Center for Endocrinology, Diabetes and Preventive Medicine, University of Cologne, Faculty of Medicine and University Hospital Cologne, Kerpener Str. 62, 50937, Köln, Germany.
Herz. 2022 Jun;47(3):220-227. doi: 10.1007/s00059-022-05113-x. Epub 2022 Apr 22.
Patients with hypertriglyceridemia (> 150 mg/dl) have an increased risk for atherosclerotic cardiovascular disease, and those with severe hypertriglyceridemia (> 880 mg/dl) also for pancreatitis. The currently available medications to decrease triglyceride levels, such as fibrates, statins, and omega‑3 fatty acids, are in many cases not able to achieve normal triglyceride levels. Therefore, new drugs are in development to address this unmet need. Recently, icosapent ethyl, a purified formulation of the omega-3-fatty acid eicosapentaenoic acid, was approved in Germany for the reduction of cardiovascular events in patients with hypertriglyceridemia and established cardiovascular disease or with diabetes and other risk factors on top of statins. Other new drugs in development are the more selective peroxisome proliferator-activated receptor α (PPARα) modulator, pemafibrate, already approved for the treatment of hypertriglyceridemia in Japan, and inhibitors of ApoC-III and angiopoietin-like 3 (ANGPTL3) in the form of antisense oligonucleotides or siRNAs or fully human monoclonal binding antibodies. Apolipoprotein C-III and ANGPTL3 protein seem to be quite promising targets based on solid genetic data. Larger studies of long duration, many of them currently ongoing, are needed to establish the role these medications will play in the treatment of hypertriglyceridemia in clinical practice.
患有高甘油三酯血症（>150mg/dl）的患者患动脉粥样硬化性心血管疾病的风险增加，而患有严重高甘油三酯血症（>880mg/dl）的患者也有患胰腺炎的风险。目前可用于降低甘油三酯水平的药物，如贝特类、他汀类和欧米伽-3 脂肪酸，在许多情况下无法使甘油三酯水平正常化。因此，正在开发新的药物来满足这一未满足的需求。最近，icosapent ethyl，一种纯化的二十碳五烯酸（EPA）制剂，在德国被批准用于降低高甘油三酯血症和已确诊心血管疾病或伴糖尿病和他汀类药物以外其他危险因素的患者的心血管事件风险。其他正在开发的新药是更具选择性的过氧化物酶体增殖物激活受体-α（PPARα）调节剂 pemafibrate，已在日本获准用于治疗高甘油三酯血症，以及反义寡核苷酸或 siRNA 或全人单克隆结合抗体形式的载脂蛋白 C-III 和血管生成素样 3（ANGPTL3）抑制剂。载脂蛋白 C-III 和 ANGPTL3 蛋白似乎是基于可靠的遗传数据相当有前途的靶点。需要进行更多长期的大型研究，其中许多正在进行中，以确定这些药物在临床实践中治疗高甘油三酯血症的作用。
