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Torcetrapib and atorvastatin: a novel combination therapy for dyslipidemia.

机译:Torcetrapib和阿托伐他汀:血脂异常的新型联合疗法。

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摘要

Epidemiological studies have identified both low-density lipoproteins (LDL) and high-density lipoproteins (HDL) as independent factors that modulate the risk of cardiovascular disease. Statins (HMG-CoA reductase inhibitors) that lower LDL and triglyceride levels are widely used for the treatment of hypercholesterolemia. Recently, a new class of drugs, cholesterol ester transfer protein (CETP) inhibitors, which significantly raise HDL and lower LDL, has been developed. Torcetrapib, a CETP inhibitor, has been shown to be effective, safe and well tolerated when used in combination with atorvastatin therapy. Torcetrapib has been shown to increase HDL cholesterol levels by 46% when given alone and by 61% when given in combination with atorvastatin, as well as to decrease LDL cholesterol levels by more than that achieved by atorvastatin alone. When the dosage of torcetrapib was doubled (at maximum tolerated dose), HDL increased by over 100%. Combination therapy appeared safe and well tolerated. Large trials evaluating the efficacy and safety of torcetrapib in combination therapy with atorvastatin are now in progress in order to establish whether CETP inhibition in combined therapy with statins will reduce the risk for atherosclerosis.
机译:流行病学研究已确定低密度脂蛋白(LDL)和高密度脂蛋白(HDL)都是调节心血管疾病风险的独立因素。降低LDL和甘油三酸酯水平的他汀类药物(HMG-CoA还原酶抑制剂)被广泛用于治疗高胆固醇血症。最近,已经开发出一种新型药物,即胆固醇酯转移蛋白(CETP)抑制剂,该抑制剂可显着提高HDL和降低LDL。当与阿托伐他汀疗法联合使用时,CETP抑制剂Torcetrapib被证明是有效,安全且耐受性良好的。单独使用Torcetrapib时,Torcetrapib可使HDL胆固醇水平增加46%,与阿托伐他汀组合使用时,可使HDL胆固醇水平增加61%,并且与单独使用阿托伐他汀相比,其降低LDL胆固醇水平的作用更大。当torcetrapib的剂量加倍(在最大耐受剂量下)时,​​HDL增加了100%以上。联合治疗似乎安全且耐受性良好。为了确定CETP在他汀类药物联合治疗中的抑制作用是否会降低动脉粥样硬化的风险,目前正在进行一项大型试验,评估托瑞特拉替尼与阿托伐他汀联合治疗的疗效和安全性。

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