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    DRUG CLASS:

    EZH1 inhibitor

    Related drugs:
    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
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    ARID1A (AT-rich interaction domain 1A) • BAP1 (BRCA1 Associated Protein 1)
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    ARID1A mutation • EZH2 mutation
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    HH2853
    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
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    Keytruda (pembrolizumab) • tulmimetostat (DZR123)
    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
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    HER-2 (Human epidermal growth factor receptor 2) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    PATHWAY antiHer2/neu (4B5) Rabbit Monoclonal Primary Antibody
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    Enhertu (fam-trastuzumab deruxtecan-nxki) • Ezharmia (valemetostat)
    25d
    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
    1m
    EZHiSWITCH: Efficacy and Safety of the Valemetostat in Patients With Selected Solid Tumors. (clinicaltrials.gov)
    P2, N=900, Not yet recruiting, Gustave Roussy, Cancer Campus, Grand Paris
    New P2 trial
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    Ezharmia (valemetostat)
    1m
    Polycomb Repressive Complexes as Therapeutic Targets in Hematologic Malignancies. (PubMed, Exp Hematol)
    Therapeutic targeting of H3K27me3 with EZH2-selective inhibitors such as tazemetostat has shown clinical benefit in lymphoma; however, their efficacy is limited by functional redundancy with EZH1. The dual EZH1/2 inhibitor valemetostat overcomes this limitation by reactivating tumor suppressor genes, achieving durable responses in ATL and peripheral T-cell lymphoma (PTCL). Nonetheless, therapeutic resistance can emerge through PRC2 gatekeeper mutations and compensatory DNA methylation. These findings underscore the value of targeting the dysregulated epigenome and support the continued clinical development of dual EZH1/2 inhibitors.
    Review • Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • KMT2D (Lysine Methyltransferase 2D) • CREBBP (CREB binding protein) • BCOR (BCL6 Corepressor) • BMI1 (BMI1 proto-oncogene, polycomb ring finger) • SUZ12 (SUZ12 Polycomb Repressive Complex 2 Subunit)
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    EZH2 mutation
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    Tazverik (tazemetostat) • Ezharmia (valemetostat)
    1m
    Targeting dysregulated epigenetic and transcription factor networks in KMT2A-rearranged AML using iPSC models. (PubMed, Blood Neoplasia)
    Treatment with the dual EZH1/2 inhibitor UNC1999 and 5-azacytidine reactivated these PRC2 target genes, specifically in AML-HSPCs, toward normal gene expression patterns. These findings suggest that targeting Polycomb repression offers a promising epigenetic strategy for improving outcomes in KMT2A-rearranged AML.
    Journal
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • KMT2A (Lysine Methyltransferase 2A) • MLLT3 (MLLT3 Super Elongation Complex Subunit)
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    KMT2A rearrangement • MLL rearrangement
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    azacitidine • UNC1999
    1m
    A Study of Valemetostat (DS-3201b) in Combination With Darolutamide in Metastatic Castration Resistant Prostate Cancer (mCRPC) (clinicaltrials.gov)
    P1, N=60, Recruiting, Daiichi Sankyo | Not yet recruiting --> Recruiting
    Enrollment open
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    Nubeqa (darolutamide) • Ezharmia (valemetostat)
    2ms
    Valemetostat Tosylate (DS-3201b), an Enhancer of Zeste Homolog (EZH) 1/2 Dual Inhibitor, for Relapsed/Refractory Peripheral T-Cell Lymphoma (VALENTINE-PTCL01) (clinicaltrials.gov)
    P2, N=155, Active, not recruiting, Daiichi Sankyo | Trial completion date: Sep 2025 --> Feb 2027
    Trial completion date
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    ALK (Anaplastic lymphoma kinase) • CD8 (cluster of differentiation 8)
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    ALK positive • ALK negative
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    Ezharmia (valemetostat)
    2ms
    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)
    2ms
    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)
    4ms
    An Open-label Dose Escalation and Expansion, Followed by a Phase II Study of Tulmimetostat (DZR123) and JSB462 (Luxdegalutamide) in Patients With Progressive Metastatic Castrate Resistant Prostate Cancer (mCRPC) (TulmiSTAR-01) (clinicaltrials.gov)
    P1/2, N=188, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    |
    tulmimetostat (DZR123) • luxdegalutamide (ARV-766)