Cohen S A, Trikha M, Mascelli M A
Cenrocor Inc. 200 Great Valley Parkway, Malvern, PA 19355, USA.,
Pathol Oncol Res. 2000;6(3):163-74. doi: 10.1007/BF03032368.
Abciximab (ReoPro) is a mouse-human chimeric monoclonal antibody Fab fragment of the parent murine monoclonal antibody 7E3, and was the first of these agents approved for use as adjunct therapy for the prevention of cardiac ischemic complications in patients undergoing percutaneous coronary intervention (PCI). Abciximab binds with high avidity to both the non-activated and activated form of the GPIIb/IIIa receptor of platelets, the major adhesion receptor involved in aggregation. Additional cardiovascular indications for abciximab are unstable angina, carotid stenting, ischemic stroke and peripheral vascular diseases. Abciximab also interacts with two other integrin receptors; the a av b b3 receptor, which is present in low numbers on platelets but in high density on activated endothelial and smooth muscle cells, and a aMb b2 integrin which is present on activated leukocytes. Cell types that express integrins GPIIb/IIIa and a av b b3 such as platelets, endothelial and tumor cells have been implicated in angiogenesis, tumor growth and metastasis. Since abciximab interacts with high avidity to integrins GPIIb/IIIa and a av b b3, it is reasonable to assume that it may possess anti-angiogenic properties in angiogenesis-related diseases, as well as anti-metastastatic properties in case of disseminating tumors expressing the target integrin receptors.
阿昔单抗（ReoPro）是亲本鼠单克隆抗体7E3的鼠-人嵌合单克隆抗体Fab片段，是这些药物中首个被批准用作辅助治疗，以预防接受经皮冠状动脉介入治疗（PCI）患者心脏缺血性并发症的药物。阿昔单抗与血小板的GPIIb/IIIa受体的非活化和活化形式均具有高亲和力结合，GPIIb/IIIa受体是参与聚集的主要黏附受体。阿昔单抗的其他心血管适应症包括不稳定型心绞痛、颈动脉支架置入术、缺血性中风和外周血管疾病。阿昔单抗还与另外两种整合素受体相互作用；αvβ3受体，其在血小板上数量较少，但在活化的内皮细胞和平滑肌细胞上高密度存在，以及αMβ2整合素，其存在于活化的白细胞上。表达整合素GPIIb/IIIa和αvβ3的细胞类型，如血小板、内皮细胞和肿瘤细胞，已被认为与血管生成、肿瘤生长和转移有关。由于阿昔单抗与整合素GPIIb/IIIa和αvβ3具有高亲和力相互作用，因此可以合理推测，它在血管生成相关疾病中可能具有抗血管生成特性，以及在表达靶整合素受体的播散性肿瘤情况下具有抗转移特性。
