Coller B S, Anderson K M, Weisman H F
Mount Sinai School of Medicine, New-York, NY 10128, USA.
Haemostasis. 1996 Oct;26 Suppl 4:285-93. doi: 10.1159/000217309.
The platelet GPIIb/IIIa receptor mediates platelet aggregation induced by all physiologic agonists. Blockade of the receptor, either by monoclonal antibodies or small molecules patterned after the arginine glycine-aspartic acid (RGD) cell recognition domain, prevents arterial thrombosis in animal models much better than does aspirin. c7E3 Fab, the Fab fragment of the mouse/human chimeric antibody 7E3 (abciximab: ReoPro), was shown to reduce ischemic events after angioplasty when given in conjunction with heparin and aspirin to patients at high risk in the EPIC study, but its was associated with an increase in bleeding. Preliminary data from the subsequent EPILOG study, in which a lower dose of heparin was used, demonstrated efficacy in low risk as well as high risk patients and no significant increase in major bleeding. Preliminary data from the CAPTURE study support the use of c7E3 Fab in patients with unstable angina who are candidates for PTCA within 24 hours. Positive trends toward decreased thrombotic events have also been observed in patients treated with small molecule inhibitors of GPIIb/IIIa receptors. This new class of agents thus holds promise for improving the therapy of angioplasty as well as perhaps other thrombotic phenomena.
血小板糖蛋白IIb/IIIa受体介导所有生理性激动剂诱导的血小板聚集。通过单克隆抗体或模仿精氨酸 - 甘氨酸 - 天冬氨酸（RGD）细胞识别域的小分子阻断该受体，在动物模型中预防动脉血栓形成的效果比阿司匹林好得多。在EPIC研究中，给高危患者联合使用肝素和阿司匹林时，小鼠/人嵌合抗体7E3（阿昔单抗：ReoPro）的Fab片段c7E3 Fab显示可减少血管成形术后的缺血事件，但其与出血增加有关。随后的EPILOG研究的初步数据表明，使用较低剂量肝素时，在低风险和高风险患者中均有效，且大出血无显著增加。CAPTURE研究的初步数据支持在24小时内适合进行经皮冠状动脉腔内血管成形术（PTCA）的不稳定型心绞痛患者中使用c7E3 Fab。在用糖蛋白IIb/IIIa受体小分子抑制剂治疗的患者中也观察到血栓形成事件减少的积极趋势。因此，这类新型药物有望改善血管成形术以及其他血栓形成现象的治疗。
