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HP560 is a novel small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, currently under development by Hinova Pharmaceuticals for the treatment of hematological malignancies, including myelofibrosis (MF) and acute myeloid leukemia (AML). The drug functions by competitively engaging the bromodomain pocket of BET proteins, which disrupts their interaction with acetylated histones and leads to their displacement from chromatin, thereby modulating the transcription of oncogenic programs. Preclinical studies have demonstrated that HP560 possesses high binding affinities for all BET proteins and exhibits potent anti-proliferative activity. In animal models, HP560 has shown therapeutic efficacy in improving survival, reducing splenomegaly, and alleviating anemia in myelofibrosis, as well as inhibiting tumor growth in AML. Furthermore, HP560 has demonstrated synergistic anti-proliferative effects when combined with the JAK1/2 inhibitor ruxolitinib.
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