^
    3d
    SHR2554 as Maintenance Therapy in Patients With Peripheral T-cell Lymphoma (clinicaltrials.gov)
    P2, N=30, Not yet recruiting, The First Affiliated Hospital with Nanjing Medical University
    New P2 trial
    |
    zeprumetostat (SHR-2554)
    4d
    Crotonate suppresses breast cancer metastasis and promotes immunotherapy response by inducing ACSS2-mediated EZH2-K348 crotonylation. (PubMed, Sci Adv)
    In comparison, crotonate showed better blocking effect than EZH2 inhibitor tazemetostat in suppressing breast cancer metastasis. The combination of crotonate and anti-PD-L1 (programmed cell death ligand 1) antibody enhances responses of breast cancer cells to immunotherapy. Together, our findings indicate that crotonate is a promising anticancer drug candidate that suppresses breast cancer growth and metastasis by specifically inducing EZH2 degradation.
    Journal
    |
    ACSS2 (Acyl-CoA Synthetase Short Chain Family Member 2)
    |
    Tazverik (tazemetostat)
    4d
    Therapeutic horizons in the development of PROTAC-based EZH2 inhibitors: recent achievements, comparative analysis, and future perspectives. (PubMed, RSC Adv)
    Despite the clinical success of tazemetostat, classical small-molecule inhibitors face limitations related to incomplete target occupancy, adaptive resistance, and non-catalytic EZH2 functions...Future directions focus on integrating novel ligases, proteome-wide selectivity mapping, and computational modeling to refine degradation efficiency and minimize off-target effects. Collectively, these developments explain a transformative therapeutic horizon where EZH2-targeting PROTACs are dignified to overcome the intrinsic limitations of enzyme inhibition, offering a new era of epigenetic cancer therapy through targeted protein degradation.
    Review • Journal
    |
    CRBN (Cereblon)
    |
    Tazverik (tazemetostat)
    6d
    Clinical Study of EZH2 Inhibitor Combined With PARP Inhibitor in the Treatment of Platinum-Sensitive Recurrent Ovarian Cancer (clinicaltrials.gov)
    P2, N=30, Not yet recruiting, Peking University Third Hospital
    New P2 trial • Platinum sensitive
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    BRCA wild-type
    |
    AiRuiYi (fluzoparib) • zeprumetostat (SHR-2554)
    6d
    EZH2 Inhibitor Zeprumetostat in Combination Therapy for Patients With Relapsed or Refractory Mature T-cell and NK-cell Lymphomas (clinicaltrials.gov)
    P1/2, N=60, Not yet recruiting, Sun Yat-sen University
    New P1/2 trial
    |
    Epidaza (chidamide) • zeprumetostat (SHR-2554) • golidocitinib (DZD4205)
    11d
    A Randomized, Double-blind, Multicenter Phase III Study of XNW5004 Tablets in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (clinicaltrials.gov)
    P3, N=120, Recruiting, Evopoint Biosciences Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    TNFRSF8 (TNF Receptor Superfamily Member 8)
    |
    TNFRSF8 positive
    |
    Epidaza (chidamide) • XNW5004
    11d
    MEVPRO-2: A Study to Learn How PF-06821497 (Mevrometostat) Works in Men With Metastatic Castration-resistant Prostate Cancer. (clinicaltrials.gov)
    P3, N=900, Recruiting, Pfizer | Trial primary completion date: Jul 2026 --> Dec 2026
    Trial primary completion date
    |
    Xtandi (enzalutamide) • abiraterone acetate • mevrometostat (PF-06821497)
    11d
    A Study to Learn About the Investigational Medicine Called PF-06821497 (Mevrometostat) in Men With mCRPC Who Were Previously Treated With Abiraterone Acetate for Prostate Cancer (MEVPRO-1). (clinicaltrials.gov)
    P3, N=600, Recruiting, Pfizer | Trial primary completion date: Dec 2025 --> Jul 2026
    Trial primary completion date
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • mevrometostat (PF-06821497)
    11d
    Pbrm1 loss induces a permissive chromatin state for cholangiocytic differentiation and cholangiocarcinoma formation. (PubMed, Cell Mol Gastroenterol Hepatol)
    PBRM1 maintains chromatin accessibility for hepatocyte differentiation-related genes. Its loss promotes differentiation toward cholangiocytes during injury or tumorigenesis, driving iCCA development.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • PBRM1 (Polybromo 1)
    |
    KRAS mutation • KRAS G12D • KRAS wild-type • RAS wild-type • KRAS G12
    |
    Tazverik (tazemetostat)
    11d
    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
    11d
    To Evaluate a Phase I/II Clinical Study of XNW5004 Tablets in Patients With Relapsed/Refractory Advanced Tumors (clinicaltrials.gov)
    P1/2, N=120, Completed, Evopoint Biosciences Inc. | Recruiting --> Completed | N=176 --> 120 | Trial completion date: Dec 2024 --> Aug 2025 | Trial primary completion date: Dec 2024 --> Aug 2025
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    TNFRSF8 (TNF Receptor Superfamily Member 8)
    |
    EZH2 mutation
    |
    XNW5004
    13d
    EZH-301: Tazemetostat in Combination With Doxorubicin as Frontline Therapy for Advanced Epithelioid Sarcoma (clinicaltrials.gov)
    P1, N=25, Terminated, Epizyme, Inc. | Phase classification: P3 --> P1
    Phase classification
    |
    doxorubicin hydrochloride • Tazverik (tazemetostat)