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Association details:
| Biomarker: | EZH2 Y641 |
|---|---|
| Cancer: | Lymphoma |
| Drug: | HM97594 (EZH2 inhibitor, EZH1 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
A Novel and Potent EZH1/2 Dual Inhibitor HM97594 for the Treatment of Hematological Malignancies
Excerpt:
HM97594 potently repressed trimethylation of H3K27 in lymphoma and myeloma cell lines... Also, HM97594 caused cell cycle G0/1 arrest and apoptosis in KARPAS-422 cells harboring EZH2 Y641 GOF mutation…HM97594 showed potent antitumor activity in KARPAS-422 lymphoma cell xenograft mouse model. Once daily orally administered HM97594 greatly inhibited tumor growth in a dose-dependent manner without body weight loss compared to the known EZH2 inhibitor.
DOI:
https://doi.org/10.1182/blood-2019-122982
