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    DRUG CLASS:

    EZH1 inhibitor

    Related drugs:
    11d
    Assessing Treatment of T-Cell Lymphoma With GW5282 in Combination With Golidocitinib (BEI-DOU3) (clinicaltrials.gov)
    P1/2, N=165, Not yet recruiting, Dizal Pharmaceuticals
    New P1/2 trial
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    doxorubicin hydrochloride • cyclophosphamide • golidocitinib (DZD4205)
    19d
    Enhancer of Zeste Homolog 1 and 2 Inhibitor-Induced Colitis Mimicking Immune Checkpoint Inhibitor-Induced Colitis. (PubMed, Intern Med)
    An 80-year-old woman with relapsed nodal T-follicular helper cell lymphoma, not otherwise specified, developed severe watery diarrhea during valemetostat therapy...To the best of our knowledge, this is the first reported case of enhancer of zeste homolog 1 and 2 (EZH1/2) inhibitor-induced colitis. EZH1/2 inhibition may lead to T cell-mediated intestinal injury through epigenetic dysregulation; therefore, patients receiving EZH1/2 inhibitors who develop persistent diarrhea should undergo early endoscopic and histological evaluations.
    Journal • Checkpoint inhibition
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    CD8 (cluster of differentiation 8) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
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    Ezharmia (valemetostat)
    20d
    DS3201-343: Phase 1 trial of valemetostat and darolutamide in mCRPC (2025-522512-16-00)
    P1, N=4, Not yet recruiting, Daiichi Sankyo Inc.
    New P1 trial
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    Nubeqa (darolutamide) • Ezharmia (valemetostat)
    22d
    Valemetostat Therapy for Relapsed Adult T-Cell Leukemia/Lymphoma After Allogeneic Hematopoietic Stem Cell Transplantation. (PubMed, Hematol Oncol)
    At the last follow-up, four patients were alive without disease, four were alive with disease, and three died due to progressive disease. Hence, valemetostat is a promising salvage therapy for relapsed adult T-cell leukemia/lymphoma after allo-HCT.
    Retrospective data • Journal
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    IL2 (Interleukin 2)
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    Ezharmia (valemetostat)
    1m
    EZHiSWITCH: Efficacy and Safety of the Valemetostat in Patients With Selected Solid Tumors. (clinicaltrials.gov)
    P2, N=900, Recruiting, Gustave Roussy, Cancer Campus, Grand Paris | Not yet recruiting --> Recruiting
    Enrollment open
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    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)
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    Ezharmia (valemetostat)
    1m
    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
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    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • cabazitaxel • tulmimetostat (DZR123) • luxdegalutamide (ARV-766)
    2ms
    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)
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    PD-L1 expression • KRAS mutation
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    PD-L1 IHC 22C3 pharmDx
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    Keytruda (pembrolizumab) • Ezharmia (valemetostat)
    2ms
    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)
    2ms
    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)
    2ms
    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)
    2ms
    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
    2ms
    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)