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1year
A Novel and Potent EZH1/2 Dual Inhibitor, HM97662 Demonstrated a Wide Spectrum of Therapeutic Potential for Hematological Malignancies (ASH 2023)
The enhancer of zeste homolog 2 (EZH2) and its homolog EZH1 are catalytic components of polycomb repressive complex 2 (PRC2), which tri-methylate histone H3 at lysine 27 (H3K27me3) to repress transcription of their target genes. In conclusion, the present preclinical studies demonstrated that HM97662, an EZH1/2 dual inhibitor, had a promising and wide spectrum of therapeutic potential for hematological malignancies. It is urgent to assess the effectiveness of HM97662 in further clinical trials.
IO biomarker
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CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • CD38 (CD38 Molecule) • PRDM1 (PR/SET Domain 1) • CDKN1C (Cyclin Dependent Kinase Inhibitor 1C) • SUZ12 (SUZ12 Polycomb Repressive Complex 2 Subunit)
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EZH2 mutation • EZH2 Y641 • EZH2 overexpression
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27 • HM97662
almost2years
A novel and potent EZH1/2 dual inhibitor, HM97662 demonstrates antitumor activity in T-cell lymphoma (AACR 2023)
We further conducted chromatin accessibility assay and identified that the chromatin structures of them were loosened and highly transcribed after the treatment of HM97662.Based our in vitro pharmacology data, we evaluated an antitumor activity of HM97662 in EZH1/2 co-expressed HuT-102 T-cell lymphoma cell mouse xenograft model, and daily oral dosing of HM97662 showed potent tumor growth inhibition.In conclusion, the present studies demonstrated that HM97662 has promising prospective for the treatment of patients with T-cell lymphoma. Given that the necessity of new treatment options on T-cell lymphoma, it is urgent to assess the effectiveness of HM97662 in further clinical trials.
PARP Biomarker
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CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • CASP3 (Caspase 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CDKN1C (Cyclin Dependent Kinase Inhibitor 1C) • SUZ12 (SUZ12 Polycomb Repressive Complex 2 Subunit)
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HM97662
2years
Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma. (PubMed, Drug Discov Ther)
Adult T-cell leukemia/lymphoma (ATL) is a mature T-cell lymphoma with a poor prognosis. Several other dual EZH1/2 inhibitors such as HH2853, HM97594, and HM97662 have also demonstrated potential in treating malignant tumors. Dual targeting EZH1/2 may have promising antitumor action in hematological malignancies and solid tumors.
Journal
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EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit)
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Ezharmia (valemetostat) • HM97594 • HH2853 • HM97662