商品名称：VASCEPA
通用名称：ICOSAPENT ETHYL
生产厂商：AMARIN PHARMS
规格：1G
剂型：胶囊

7月26日，FDA批准专利合成制剂乙酯二十碳五烯酸（EPA）——二十碳五烯酸乙酯（Vascepa，以前称AMR101，Amarin公司）用于治疗高甘油三酯血症，这也是当今医药市场第二种处方用ω-3多不饱和脂肪酸（PUFA）制剂。
Amarin公司在其报告中指出，Vascepa是一种纯海洋油制剂，其EPA含量“不低于96%”，另一种活性ω-3PUFA二十二碳六烯酸（DHA）的含量极低。DHA是非处方鱼油胶囊和Lovaza(葛兰素史克公司)的主要成分，在多年前就已获得FDA批准。
　　据Heartwire报道，通过对长期的不良反应较为熟悉的EPA/DHAω-3多不饱和脂肪酸（包括Lovaza）的观察证据显示，仅含EPA的Vascepa不会升高低密度胆固醇（LDL-C）水平。去年的一项研究为公司了解该可能优势的机理提供了线索，该研究提示，仅含EPA的ω-3PUFA补剂对LDL的氧化作用低于EPA/DHA制剂。
7月26日，审批主要是基于为期12周的阶段3MARINE试验的有效性和安全性资料。在该项试验中，甘油三酯水平下降，其他相关标记物的LDL-C水平，包括总胆固醇、载脂蛋白B（apo-B）、脂蛋白相关磷脂酶A2（Lp-PLA2）及高敏感度C反应蛋白（hs-CRP）等，均得到改善。
Amarin称，它正寻求FDA单独批准Vascepa用于使用他汀类药物的高甘油三酯患者，也就是ANCHOR试验所研究的人群。ANCHOR试验曾被heartwire报道过，并于7月20日发表在《美国心脏病学杂志》上[Am J Cardiol,2012-07-20]。值得注意的是，在ANCHOR试验中，在他汀类药物中每天添加4gVascepa显著降低LDL-C水平(p=0.0067)。
MARINE和ANCHOR均未对临床结果进行检查。
Amarin最近推进的另外一项随机试验，即“EPA治疗减少心血管事件—干预试验（REDUCE-IT）”，在该试验中，Vascepa被添加到接受他汀治疗的甘油三酯升高伴冠状动脉疾病或CAD风险因子的“高危”患者治疗中，其主要终点包括心血管事件率。
据Amarin公司介绍，REDUCE-IT试验正在以美国为主的全球约300个地方进行，并其目标登记人数为8000左右，计划用6年时间完成。

“Vascepa获批意味着一种针对重度高甘油三酯血症患者的重要新型治疗方法被引入到临床。在Amarin开展的一项名为MARINE的临床试验中，Vascepa能够显著性降低用安慰剂校正的甘油三酯水平，而不会升高低密度脂蛋白胆固醇水平（即通常所称”坏胆固醇“），”Amarin公司总裁兼CEOJoseph Zakrzewski表示。“Amarin预期会在2013年第一季度将Vascepa推向市场，公司正考虑以三种可能方式进行该药的市场营销及产品销售：Amarin被别的公司收购、战略性合作或自主商业开发，后者包括第三方支持。我们想在正致力于Vascepa销售筹备工作，包括但不限于：向管理式医疗保健计划介绍Vascepa以获得处方权，建立库存水平以及其它上市前的协调工作。”
Amarin在名为MARINE的临床试验中评估了Vascepa的有效性和安全性，这是一项随机、安慰剂对照、双盲、平行设计的临床试验，在空腹甘油三酯水平极高（介于500 mg/dL和 2000 mg/d之间）患者中间开展。在基线期，25%患者联合使用他汀类治疗，28%患者患有糖尿病，39%患者甘油三酯水平＞750 mg/dL。患者应用4g Vascepa治疗12周后显示：用安慰剂校正的平均甘油三酯水平较显著性降低33%(p<0.001)，LDL-C水平与安慰剂组相比未见升高。与基线期相比，Vascepa 4g/d 还可以显著性降低非HDL-C（总胆固醇减去好胆固醇）、总胆固醇（TC）、极低密度脂蛋白胆固醇（VLDL-C)18%、载脂蛋白B(Apo B)，降幅分别为18%、16%、29%、9%。
Vascepa治疗患者最常见的不良反应（发生率＞2%，并且高于安慰剂组）为关节痛（Vascepa 2.3% vs.安慰剂 1.0% ）。
Generic Name: icosapent ethyl
Date of Approval: July 26, 2012
Company: Amarin Corporation plc
Treatment for: Vascepa
FDA Approves Vascepa
The U.S. Food and Drug Administration (FDA) has approved Vascepa (icosapent ethyl) capsules as an adjunct to diet to reduce triglyceride (TG) levels in adult patients with severe (TG greater than or equal to 500mg/dL) hypertriglyceridemia (very high triglycerides).
Vascepa (icosapent ethyl) capsules, known in scientific literature as AMR101, is a patented, ultra-pure omega-3 fatty acid product, comprising not less than 96% EPA in a 1 gram capsule.
The daily dose of Vascepa is 4 grams administered orally. Patients should engage in appropriate nutritional intake and physical activity before receiving Vascepa, which should continue during treatment.
Important Safety Information
Attempts should be made to control any medical problems such as diabetes mellitus, hypothyroidism and alcohol intake that may contribute to the lipid abnormalities. Lipid levels should be consistently abnormal before initiating Vascepa.
Medications affecting coagulation (e.g., anti-platelet agents) should be monitored periodically.
In patients with hepatic impairment, alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels should be monitored periodically during therapy. Use with caution in patients with known hypersensitivity to fish and/or shellfish.
The most commonly reported adverse reaction (incidence >2% and greater than placebo) in Vascepa treated patients was arthralgia (joint pain) (2.3% for Vascepa vs. 1.0% for placebo).
Vascepa Patient Information
Read this Patient Information before you start taking Vascepa and each time you get a refill. There may be new information. This information does not take the place of talking with your doctor about your medical condition or your treatment.
What is Vascepa?
Vascepa is a prescription medicine used along with a low-fat and low-cholesterol diet to lower high levels of triglycerides (fats) in adults.
It is not known if Vascepa changes your risk of having inflammation of your pancreas (pancreatitis).
It is not known if Vascepa prevents you from having a heart attack or stroke.
It is not known if Vascepa is safe and effective in children.
Who should not take Vascepa?
Do not take Vascepa if you are allergic to icosapent ethyl or any of the ingredients in Vascepa. See the end of this leaflet for a complete list of ingredients in Vascepa.
Before taking Vascepa
Before you take Vascepa, tell your doctor if you:
•have diabetes.
•have a low thyroid problem (hypothyroidism).
•have a liver problem.
•have a pancreas problem.
•are allergic to fish or shellfish. It is not known if people who are allergic to fish or shellfish are also allergic to Vascepa.
•are pregnant, or planning to become pregnant. It is not known if Vascepa will harm your unborn baby.
•are breastfeeding or plan to breastfeed. Vascepa can pass into your milk, and may harm your baby. Talk to your doctor about the best way to feed your baby if you take Vascepa.
Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and dietary or herbal supplements.
Vascepa can interact with certain other medicines that you are taking.
Especially tell your doctor if you take medicines that affect your blood clotting (anticoagulants or blood thinners).
Know the medicines you take. Keep a list of them to show your doctor and pharmacist when you get a new medicine.
How should I take Vascepa?
•Take Vascepa exactly as your doctor tells you to take it.
•Do not change your dose or stop taking Vascepa without talking to your doctor.
•You should not take more than 4 capsules of Vascepa each day. Do not take more capsules than what is prescribed by your doctor.
•Take Vascepa capsules whole. Do not break, crush, dissolve, or chew Vascepa capsules before swallowing.
•If you miss a dose of Vascepa, take it as soon as you remember. However, if you miss one day of Vascepa, do not double your dose when you take it.
•Your doctor may start you on a diet that is low in saturated fat, cholesterol, carbohydrates, and low in added sugars before giving you Vascepa. Stay on this diet while taking Vascepa.
•Your doctor may do blood tests to check your triglyceride and other lipid levels while you take Vascepa.
Vascepa side effects
If you have liver problems and are taking Vascepa, your doctor should do blood tests during treatment.
The most common side effect of Vascepa is joint pain. As with all drugs, you may experience a serious side effect when taking Vascepa. Talk to your doctor if you have a side effect that bothers you or does not go away.
This is not the only side effect of Vascepa. For more information, ask your doctor or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1- 800-FDA-1088.
How should I store Vascepa?
•Store Vascepa at room temperature between 68° to 77° F (20° to 25° C).
•Safely throw away medicine that is out of date or no longer needed.
Keep Vascepa and all medicine out of the reach of children.
General information about the safe and effective use of Vascepa
Medicines are sometimes prescribed for purposes other than those listed in Patient Information Leaflets. Do not use Vascepa for a condition for which it was not prescribed. Do not give Vascepa to other people, even if they have the same symptoms you have. It may harm them.
This Patient Information summarizes the most important information about Vascepa. If you would like more information, talk with your doctor or pharmacist. You can ask your doctor or pharmacist for information about Vascepa that is written for health professionals.