Platelet GPIIb/IIIa antagonists: The first anti-integrin receptor therapeutics

Platelet GPIIb/IIIa antagonists: The first anti-integrin receptor therapeutics
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DOI:
10.1172/jci119307
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发表时间:
1997-04-01
影响因子:
15.9
通讯作者:
Coller, BS
Coller, BS
中科院分区:
医学1区
文献类型:
--
作者:
Coller, BS

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血小板膜糖蛋白GPIIb/IIIa(IIb3)拮抗剂C7E3Fab(鼠/人嵌合单抗7E3的Fab片段;阿昔单抗;ReoPro™)于1994年12月在美国获准用于人类,原因是它的安全性和降低经皮冠状动脉介入治疗(PCI;1血管成形术或动脉粥样硬化切除术)后缺血性并发症的有效性(1,2)。这种药物的成功反映了我们正在形成的能力,即识别黏附分子作为治疗靶点,然后构建符合新药所需严格安全标准的有效抑制剂。作为第一个合理设计的抗血小板和抗整合素受体药物,C7E3Fab是其他抗整合素受体,更广泛地说,是用于治疗和/或预防人类疾病的抗黏附受体的原型。
The platelet glycoprotein GPIIb/IIIa (IIb 3) antagonist c7E3 Fab (the Fab fragment of the mouse/human chimeric monoclonal antibody 7E3; abciximab; ReoPro™) was approved for human use in the United States in December 1994 based on its safety and its efficacy in reducing the risk of ischemic complications after percutaneous coronary intervention (PCI; 1 angioplasty or atherectomy)(1, 2). The success of this agent reflects our emerging ability to identify adhesion molecules as therapeutic targets, and then construct effective inhibitors that meet the stringent safety standards required for a new drug. As the first rationally designed antiplatelet and anti-integrin receptor drug, c7E3 Fab serves as a prototype for other anti-integrin receptor, and more generally, antiadhesion receptor, agents designed to treat and/or prevent human disease.