【中文品名】非诺贝酸
【药效类别】降血脂药>氯贝特类
【通用药名】FENOFIBRIC ACID
【别　　名】
【化学名称】 2-[4-(4-Chlorobenzoyl)phenoxy]-2-methyl-propanoic acid
【CA登记号】[]
【结 构 式】

【分 子 式】C₁₇H₁₅ClO₄
【分 子 量】318.76
【收录药典】
美国FDA批准雅培公司的非诺贝酸控释胶囊（fenofibricacid，Trilipix）上市，本药品用于同时控制饮食降低血脂疾病患者的甘油三酯和低密度脂蛋白（LDL），升高高密度脂蛋白（HDL）。对一些高血脂患者，临床治疗准则推荐采用非诺贝酸类药物与他汀类药物联合用药来进一步改善血脂。非诺贝酸控释胶囊是首个和迄今唯一获准可与他汀类药物联合使用的非诺贝酸类药品。目前尚未有研究可证明本品可预防心脏疾病或心脏病发作。

美国FDA批准本品上市是基于评价非诺贝酸与各种他汀类药物联合用药疗效和安全性迄今最大的临床研究数据。本品与3种最普遍处方的他汀类药物（罗苏伐他汀、阿托伐他汀和辛伐他汀）对2698例混合型血脂异常患者进行了3项12周随机多中心双盲对照的疗效和安全性Ⅲ期临床研究。研究纳入的患者LDL>130mg/dL，甘油三酯>150mg/dL，而HDL男性<40mg/dL、女性<50mg/dL。

总共1911例患者完成了12周的临床研究，而后进入52周长期开放式进一步的研究。此项Ⅲ期临床研究结果均符合其主要治疗目标。联合用药治疗较单独使用他汀类药物显著改善了HDL和甘油三酯水平，较本品单独用药显著改善了LDL。所有联合用药和他汀类药物均具有降低LDL的临床作用。本品与处方量最大的他汀类药物联合用药改善3种脂质的效果较单一用药佳。

TRILIPIX

Indication(s):

Adjunct to diet: In combination with a statin, to reduce triglycerides (TG) and increase high-density lipoprotein cholesterol (HDL-C) in patients with mixed dyslipidemia and CHD or a CHD risk equivalent who are on optimal statin therapy to achieve LDL-C goal; As monotherapy to reduce TG in severe hypertriglyceridemia, and to reduce elevated LDL-C, total cholesterol (total-C), TG, and apolipoprotein B (Apo B), and to increase HDL-C in primary hyperlipidemia or mixed dyslipidemia.

Pharmacology:

Elevated blood levels of total-C, LDL-C, and Apo B and decreased levels of HDL-C have been shown to increase the risk for atherosclerosis. Fenofibric acid, the active moiety of fenofibrate, is a lipid modifying agent that increases lipolysis and the elimination of TG-rich particles from plasma by activating lipoprotein lipase and reducing the production of apolipoprotein CIII.

Trilipix can be used in combination with a statin in patients with mixed dyslipidemia and CHD or a CHD risk equivalent, which include other forms of atherosclerotic disease, diabetes, and multiple risk factors that confer a 10-year risk for CHD >20%. It has not been established that the use of Trilipix reduces morbidity and mortality more than the use of a statin alone.

Clinical Trials:

Three 12-week Phase 3 studies and one 52-week, open label extension study were conducted to evaluate safety and efficacy of this product. In the Phase 3 studies, Trilipix was studied in combination with rosuvastatin, atorvastatin or simvastatin. A total of 1,895 patients who completed one of the Phase 3 studies were then treated in the open-label study in which 568 patients completed 52 weeks of treatment with Trilipix plus a statin. The primary endpoints for each of the studies was the mean % change from baseline to final value in HDL-C, TG, and LDL-C. The results of these studies indicated that combination therapy with low-dose and moderate-dose statins significantly improved HDL-C and TG compared to statin therapy alone, and significantly improved LDL-C compared to Trilipix alone. The use of each of the combinations and the statins resulted in significant reductions in LDL-C.

Legal Classification:

Rx

Adults:

Mixed dyslipidemia, primary hyperlipidemia: 135mg once daily. Hypertriglyceridemia: 45–135mg once daily. Titrate at 4–8week intervals; max 135mg/day. Mild to moderate renal impairment: initially 45mg once daily.

Children:

Not recommended.

Contraindication(s):

Severe renal dysfunction (including dialysis). Active liver disease. Primary biliary cirrhosis. Gallbladder disease. Nursing mothers.

Warnings/Precautions:

Renal failure, diabetes, hypothyroidism, elderly: increased risk of myopathy with concomitant statins. Monitor liver function; discontinue if LFTs >3xULN persist. Discontinue if markedly elevated CPK levels, myopathy, or gallstones occur. Pregnancy (Cat.C).

Interaction(s):

Avoid with max doses of a statin (myopathy). Potentiates warfarin (monitor). Separate dosing of bile acid sequestrants. Caution with cyclosporine.

Adverse Reaction(s):

Headache, back pain, nasopharyngitis, myalgia, GI upset, URI, elevated LFTs, serum creatinine; myopathy, rhabdomyolysis, hematological changes (eg, hgb, hct), cholelithiasis, pancreatitis.

How Supplied:

Caps—90

Last Updated:

1/21/2009