Brown W V
Section on Arteriosclerosis and Lipid Metabolism, Emory Clinic, Emory University School of Medicine, Atlanta, Georgia 30322, USA.
Clin Cardiol. 2001 Aug;24(8 Suppl):III24-7. doi: 10.1002/clc.4960241506.
Statins are powerful agents for the reduction of low-density lipoprotein cholesterol (LDL-C) and reduction of cardiovascular risk. Newly developed statins with increased potency, such as rosuvastatin (Crestor) and NK-104 (in earlier clinical development), are capable of achieving marked LDL-C reductions. Cholesterol-lowering agents with mechanisms of action distinct from those of the statins are in active development. These include bile transport inhibitors, such as improved bile acid-absorbing resins and specific inhibitors of the ileal Na+/bile acid cotransporter. There are also specific inhibitors of cholesterol absorption, such as ezetimibe, which may provide cholesterol lowering that is additive to that achieved with statin treatment. Another approach is to reduce cardiovascular risk by modifying atherosclerotic processes within the arterial wall, as represented by the acyl CoA:cholesterol acyltransferase (ACAT) inhibitor avasimibe; ACAT inhibitors may reduce atherosclerotic lesions by inhibiting macrophage cholesterol storage.
他汀类药物是降低低密度脂蛋白胆固醇（LDL-C）和降低心血管风险的强效药物。新开发的效力增强的他汀类药物，如瑞舒伐他汀（可定）和NK-104（处于早期临床开发阶段），能够显著降低LDL-C。作用机制与他汀类药物不同的降胆固醇药物正在积极研发中。这些药物包括胆汁转运抑制剂，如改良的胆汁酸吸收树脂和回肠Na+/胆汁酸共转运体的特异性抑制剂。还有胆固醇吸收的特异性抑制剂，如依折麦布，它可能提供与他汀类药物治疗相加的降胆固醇效果。另一种方法是通过改变动脉壁内的动脉粥样硬化过程来降低心血管风险，以酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制剂阿伐麦布为代表；ACAT抑制剂可能通过抑制巨噬细胞胆固醇储存来减少动脉粥样硬化病变。
