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    DRUG:

    APG-5918

    i
    Other names: APG-5918, EEDi-5273
    Associations

    News

    Trials
    Company:
    Ascentage Pharma
    Drug class:
    EED inhibitor
    Related drugs:
    Associations

    News

    Trials
    11d
    A Study to Investigate the Safety, Pharmacokinetics and Efficacy of APG-5918 in Healthy Subjects or Anemic Patients (clinicaltrials.gov)
    P1, N=105, Recruiting, Ascentage Pharma Group Inc. | Trial completion date: Mar 2026 --> Jul 2028 | Trial primary completion date: Aug 2025 --> Dec 2027
    Trial completion date • Trial primary completion date
    |
    APG-5918
    2years
    Embryonic Ectoderm Development (EED) Inhibitor APG5918 Improves Chronic Kidney Disease- (CKD)-Induced Hemoglobin Insufficiency in Preclinical Models of Anemia (ASH 2023)
    76-fold of the control group, respectively, which was pharmacologically superior to effects observed with hydroxyurea at 33 µM (~6. APG-5918 also showed synergistic antianemia effects when combined with EPO. These findings support APG-5918 as a novel treatment option for CKD-induced anemia.
    Preclinical
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    CD34 (CD34 molecule) • HBB (Hemoglobin Subunit Beta) • SUZ12 (SUZ12 Polycomb Repressive Complex 2 Subunit)
    |
    hydroxyurea • APG-5918
    3years
    Study of Safety, Pharmacokinetic and Efficacy of APG-5918 in Advanced Solid Tumors or Lymphomas (clinicaltrials.gov)
    P1, N=90, Recruiting, Ascentage Pharma Group Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
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    SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1)
    |
    EZH2 mutation
    |
    APG-5918
    over3years
    Study of Safety, Pharmacokinetic and Efficacy of APG-5918 in Advanced Solid Tumors or Lymphomas (clinicaltrials.gov)
    P1, N=90, Not yet recruiting, Ascentage Pharma Group Inc. | Trial completion date: Oct 2024 --> Sep 2025
    Trial completion date
    |
    SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • CAST (Calpastatin)
    |
    EZH2 mutation
    |
    APG-5918
    over3years
    Study of Safety, Pharmacokinetic and Efficacy of APG-5918 in Advanced Solid Tumors or Lymphomas (clinicaltrials.gov)
    P1, N=84, Not yet recruiting, Ascentage Pharma Group Inc.
    New P1 trial
    |
    SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1)
    |
    EZH2 mutation
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    APG-5918
    over3years
    Preclinical development of embryonic ectoderm development (EED) inhibitor APG-5918/EEDi-5273 for cancer therapy (AACR 2022)
    With regulatory approval of EZH2 inhibitor tazemetostat, a potentially effective successful cancer therapeutic strategy is now available for patients with epitheloid sarcoma and relapsed or refractory follicular lymphoma. In a mouse xenograft model derived from EZH2mut KARPAS-422 DLBCL cells, single-agent APG-5918 conferred potent and dose-dependent antitumor activity, resulting in durable complete tumor regression that correlated with inhibition of H3K27me3, induction of PRC2 target genes, and drug exposure in tumors. In summary, our results provide scientific rationale for the clinical development of APG-5918/EEDi-5273 in EZH2mut lymphomas and, potentially, other hematologic malignancies and solid tumors.
    Preclinical
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    EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • SUZ12 (SUZ12 Polycomb Repressive Complex 2 Subunit)
    |
    EZH2 mutation
    |
    Tazverik (tazemetostat) • APG-5918