AZD5153

AZD5153 is a potent, selective, and orally available small molecule inhibitor of the bromodomain and extraterminal (BET) family protein BRD4. It acts as a reversible, bivalent inhibitor by simultaneously binding to both bromodomains in BRD4, preventing its interaction with acetylated lysines on histones. This disrupts transcriptional programs critical for tumor growth and survival, particularly those involving oncogenes such as MYC and YAP1. AZD5153 has demonstrated preclinical antitumor activity in various cancers including hematologic malignancies (acute myeloid leukemia, multiple myeloma, diffuse large B-cell lymphoma), hepatocellular carcinoma, colorectal cancer, ovarian cancer (where it also modulates the tumor immune microenvironment), and solid tumors. The drug is being developed primarily by AstraZeneca for oncology indications[1][2][4][5][6][7][8].

Other names

bivalent BRD4 inhibitor AZD5153