New Antiplatelet Agents: Platelet GPIIb/llla Antagonists
New Antiplatelet Agents: Platelet GPIIb/llla Antagonists
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新型抗血小板药物：血小板 GPIIb/IIIa 拮抗剂
DOI：
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发表时间：
1995
影响因子：
6.7
通讯作者：
H. Weisman
中科院分区：
文献类型：
--
作者：
B. Coller;K. Anderson;H. Weisman
GPIIb/IIIa （α IIb β 3）受体在血小板聚集和血小板血栓形成中起重要作用。用小鼠/人嵌合单克隆抗体7E3的Fab片段、含有精氨酸-甘氨酸-天冬氨酸（RGD）序列的蛇毒肽或基于RGD序列的肽或肽拟物抑制GPIIb/IIIa，可消除血小板聚集和血小板血栓形成。这在动物模型中导致血栓闭塞的深刻抑制。III期EPIC研究表明，在冠状动脉成形术后急性缺血性并发症的高风险患者中，c7E3 Fab作为大剂量给药，然后输注12小时，可将此类并发症的风险降低约35%。接受治疗的患者大出血风险增加了2倍，但脑出血或致死性出血没有增加。使用c7E3 Fab治疗可能对6个月时的临床再狭窄有有益的影响，但这需要证实。在EPIC中也发现了c7E3 Fab可能的抗凝作用，并且体外研究支持了这种可能性。随着c7E3 Fab （abciximab; ReoPro）在美国和几个欧洲和斯堪的纳维亚国家被批准用于高危血管成形术患者，GPIIb/IIIa抑制剂加入了抗血栓药物的行列。
The GPIIb/IIIa (α IIb β 3 ) receptor plays a crucial role in platelet aggregation and platelet thrombus formation. Inhibition of GPIIb/IIIa with the Fab fragment of the mouse/human chimeric monoclonal antibody 7E3, snake venom peptides containing the arginine-glycine-aspartic acid (RGD) sequence, or peptides or peptidomimetics based on the RGD sequence results in abolition of platelet aggregation and platelet thrombus formation. This results in profound inhibition of thrombotic occlusions in animal models. The Phase III EPIC study demonstrated that c7E3 Fab, given as bolus followed by a 12 h infusion, reduced the risk of acute ischemic complications after coronary angioplasty by ∼35 % in patients at high risk of suffering such complications. Treated patients had an ∼2-fold increased risk of major bleeding, but no increase in cerebral hemorrhage or lethal bleeding. Treatment with c7E3 Fab may have had a beneficial effect on clinical restenosis at 6 months, but this needs to be confirmed. A possible anticoagulant effect of c7E3 Fab was also identified in EPIC, and in vitro studies support this possibility. With the approval of c7E3 Fab (abciximab ; ReoPro) for patients undergoing high-risk angioplasty in the US and several European and Scandinavian countries, GPIIb/IIIa inhibition joins the armamentarium of antithrombotic agents.
影响因子：
20.3
作者：
D. Phillips;I. Charo;L. Parise;L. Fitzgerald
通讯作者：
D. Phillips;I. Charo;L. Parise;L. Fitzgerald
影响因子：
56.9
作者：
PYTELA, R;PIERSCHBACHER, MD;RUOSLAHTI, E
通讯作者：
RUOSLAHTI, E