通用名：（prasugrel HCl，普拉格雷盐酸盐）
适应症：血管成形术后的抗凝（Blood thinner for patients undergoing angioplasty）
生产商：礼来（Eli Lilly）/第一三共（Daiichi Sankyo）
批准日期：7月10日

礼来抗凝血药Effient正式在美国上市

礼来和Daiichi Sankyo公司共同推出的抗凝血药物Effient (prasugrel)已通过FDA批准，该药用于那些进行过血管修复术去除冠状动脉阻塞的患者，以降低他们的凝血风险，但药物标签需附带警示信息

Effient获准的依据是一项13608名受试者参加的临床实验。在实验过程中，对比了这种药物和赛诺菲-安万特和百时美-施贵宝同类畅销药Plavix (clopidogrel)的疗效，受试者均为极有可能突发急性心脏病，需要接受血管修复术的高危患者。

将两组受试者的治疗情况进行对比之后发现，在减少患者非致命性心脏病发作几率上Effient疗效更胜一筹，其中Plavix受试组的发作几率为9.1%，而Effient受试组的发作几率则降到7%。然而，FDA称在死亡病例和心肌梗塞发作率方面，两个受试组的情况相当，而那些出现过心肌梗塞的患者使用Effient后再次发作的几率更高。

FDA还表明，在使用Effient治疗的患者当中，出现致命性出血风险的几率也更高，因此要求该药的标签信息中增加相应的警示说明。此外，FDA提醒那些伴有急性病理性出血、轻微中风/中风或急需进行手术治疗(包括冠状动脉搭桥术)的患者不宜使用这种药物进行治疗。FDA新药监管办公室负责人John Jenkins表示：“医生在确定哪些患者适宜采用Effient时，必须对药物疗效和潜在风险再三衡量。”

礼来首席执行官John Lechleiter称，今年2月份Effient已在欧洲获准，而现在又得到了FDA的认可，这对治疗急性动脉综合症来说是一个重要的进展。

Daiichi Sankyo, Lilly Submit New Drug Application for Investigational Antiplatelet Drug, Prasugrel, with U.S. Food and Drug Administration

TOKYO and INDIANAPOLIS, January 04, 2008 /PRNewswire-FirstCall/ -- Daiichi Sankyo Company, Limited and Eli Lilly and Company today announced that on Wednesday, Dec. 26, 2007, they submitted a New Drug Application (NDA) for prasugrel to the U.S. Food and Drug Administration (FDA). Prasugrel is an oral antiplatelet agent, initially in development for the treatment of patients with acute coronary syndrome (ACS) who are managed with percutaneous coronary intervention (PCI), including coronary stenting.

If approved for marketing in the United States, the trade name for prasugrel will be Effient, company officials added.

"We are elated," said J. Anthony Ware, M.D., Lilly vice president and cardiovascular/acute care platform leader for prasugrel. "We feel confident in the strength and completion of this submission package, and plan to complete our submission in Europe in the first quarter of 2008. The benefit/risk profile of this compound, in comparison with the current standard of care, has the potential to improve outcomes for ACS patients undergoing PCI."

The NDA is based upon data from several trials, including the landmark TRITON-TIMI 38 clinical trial, which evaluated the safety and efficacy of prasugrel compared with clopidogrel (Plavix(R)/Iscover(R)) in reducing ischemic events such as non-fatal heart attack, non-fatal stroke and cardiovascular death in 13,608 patients. In the study, treatment with prasugrel resulted in a:

• 19 percent relative risk reduction compared with clopidogrel in all ACS patients in the primary composite endpoint of non-fatal heart attack, non-fatal stroke or cardiovascular death (p<0.001).
  
• 52 percent reduction compared with clopidogrel in stent thrombosis (p<0.0001).
  
• 30 percent relative risk reduction compared to clopidogrel in a subset of patients with diabetes (p<0.001) on the composite endpoint of non-fatal heart attack, non-fatal stroke, or cardiovascular death.

Risk reductions in the primary composite endpoint with prasugrel compared to clopidogrel were seen as early as three days and continued to diverge for 15 months (the duration of the trial.)

Though the incidence of non-coronary artery bypass grafting(non-CABG) bleeding in TRITON was low in both the prasugrel and clopidogrel treatment groups, prasugrel-treated patients experienced significantly higher non-CABG major bleeding (2.2% vs. 1.7%, respectively) and higher rates of life- threatening bleeding (1.3% vs. 0.8%, respectively). Death from cardiovascular causes (2% vs. 2.2%, respectively) and all-cause death (2.8% vs. 2.9%, respectively) was comparable among prasugrel-treated patients and clopidogrel- treated patients. The overall results demonstrated that for every 1,000 patients treated with prasugrel as compared with clopidogrel, there were 22 fewer patients with heart attacks and five more non-CABG-related TIMI major bleeds.

"Given the overall results from TRITON, this submission is particularly meaningful considering that cardiovascular disease is the leading cause of death in the United States and worldwide, killing 16.7 million people each year," said John Alexander, M.D., M.P.H., global head of research and development, Daiichi Sankyo Company, Limited.

Acute heart attacks and unstable angina, called acute coronary syndrome, affect more than 840,000 Americans each year and 800,000 people in Europe. Utilizing current medical interventions and treatments, 300,000 people continue to experience recurrent heart attacks and 450,000 people die from heart attacks annually in the U.S.

About prasugrel
Daiichi Sankyo Company, Limited , and Eli Lilly and Company are co-developing prasugrel, an investigational oral antiplatelet agent invented by Daiichi Sankyo and its Japanese research partner Ube Industries, Ltd., as a potential treatment, initially for patients with acute coronary syndrome who are managed with PCI. Prasugrel works by inhibiting platelet activation and subsequent aggregation by blocking the P2Y12 adenosine diphosphate (ADP) receptor on the platelet surface. Antiplatelet agents prevent platelets from clumping or sticking together, which can result in clogged arteries and may lead to heart attack or stroke.

About Daiichi Sankyo Company, Limited
Daiichi Sankyo Company, Limited, established in 2005 after the merger of two leading century-old Japanese pharmaceutical companies, is a global pharmaceutical innovator, continuously generating innovative drugs that enrich the quality of life for patients around the world. The company uses its cumulative knowledge and expertise in the fields of cardiovascular disease, cancer, metabolic disorders, and infection as a foundation for developing an abundant product lineup and R&D pipeline.

About Eli Lilly and Company
Lilly, a leading innovation-driven corporation, is developing a growing portfolio of first in class and best-in-class pharmaceutical products by applying the latest research from its own worldwide laboratories and from collaborations with eminent scientific organizations. Headquartered in Indianapolis, Ind., Lilly provides answers - through medicines and information - for some of the world's most urgent medical needs.