基本信息来源于合作网站,原文需代理用户跳转至来源网站获取       
摘要:
Significant progress was achieved in the search of a thrombin receptor antagonist as a novel antithrombotic treatment since the thrombin receptor (protease-activated receptor-1, PAR-1) was cloned 20 years ago. Previous works have shown that it is possible to develop potent thrombin receptor antagonists to compete effectively with the receptor’s internal “tethered” ligand to block platelet activation. Vorapaxar (SCH 530348) from Schering-Plough (now Merck) and atopaxar (E5555) from Eisai have been advanced to human clinical trials. Recently, the pivotal phase III clinical trial results for vorapaxar were published. In this article we review these results plus the phase II results from atopaxar. Several newly described thrombin receptor antagonists from the literature will also be discussed. The phase III results from vorapaxar demonstrated that a thrombin receptor antagonist can achieve efficacy in addition to current standard- of-care in treating atherothrombotic patients, especially those with previous myocardial infarction (MI). However, the increased moderate and severe bleeding, especially intracranial bleeding, point to the limitations of current thrombin receptor antagonists. Future thrombin receptor antagonists that can improve on the efficacy and bleeding profile of current ones should have a promising place in meeting the unmet medical need in treating atherothrombotic patients using current standard therapy.
推荐文章
Application analysis of novel purple sweet corn inbred line development for hybrid nutrient-rich fru
紫甜玉米
自交系
Smith-Hazel指数
一般配合力(GCA)
Line×Tester模型
构建 SLE 患者 novel microRNA 差异性表达谱及其靶基因的功能分析
系统性红斑狼疮
新小核糖核酸
靶基因
差异性表达
GO 富集
KEGG 通路
化感--外来入侵植物的"Novel Weapons"
化感
外来入侵植物
NW假说
内容分析
关键词云
关键词热度
相关文献总数  
(/次)
(/年)
文献信息
篇名 Recent Development in Thrombin Receptor Antagonist as Novel Antithrombotic Agent
来源期刊 药物化学期刊(英文) 学科 医学
关键词 THROMBIN Receptor ANTAGONIST PAR-1 ANTAGONIST VORAPAXAR ANTITHROMBOTIC Review
年,卷(期) 2012,(4) 所属期刊栏目
研究方向 页码范围 112-118
页数 7页 分类号 R73
字数 语种
DOI
五维指标
传播情况
(/次)
(/年)
引文网络
引文网络
二级参考文献  (0)
共引文献  (0)
参考文献  (0)
节点文献
引证文献  (0)
同被引文献  (0)
二级引证文献  (0)
2012(0)
  • 参考文献(0)
  • 二级参考文献(0)
  • 引证文献(0)
  • 二级引证文献(0)
研究主题发展历程
节点文献
THROMBIN
Receptor
ANTAGONIST
PAR-1
ANTAGONIST
VORAPAXAR
ANTITHROMBOTIC
Review
研究起点
研究来源
研究分支
研究去脉
引文网络交叉学科
相关学者/机构
期刊影响力
药物化学期刊(英文)
季刊
2164-3121
武汉市江夏区汤逊湖北路38号光谷总部空间
出版文献量(篇)
64
总下载数(次)
0
论文1v1指导