^
    3d
    SHR2554/AZA + Overlapped Modified BUCY for High-risk/Relapsed Leukemia/MDS (clinicaltrials.gov)
    P2, N=180, Not yet recruiting, The First Affiliated Hospital of Soochow University
    New P2 trial
    |
    cytarabine • azacitidine • cyclophosphamide • zeprumetostat (SHR-2554)
    5d
    Comprehensive Genomic Profiling of Sinonasal Carcinomas: Identification of Common Mutations and Potential Targets for Therapy. (PubMed, J Neurol Surg B Skull Base)
    Treatments include surgery, radiation, and chemotherapy, with ongoing trials investigating agents like cetuximab, cisplatin, and Tazemetostat. Tazemetostat, targeting KMT2D-related DNA (deoxyribonucleic acid) methylation, and cetuximab, targeting the PIK3CA signaling cascade, may offer therapeutic benefits. Further research on mutation-specific therapies could improve treatment strategies.
    Journal
    |
    TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • KMT2D (Lysine Methyltransferase 2D) • FAT1 (FAT atypical cadherin 1) • PRKDC (Protein Kinase, DNA-Activated, Catalytic Subunit)
    |
    TP53 mutation • PIK3CA mutation • IDH2 mutation
    |
    Erbitux (cetuximab) • cisplatin • Tazverik (tazemetostat)
    6d
    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, Active, not recruiting, Pfizer | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    docetaxel • Xtandi (enzalutamide) • abiraterone acetate • mevrometostat (PF-06821497)
    8d
    EZH2 inhibition in resistant glioblastoma stem cells counteracts oxidative stress protection and triggers ferroptosis. (PubMed, Biomed Pharmacother)
    GSK343 overcame resistant dGSC protection to trigger cell death by a mechanism involving oxidative stress. To conclude, GSK343-mediated EZH2 inhibition efficiently eliminated resistant GSC through ferroptosis, in a H3K27me3-independent manner.
    Journal
    |
    BMI1 (BMI1 proto-oncogene, polycomb ring finger)
    |
    GSK343
    10d
    SHR2554/AZA + Overlapped TBF for High-risk/Relapsed Leukemia/MDS (clinicaltrials.gov)
    P2, N=160, Not yet recruiting, The First Affiliated Hospital of Soochow University
    New P2 trial
    |
    cytarabine • azacitidine • cyclophosphamide • zeprumetostat (SHR-2554)
    12d
    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 | N=13 --> 60
    Enrollment change • Trial initiation date
    |
    KLK3 (Kallikrein-related peptidase 3)
    |
    Nubeqa (darolutamide) • Ezharmia (valemetostat)
    12d
    CLIN-60200-456: Study of Tazemetostat in Adults With Follicular Lymphoma Previously Treated With at Least Two Therapies (clinicaltrials.gov)
    P=N/A, N=0, Withdrawn, Ipsen | N=63 --> 0 | Not yet recruiting --> Withdrawn
    Enrollment change • Trial withdrawal • Real-world evidence
    |
    EZH2 mutation
    |
    Tazverik (tazemetostat)
    13d
    CUREFL03: Mosunetuzumab and Zeprumetostat in Treating Patients With Follicular Lymphoma (clinicaltrials.gov)
    P2, N=80, Not yet recruiting, Institute of Hematology & Blood Diseases Hospital, China
    New P2 trial
    |
    CD20 positive
    |
    zeprumetostat (SHR-2554) • Lunsumio (mosunetuzumab-axgb)
    13d
    DS3201-A-J101: DS-3201b in Participants With Lymphomas (clinicaltrials.gov)
    P1, N=100, Active, not recruiting, Daiichi Sankyo Co., Ltd. | Trial completion date: Dec 2026 --> Dec 2027
    Trial completion date
    |
    Ezharmia (valemetostat)
    15d
    HHV-6A Drives Epigenetic Reprogramming via an EZH2-SIRT1 Axis to Sustain Mutant p53 and Reshape Oncogenic Inflammatory Signaling. (PubMed, Viruses)
    Pharmacological inhibition of EZH2 using DS-3201 reproduced some of the molecular effects of viral infection, including increased mutp53 stability...Indeed, the inhibition of SIRT1 with EX-527 reversed mutp53 accumulation but restored c-Myc expression and increased extracellular IL-6 release...These results establish a mechanistic link between viral infection, epigenetic remodeling, and oncogenic dependency. They also suggest that targeting IL-6 signaling could represent a therapeutic vulnerability in HHV-6A-associated thyroid cancer, particularly in combination with SIRT1 inhibitors.
    Journal
    |
    TP53 (Tumor protein P53) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • IL6 (Interleukin 6)
    |
    TP53 mutation • EZH2 mutation
    |
    selisistat (SEN-196) • Ezharmia (valemetostat)
    19d
    Clinical Study of XNW5004 Tablets in the Treatment of Relapsed and Refractory Follicular Lymphoma (clinicaltrials.gov)
    P2, N=65, Recruiting, Evopoint Biosciences Inc.
    New P2 trial
    |
    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
    |
    EZH2 mutation
    |
    igermetostat (XNW5004)
    20d
    HMGCS1 as a Potential Mediator of Resistance to EZH2 Inhibition via Ferroptosis mediated by PI3K/AKT/mTOR Pathway in the Pancreatic Neuroendocrine Neoplasms. (PubMed, Endocr Relat Cancer)
    Furthermore, combining GSK126 with everolimus, an mTOR inhibitor used clinically for pNENs, more effectively inhibited cell proliferation and tumor growth. In summary, Our findings reveal that the EZH2 inhibitor GSK126 induces ferroptosis by inhibiting the PI3K/AKT/mTOR pathway, suppressing pNENs progression, and HMGCS1 may mediate resistance to EZH2 inhibitors, offering new insights into pNENs treatment.
    Journal
    |
    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • HMGCS1 (3-Hydroxy-3-Methylglutaryl-CoA Synthase 1)
    |
    everolimus • GSK2816126