生产企业：Opna Bio
OPN-2853 (formerly PLX2853, now dubbed zavabresib) is a potent, orally active small molecule BET bromodomain inhibitor in clinical development. In myelofibrosis (MF), BET inhibition controls inflammation triggered by epigenetic changes in the BRD4/NF-kB dependent regulatory network and normalizes megakaryocytic differentiation; the drug is being tested in combination with ruxolitinib for patients who have not responded to ruxolitinib alone.
OPN-2853 (formerly PLX2853, now dubbed zavabresib) is a potent, orally active small molecule BET bromodomain inhibitor in clinical development. In myelofibrosis (MF), BET inhibition controls inflammation triggered by epigenetic changes in the BRD4/NF-kB dependent regulatory network and normalizes megakaryocytic differentiation; the drug is being tested in combination with ruxolitinib for patients who have not responded to ruxolitinib alone.
BET bromodomain inhibitor. Bromo- and extra-terminal domain (BET) proteins regulate transcription by reading acetylation marks on histones; zavabresib (OPN-2853) selectively inhibits BET protein recognition of acetylated histones and down-regulates oncogenic gene expression.
OPN-2853 (zavabresib) is in clinical development for myelofibrosis, where it is being tested in combination with ruxolitinib in patients who have not responded to ruxolitinib alone; early-phase clinical evidence also covers advanced solid tumors and non-Hodgkin lymphoma (NHL).
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