pelabresib

Pelabresib is an investigational, oral small-molecule inhibitor of bromodomain and extraterminal (BET) proteins, including BRD2, BRD3, BRD4, and BRDT. By binding to the bromodomains of these BET proteins, pelabresib disrupts their interaction with acetylated histones and transcription factors. This action interferes with chromatin remodeling and downregulates the expression of oncogenes such as MYC, BCL-2, and NF-kB. The result is reduced cancer cell proliferation and increased apoptosis. Pelabresib is being developed primarily for hematologic malignancies such as myelofibrosis (including primary myelofibrosis, post-polycythemia vera myelofibrosis, post-essential thrombocythemia myelofibrosis), essential thrombocythemia, relapsed/refractory lymphomas, acute leukemia, myelodysplastic syndrome (MDS), and other advanced cancers[1][2][4][5][6][7][8].

Other names

pelabresib anhydrous