^
    9d
    TulmiSTAR-02: A Phase I/II Open-label Study of Tulmimetostat in Combination With Darolutamide vs. Darolutamide, and Tulmimetostat With Abiraterone in Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC) (clinicaltrials.gov)
    P1/2, N=203, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
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    abiraterone acetate • Nubeqa (darolutamide) • tulmimetostat (DZR123)
    10d
    Prevention of cancer initiation by augmenting MHC-I antigen presentation via EZH2 inhibition. (PubMed, Oncogene)
    As EZH2 is highly expressed in numerous precancers, PPT@GSK126 has broad application prospects for reducing these tumor burdens. Schematic images presenting the mechanism of action regarding EZH2 in promoting MT of OLK into HNSCC via inhibiting MHC-I associated APM (left panel) and the proposed therapeutic strategy for preventing OLK carcinogenesis (right panel).
    Journal
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    CD8 (cluster of differentiation 8) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • B2M (Beta-2-microglobulin) • GZMB (Granzyme B) • HLA-B (Major Histocompatibility Complex, Class I, B) • TAP1 (Transporter 1) • HLA-C (Major Histocompatibility Complex, Class I, C)
    |
    GSK2816126
    10d
    A Study of Valemetostat (DS-3201b) in Combination With Darolutamide in Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov)
    P1, N=60, Not yet recruiting, Daiichi Sankyo
    New P1 trial
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    Nubeqa (darolutamide) • Ezharmia (valemetostat)
    13d
    Enhancing Triple-Negative Breast Cancer Radiotherapy via EZH2-Targeted Nanoplatform and Radionuclide Therapy. (PubMed, Mol Pharm)
    A cancer cell membrane (CCm)-camouflaged nanoplatform (CCm-HSA-Taz) was engineered to encapsulate the EZH2 inhibitor Tazemetostat (Taz), enabling tumor-targeted delivery...Nuclear medicine imaging revealed reduced tumor glucose metabolism and improved immune cell cytotoxicity. Utilizing components approved by the FDA suggests the potential for this strategy to be translated into clinical settings.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
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    Tazverik (tazemetostat)
    16d
    Phase II Clinical Study of SHR2554 Tablets Combined With Other Anti-tumor Treatments in Non-small Cell Lung Cancer Subjects (clinicaltrials.gov)
    P2, N=200, Recruiting, Jiangsu HengRui Medicine Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
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    retlirafusp alfa (SHR-1701) • zeprumetostat (SHR-2554) • SHR-A2102 • AiRuiLi (adebrelimab)
    17d
    A Study of SHR3680, HS-20093 and SHR2554 in Subjects With Prostate Cancer (clinicaltrials.gov)
    P2, N=218, Not yet recruiting, Jiangsu HengRui Medicine Co., Ltd.
    New P2 trial
    |
    abiraterone acetate • zeprumetostat (SHR-2554) • AiRuiEn (rezvilutamide) • GSK5764227
    20d
    C2321001: A Study of Mevrometostat for Treatment of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma (clinicaltrials.gov)
    P1, N=433, Recruiting, Pfizer | Trial completion date: Mar 2026 --> Mar 2029 | Trial primary completion date: Mar 2026 --> May 2028
    Trial completion date • Trial primary completion date
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    Xtandi (enzalutamide) • itraconazole • mevrometostat (PF-06821497)
    22d
    EZH2 Inhibition in Mesothelioma Cells Increases the Release of Extracellular Vesicles That Skew Neutrophils Toward a Protumor Phenotype. (PubMed, Int J Mol Sci)
    Moreover, we observed changes in the EV cargo derived from EZH2 inhibitor-treated spheroids. Our findings highlight the significant role of EVs in creating an immunosuppressive microenvironment, and underscore the urgent need for further investigation into the regulation of neutrophil biology and function in the PM.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • BAP1 (BRCA1 Associated Protein 1) • MSLN (Mesothelin)
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    Tazverik (tazemetostat)
    22d
    Cytopathologic and histopathologic characteristics of SMARCB1 deficient neoplasm and correlation with molecular and immunohistochemical findings. (PubMed, Hum Pathol)
    The ancillary testing of SMARCB1 (INI-1) should be considered in a subset of patients whose tumor demonstrates bizarre cytomorphology, especially in poorly differentiated or markedly pleomorphic tumors. The cytological recognition is critical for appropriate management.
    Journal
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    SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • PIK3C2B (Phosphatidylinositol-4-Phosphate 3-Kinase Catalytic Subunit Type 2 Beta) • FBXO11 (F-Box Protein 11) • MAP3K14 (Mitogen-Activated Protein Kinase Kinase Kinase 14)
    |
    Tazverik (tazemetostat)
    1m
    EZH2-mediated hypermethylation of H3K27me3 downregulates claudin-4 and upregulates the Wnt/β-catenin signaling pathway in hepatocellular carcinoma metastasis. (PubMed, Biochim Biophys Acta Mol Cell Res)
    This leads to increased levels of Matrix metalloproteinase-9 (MMP-9) and vimentin, enhancing the invasion, migration, and metastasis of hepatocellular carcinoma (HCC) cells. However, inhibiting EZH2 with tazemetostat subsequently enhanced claudin-4 expression by reducing Wnt/β-catenin signaling activity and inhibiting EMT-inducing factors.
    Journal
    |
    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • VIM (Vimentin) • MMP9 (Matrix metallopeptidase 9)
    |
    Tazverik (tazemetostat)
    1m
    TRuST: A Study to Assess Long-term Safety of Tazemetostat in Adult Participants of All Ages With Any Disease Treated With Tazemetostat in a Previous Clinical Study (clinicaltrials.gov)
    P1/2, N=58, Completed, Epizyme, Inc. | Active, not recruiting --> Completed
    Trial completion
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    Tazverik (tazemetostat)