The Hatter Cardiovascular Institute, University College London Hospital, London, United Kingdom.
Curr Opin Cardiol. 2009 Sep;24(5):473-82. doi: 10.1097/HCO.0b013e32832ebfe7.
Despite optimally reducing low-density lipoprotein cholesterol (LDL-C) levels to recommended targets using intensive statin therapy, the risk of cardiovascular disease (CVD) remains significant. Low levels of high-density lipoprotein cholesterol (HDL-C; <1.03 mmol/l or <40 mg/dl) are an independent risk factor for CVD, and raising levels of HDL-C is a major treatment strategy for regressing atherosclerosis and enhancing CVD risk reduction. This can be achieved by both nonpharmacological lifestyle measures and pharmacological treatment strategies.
This article will focus on the currently available and emerging pharmacological treatment strategies for raising HDL-C. Extended-release nicotinic acid (or Niacin) remains the most effective pharmacological treatment currently available for elevating HDL-C, having recently been combined with simvastatin (as Simcor) and laropripant (as Cordaptive, to reduce flushing). Other HDL-C-raising agents in current clinical use or in clinical development are fibrates, peroxisome proliferator-activated receptor agonists, cholesteryl ester transfer protein inhibitors, and HDL-C mimetics. Novel pharmacological targets for raising HDL-C also include the nuclear liver X and farnesoid X receptors and endothelial lipase.
Novel well tolerated and efficacious treatment strategies for raising HDL-C are required to target atherosclerosis and enhance CVD risk reduction.
尽管通过强化他汀类药物治疗将低密度脂蛋白胆固醇(LDL-C)水平降至推荐目标,但心血管疾病(CVD)的风险仍然很大。低水平的高密度脂蛋白胆固醇(HDL-C;<1.03mmol/l 或 <40mg/dl)是 CVD 的独立危险因素,升高 HDL-C 水平是逆转动脉粥样硬化和增强 CVD 风险降低的主要治疗策略。这可以通过非药物生活方式措施和药物治疗策略来实现。
本文将重点介绍目前可用于升高 HDL-C 的药物治疗策略。烟酸(或烟碱)的缓释剂仍然是目前升高 HDL-C 最有效的药物治疗方法,最近已与辛伐他汀(Simcor)和拉罗匹仑(Cordaptive)联合使用,以减少潮红。其他目前在临床使用或临床开发中的升高 HDL-C 的药物包括贝特类药物、过氧化物酶体增殖物激活受体激动剂、胆固醇酯转移蛋白抑制剂和 HDL-C 模拟物。升高 HDL-C 的新的药物靶点还包括核肝 X 和法呢醇 X 受体以及内皮脂肪酶。
需要新型、耐受良好且有效的升高 HDL-C 的治疗策略来靶向动脉粥样硬化并增强 CVD 风险降低。