Novel therapeutic agents for lowering low density lipoprotein cholesterol

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• 作者：Tisha R. Joy ; ^{tisjoy@hotmail.com}
• 关键词：Apo ; apolipoprotein ; ASO ; antisense oligonucleotide ; CHD ; coronary heart disease ; CVD ; cardiovascular disease ; CYP ; cytochrome P450 ; ED50 ; effective dose ; FH ; familial hypercholesterolemia ; HDL-C ; high-density lipoprotein cholesterol ; IC50 ; half maximal i
• 刊名：Pharmacology and Therapeutics
• 出版年：2012
• 期刊代码：41_01637258
• 类别：pha
• 出版时间：July, 2012
• 卷：135
• 期：1
• 页码：31-43
• 文件大小：686 K

摘要

Elevated low density lipoprotein cholesterol (LDL-C) levels have been associated with an increased risk for cardiovascular disease (CVD). Despite a 25-30%reduction in CVD risk with LDL-C reducing strategies, there is still a significant residual risk. Moreover, achieving target LDL-C values in individuals at high CVD risk is sometimes limited because of tolerability and/or efficacy. Thus, novel therapeutic agents are currently being developed to lower LDL-C levels further. This review will highlight some of these therapeutic agents including anti-sense oligonucleotides focused on apolipoprotein B, proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, microsomal triglyceride transfer protein inhibitors, and thyromimetics. For each therapeutic class, an overview of the mechanism of action, pharmacokinetic data, and efficacy/safety evidence will be provided.