ST LOUIS (MD Consult) - On August 3, 2009, the US Food and Drug Administration (FDA) and Kowa Pharmaceuticals America announced the approval of Livalo (pitavastatin) for the primary treatment of hypercholesterolemia and combined dyslipidemia. Livalo is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.

 

Like other statin drugs, Livalo is intended for use in patients after diet and exercise fail to lower elevated blood cholesterol levels. Statins improve these levels primarily by inhibiting a liver enzyme known as HMG Co-A reductase, an enzyme involved in the liver's cholesterol manufacturing process.

 

Livalo differs from other, currently available statins in the United States in that it has a unique cyclopropyl group added to its base structure. This chemical structure allows for a more effective inhibition of the HMG-CoA reductase enzyme, resulting in improved inhibition of cholesterol production, and potentially affording greater low-density lipoprotein cholesterol (LDL-C) clearance and reduction of plasma cholesterol. One benefit of pitavastatin is that it is only minimally metabolized by the liver through the cytochrome P-450 pathway, the means by which many other medications are metabolized.

 

In pivotal phase 3 clinical trials, Livalo effectively reduced LDL-C and improved other parameters of lipid metabolism in special patient populations, including older adults, patients with diabetes, and patients at higher cardiovascular risk. According to the manufacturer, the overall safety and tolerability of Livalo are consistent with other commonly prescribed statins. An FDA press release states that Livalo was approved on the basis of data from 5 clinical trials comparing the drug's efficacy and safety with that of 3 currently marketed statins.

 

The most frequently reported adverse reactions associated with Livalo are constipation, myalgia, and back and joint pain.

 

Kowa expects to launch Livalo in the United States in early 2010. The drug will be available in 3 dosage sizes (1-, 2-, and 4-mg).

 

圣路易斯(MD Consult)——2009年8月3日，美国食品药品管理局(FDA)和日本兴和(美国)制药公司宣布，利维乐(Livalo，别名“力清之”，即匹伐他汀)已获准用作高胆固醇血症和混合型高脂血症的基础治疗药。利维乐是一种3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂。

与其他他汀类药物相近，利维乐适用于通过饮食和运动疗法控制而血胆固醇水平仍居高不下的患者。他汀类药物改善血脂水平的主要机制是抑制一种名为HMGCo-A还原酶的肝酶，此酶参与肝内的胆固醇合成。

利维乐与目前在美国上市的其他他汀类药物的区别在于，其基础结构中添加了一个特异性环丙基基团。这种化学结构使其能更有效地抑制HMG-CoA还原酶，从而增强对胆固醇合成的抑制作用，进而大大提高低密度脂蛋白胆固醇(LDL-C)的清除率，降低血胆固醇水平。匹伐他汀益处之一为，它经肝脏细胞色素P-450途径代谢得极少，而其他许多药物均通过此途径代谢。

在关键性的3期临床试验中，利维乐在特殊患者群中可有效降低LDL-C水平、改善脂质代谢的其他指标，此患者群包括年长者、糖尿病患者及心血管风险较高的患者。据生成厂家声称，利维乐的总体安全性和耐受性与其他常规使用的他汀类药物一致。FDA在一次新闻发布会声明，有5项临床试验对此药与其他3种当前市售的他汀类药物的疗效和安全性进行了比较，而FDA正是基于这5项研究的数据批准了利维乐。

利维乐最常报告的不良反应为便秘、肌痛、背痛及关节痛。

兴和制药公司预期于2010年初将利维乐推向美国市场，届时该药将有3种剂量规格(1 mg，2 mg及4 mg)出售。