alobresib

Alobresib is an orally bioavailable small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, including BRD2, BRD3, BRD4, and BRDT. By binding to the acetylated lysine recognition motifs in BET bromodomains, alobresib prevents BET proteins from interacting with acetylated histones. This disrupts chromatin remodeling and gene expression—particularly genes involved in cell growth such as c-MYC—leading to inhibition of proliferation in tumor cells that overexpress BET proteins. Alobresib has been investigated primarily for its antineoplastic activity in solid tumors and hematologic malignancies such as metastatic castration-resistant prostate cancer, HER2-negative breast cancer, diffuse large B-cell lymphoma, and other lymphomas. The drug was developed by Gilead Sciences[1][2][3][4][5].

Other names

alobresibumAlobresib [INN](2-cyclopropyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-benzimidazol-4-yl)bis(pyridin-2yl)methanol