GFH009 disrupts growth signals and triggers apoptosis in hematologic malignancies

A new research paper was published in Oncotarget’s Volume 14 on December 20, 2023, entitled, “The pharmacodynamic and mechanistic foundation for the antineoplastic effects of GFH009, a potent and highly selective CDK9 inhibitor for the treatment of hematologic malignancies.” The study aimed to summarize current knowledge underlying the mechanism of action (MOA) of GFH009, a potent, highly selective CDK9 small molecule inhibitor, and explain its robust anti-cancer activity. The research showed that GFH009 demonstrated antiproliferative activity in assorted HHM-derived cell lines, inducing apoptosis at IC50 values below 0.2 μM in 7/10 lines tested. The results mechanistically establish CDK9 as a targetable vulnerability in assorted HHMs, supporting the rationale for ongoing clinical studies with this agent in acute myeloid leukemia and other HHMs.

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