Mazurov A V, Pevzner D V, Semenov A V, Antonova O A, Dudnik O A, Khaspekova S G, Vlasik T N, Samko A N, Staroverov I I, Ruda M Ia
Kardiologiia. 2002;42(6):8-17.
Preparation framon [F(ab')2 fragments of the anti-glycoprotein (GP) IIb/IIIa monoclonal antibody (FRaMon)] blocks fibrinogen binding to GP IIb/IIIa and platelet aggregation. Dynamics of platelet aggregation inhibition, safety, and clinical effects of framon were studied in high-risk coronary angioplasty. Twenty seven patients underwent angioplasty with framon, 29 - with abciximab and 28 - with no GP IIb/IIIa antagonists. Framon at 0.2 mg/kg (n=16) and 0.25 mg/kg (n=11) bolus administration inhibited platelet aggregation induced by 20 mcM ADP by more than 90%, 80%, 60% and 30% in comparison with the predrug level 1, 12, 24 and 72 h after injection, respectively. Almost the same dynamics of aggregation inhibition was observed upon abciximab administration at 0.25 mg/kg bolus + 0.125 mcg/kg/min infusion for 12 h. No signs of individual intolerance and side effects including allergic reactions and bleedings were detected in patients treated with framon. Slight decrease of platelet count (15-20%) was observed on the first day after framon administration. Antibodies against framon were detected in 1 out of 22 tested patients. Free (nonbound to platelets) framon was completely removed from the circulation 12 h after injection. The number of endpoints (death, myocardial infarction and indications for repeat revascularization) within 1 year after angioplasty was approximately the same in the groups with framon and abciximab - 7 of 25 (28%) and 7 of 28 (25%), respectively, and more than 1.5 fold higher in the group without GP IIb/IIIa blockers - 12 of 27 (44,4%).
抗糖蛋白（GP）IIb/IIIa单克隆抗体片段（FRaMon）可阻断纤维蛋白原与GP IIb/IIIa的结合以及血小板聚集。在高危冠状动脉血管成形术中研究了FRaMon抑制血小板聚集的动力学、安全性及临床效果。27例患者接受了使用FRaMon的血管成形术，29例使用阿昔单抗，28例未使用GP IIb/IIIa拮抗剂。0.2mg/kg（n = 16）和0.25mg/kg（n = 11）静脉推注的FRaMon，与注射前水平相比，分别在注射后1、12、24和72小时抑制20μM ADP诱导的血小板聚集超过90%、80%、60%和30%。以0.25mg/kg静脉推注+0.125μg/kg/min输注12小时给予阿昔单抗后，观察到几乎相同的聚集抑制动力学。接受FRaMon治疗的患者未检测到个体不耐受迹象和包括过敏反应及出血在内的副作用。在给予FRaMon后的第一天观察到血小板计数略有下降（15 - 20%）。在22例接受检测的患者中有1例检测到抗FRaMon抗体。游离（未与血小板结合）的FRaMon在注射后12小时从循环中完全清除。血管成形术后1年内，使用FRaMon和阿昔单抗的组中终点事件（死亡、心肌梗死和再次血管重建指征）的数量大致相同，分别为25例中的7例（28%）和28例中的7例（25%），而未使用GP IIb/IIIa阻滞剂的组中该数量则高出1.5倍以上，为27例中的12例（44.4%）。
