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    DRUG CLASS:

    EZH1 inhibitor

    Related drugs:
    10d
    CDZR123A12107: A clinical trial to learn about the effects of DZR123 and JSB462 given together in men with advanced prostate cancer that has stopped responding to other treatments (2025-521880-10-00)
    P1/2, N=76, Recruiting, Novartis Pharma AG | Not yet recruiting --> Recruiting
    Enrollment open
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • cabazitaxel • tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    18d
    DS3201-330: A Study of Valemetostat Tosylate Plus Pembrolizumab versus Pembrolizumab Alone in First-Line NSCLC Without Actionable Genomic Alterations (2024-519671-26-00)
    P1/2, N=21, Completed, Daiichi Sankyo Inc.
    New P1/2 trial
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    PD-L1 expression • KRAS mutation
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    PD-L1 IHC 22C3 pharmDx
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    Keytruda (pembrolizumab) • Ezharmia (valemetostat)
    18d
    CDZR123A12107: A clinical trial to learn about the effects of DZR123 and JSB462 given together in men with advanced prostate cancer that has stopped responding to other treatments (2025-521880-10-00)
    P1/2, N=76, Not yet recruiting, Novartis Pharma AG
    New P1/2 trial
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • cabazitaxel • tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    18d
    2024/3993 EZHiSWITCH: An open label phase II platform modular study exploring the efficacy and safety of the Valemetostat (EZH1/2 inhibitor) in patients with selected solid tumors. (2024-519788-16-00)
    P1/2, N=600, Not yet recruiting, Institut Gustave Roussy
    New P1/2 trial
    |
    ARID1A (AT-rich interaction domain 1A) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • PBRM1 (Polybromo 1) • BAP1 (BRCA1 Associated Protein 1) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • SMARCA2 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2)
    |
    Ezharmia (valemetostat)
    18d
    CDZR123C12101: TulmiSTAR-02: 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) (2025-521873-15-00)
    P1/2, N=54, Recruiting, Novartis Pharma AG
    New P1/2 trial
    |
    abiraterone acetate • Nubeqa (darolutamide) • tulmimetostat (DZR123)
    24d
    A Phase 1/2 Study of GW5282 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=203, Recruiting, Dizal Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    24d
    Tulmimetostat (DZR123) in Patients With Mycosis Fungoides and Sézary Syndrome (clinicaltrials.gov)
    P1, N=24, Active, not recruiting, Washington University School of Medicine | Recruiting --> Active, not recruiting | N=36 --> 24 | Trial completion date: Jan 2030 --> Jan 2029 | Trial primary completion date: Feb 2028 --> Feb 2027
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    tulmimetostat (DZR123)
    26d
    EZH2 Inhibition Reshapes 3D Chromatin Architecture to Induce Immunogenic Phenotype in Small Cell Lung Cancer. (PubMed, bioRxiv)
    Employing Micro-C, a micrococcal nuclease-based 3D genome mapping technique, we show that EZH1/2 inhibition with Valemetostat induced significant changes at multiple genome organizational levels (compartment, topological associated domain, and chromatin loop) without incurring cell death in NE SCLC...Notably, EZH1/2 inhibition reactivated Class I MHC expression by facilitating enhancer-promoter looping. Our results demonstrate that repression of a subset of EZH2 targets including Class I MHC genes is affected through modulation of 3D genome structure to the level of chromatin looping and further support clinical investigation of EZH2 inhibition in boosting therapeutic efficacy of ICI in SCLC patients.
    Journal • IO biomarker
    |
    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • SLFN11 (Schlafen Family Member 11) • HLA-B (Major Histocompatibility Complex, Class I, B)
    |
    Ezharmia (valemetostat)
    1m
    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
    |
    HH2853
    1m
    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)
    2ms
    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)
    2ms
    A Phase 1/2 Study of GW5282 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=203, Not yet recruiting, Dizal Pharmaceuticals
    New P1/2 trial