostat, Azacitidine Combined With Lipo-MIT in R/R PTCL (clinicaltrials.gov)
    P2, N=26, Recruiting, The First Affiliated Hospital of Soochow University
    New P2 trial
    |
    azacitidine • zeprumetostat (SHR-2554) • Duoenda (mitoxantrone liposomal)
    7d
    EZH2 Inhibitor, Tulmimetostat, and PD-1 Blockade for Treatment of Advanced Non-small Cell Lung Cancer (clinicaltrials.gov)
    P1/2, N=66, Recruiting, VA Office of Research and Development | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Keytruda (pembrolizumab) • tulmimetostat (DZR123)
    7d
    Testing the Addition of the Anti-cancer Drug, Tazemetostat, to the Usual Treatment (Dabrafenib and Trametinib) for Metastatic Melanoma That Has Progressed on the Usual Treatment (clinicaltrials.gov)
    P1/2, N=16, Active, not recruiting, National Cancer Institute (NCI) | N=58 --> 16 | Trial completion date: Nov 2025 --> Jan 2027
    Enrollment change • Trial completion date
    |
    BRAF V600E • BRAF V600 • BRAF V600K • EZH2 mutation
    |
    Guardant360® CDx
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Tazverik (tazemetostat)
    13d
    Epcoritamab and Tazemetostat for the Treatment of Relapsed or Refractory Grade I-IIIa Follicular Lymphoma (clinicaltrials.gov)
    P2, N=33, Suspended, City of Hope Medical Center | Recruiting --> Suspended
    Trial suspension
    |
    Tazverik (tazemetostat) • Epkinly (epcoritamab-bysp)
    14d
    Regulation of ferroptosis in colorectal cancer through therapeutic modulation and miRNA targeting. (PubMed, Biochem Biophys Rep)
    Interestingly, we also found that medications such as prasterone, tazemetostat, isoxyl, gemcitabine, ponsegromab, scx-2023, and nicotinamide could potentially be used in combination with the identified miRNAs to target ferroptosis in CRC. To further validate the stability and reliability of the predicted protein-ligand interactions, molecular dynamics (MD) simulations and MM-PBSA analyses were performed on selected top-ranking complexes, which confirmed their stable and favorable binding and supported the robustness of our docking results. These findings suggest that targeting these miRNAs and their associated genes, along with using the identified drugs, could be a promising strategy for CRC treatment, leveraging the potential of ferroptosis-inducing therapies.
    Journal • PARP Biomarker
    |
    PARP1 (Poly(ADP-Ribose) Polymerase 1) • RRM2 (Ribonucleotide Reductase Regulatory Subunit M2) • SLC7A11 (Solute Carrier Family 7 Member 11) • MIR16 (MicroRNA 16) • MIR15A (MicroRNA 15a) • MIR423 (MicroRNA 423) • MIR93 (MicroRNA 93)
    |
    gemcitabine • Tazverik (tazemetostat) • ponsegromab (PF-06946860)
    14d
    Phase 1b Study of EZH1/2 Inhibitor Valemetostat in Combination With Trastuzumab Deruxtecan in Subjects With HER2 Low/Ultra-low/Null Metastatic Breast Cancer (clinicaltrials.gov)
    P1, N=17, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting | N=37 --> 17
    Enrollment closed • Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
    |
    PATHWAY antiHer2/neu (4B5) Rabbit Monoclonal Primary Antibody
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • Ezharmia (valemetostat)