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Ezetimibe and bile acid sequestrants: Impact on lipoprotein metabolism and beyond

机译：依泽替米贝和胆汁酸螯合剂：对脂蛋白代谢的影响及其他

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Purpose of review Several lines of evidence indicate that the enterocyte plays a pivotal role in cholesterol homeostasis. The development of the selective inhibitor of cholesterol absorption ezetimibe and bile acid sequestrants (BAS) interrupting the enterohepatic circulation of bile salts has expanded the options for preventing and treating cardiovascular disease. We discuss here a selection of recently published studies that evaluated the effects of ezetimibe and BAS on lipoprotein metabolism. Recent findings Although significant progress has been made in recent years in elucidating the impacts of ezetimibe and BAS on lipoprotein metabolism, underlying mechanisms are not completely understood. Important new insights have been provided by using in-vivo kinetic studies of apolipoproteins labelled with a stable isotope. Other reports indicated that ezetimibe and BAS modulate the expression of several key genes involved in intestinal lipoprotein metabolism. Many of these effects have been related to the local effects of ezetimibe and BAS on intestinal cholesterol homeostasis. Summary A substantial effort is being made by researchers to fully understand the mechanisms by which ezetimibe and BAS improve lipid profile. The efficacy of combination therapy of statins with ezetimibe or BAS for the prevention of cardiovascular disease remains to be confirmed in clinical endpoint studies.
机译：复习目的几条证据表明，肠上皮细胞在胆固醇稳态中起关键作用。胆固醇吸收性依泽替米贝和胆汁酸螯合剂（BAS）的选择性抑制剂的开发中断了胆汁盐的肠肝循环，扩大了预防和治疗心血管疾病的选择。我们在这里讨论一些最近发表的研究，这些研究评估了依泽替米贝和BAS对脂蛋白代谢的影响。最新发现尽管近年来在阐明依泽替米贝和BAS对脂蛋白代谢的影响方面取得了重大进展，但尚未完全理解其潜在机制。通过使用标记有稳定同位素的载脂蛋白的体内动力学研究，提供了重要的新见解。其他报道表明，依泽替米贝和BAS调节肠道脂蛋白代谢中涉及的几个关键基因的表达。这些影响中有许多与依泽替米贝和BAS对肠道胆固醇稳态的局部影响有关。总结研究人员正在作出巨大的努力，以充分了解依泽替米贝和BAS改善脂质分布的机制。他汀类药物与依泽替米贝或BAS联合治疗预防心血管疾病的功效在临床终点研究中仍有待证实。

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