Dipartimento Biomedico di Medicina Interna e Specialistica, Università degli Studi di Palermo, Palermo, Italy,
Curr Atheroscler Rep. 2014 Jun;16(6):414. doi: 10.1007/s11883-014-0414-4.
Statins are the first-line therapy in LDL-Cholesterol (LDL-C) reduction and its clinical use has contributed to significant prevention and treatment of atherosclerotic vascular disease. Yet, a significant proportion of patients remain at high risk. Recently, a number of new therapies have been developed to further lower LDL-C. These agents may provide clinical benefit on top of statin therapy in patients with high residual risk, severe hypercholesterolemia or as an alternative for patients who are intolerant to statins. We review four novel approaches based on the inhibition of proprotein convertase subtilisin/kexin type 9 (PCSK9), apolipoprotein-B100 (apoB), Cholesteryl ester transport protein (CETP) and microsomal triglyceride transfer protein (MTP). ApoB and MTP inhibitors (Mipomersen and Lomitapide) are indicated only for homozygous familial hypercholesterolemia patients. The results of ongoing trials with CETP and PCSK9 inhibitors may warrant a wider employment in different categories of patients at high risk for cardiovascular disease.
他汀类药物是降低 LDL 胆固醇（LDL-C）的一线治疗药物，其临床应用为动脉粥样硬化性血管疾病的预防和治疗做出了重大贡献。然而，仍有相当一部分患者处于高风险状态。最近，已经开发出许多新的治疗方法来进一步降低 LDL-C。这些药物可能会在高残余风险、严重高胆固醇血症的患者中，或在不耐受他汀类药物的患者中提供他汀类药物治疗之外的临床获益。我们综述了基于以下四种新方法的治疗策略：前蛋白转化酶枯草溶菌素 9（PCSK9）、载脂蛋白 B100（apoB）、胆固醇酯转运蛋白（CETP）和微粒体甘油三酯转移蛋白（MTP）的抑制剂。仅适用于纯合子家族性高胆固醇血症患者的 apoB 和 MTP 抑制剂（米泊美生和洛美他派）。正在进行的 CETP 和 PCSK9 抑制剂试验的结果可能需要在高心血管疾病风险的不同类别患者中更广泛地应用。
