Brandts Julia, Ray Kausik K
Department of Medicine I, University Hospital RWTH Aachen, Aachen, Germany.
Imperial Centre for Cardiovascular Disease Prevention, School of Public Health, Imperial College London, London, UK.
Future Cardiol. 2020 Sep;16(5):385-395. doi: 10.2217/fca-2020-0017. Epub 2020 May 7.
Apabetalone is the first selective BET protein inhibitor in the field of cardiovascular diseases (CVD). BET proteins are epigenetic regulators that link upstream epigenetic modifications to downstream gene expression. Inhibition of BET proteins by apabetalone has been shown to modulate reverse cholesterol transport, coagulation, inflammation and vascular calcification. Furthermore, apabetalone reduces circulating markers of CVD risk and plaque vulnerability. pooled analyses suggest a potential reduction in risk of major adverse cardiac events (MACE) in patients with Type 2 diabetes (T2D) and stable CVD. However, the current cardiovascular outcomes trial BET-on-MACE failed to detect the assumed 30% reduction of MACE by apabetalone in patients with T2D after an acute coronary syndrome.
阿巴他龙是心血管疾病（CVD）领域的首个选择性溴结构域和额外末端结构域（BET）蛋白抑制剂。BET蛋白是表观遗传调节因子，可将上游表观遗传修饰与下游基因表达联系起来。已证明阿巴他龙抑制BET蛋白可调节逆向胆固醇转运、凝血、炎症和血管钙化。此外，阿巴他龙可降低心血管疾病风险和斑块易损性的循环标志物。汇总分析表明，2型糖尿病（T2D）和稳定型心血管疾病患者发生主要不良心脏事件（MACE）的风险可能降低。然而，目前的心血管结局试验BET-on-MACE未能检测到阿巴他龙在急性冠状动脉综合征后对T2D患者MACE的预期降低30%的效果。
