Mivebresib (ABBV-075), also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.

BET:1.5 nM(ki)

Mivebresib在来源于实体瘤、白血病和淋巴瘤的癌症细胞系上的细胞活性检测中展示活性。它能够干扰细胞周期控制，导致G1期阻滞后进入衰老状态，抑制致癌因子从而触发凋亡，并有可能针对肿瘤微环境以提供额外治疗效益[1]。

ABBV-075在非小细胞肺癌、小细胞肺癌、胰腺癌、乳腺癌、前列腺癌、头颈癌、多发性骨髓瘤、弥漫大B细胞淋巴瘤和白血病的侧腹移植小鼠模型中，与标准治疗药物相比，具有相当或更优的疗效[1]。