Walker I D, Davidson J F, Rae A P, Hutton I, Lawrie T D
Thromb Haemost. 1984 Apr 30;51(2):204-6.
BRL 26921 is the p- anisoyl derivative of the primary streptokinase-human plasminogen complex in which the acyl group is specifically located at the catalytic centre of the enzyme. Doses of BRL 26921 ranging from 5 mg to 25 mg were given intravenously or into a coronary artery to 12 patients with acute myocardial infarction. The complex was well tolerated and produced no serious bleeding. Coronary artery reperfusion was demonstrated angiographically in three patients. In most patients, fibrinogen, plasminogen, alpha 2 antiplasmin and alpha 2 macroglobulin levels fell and the level of fibrinogen degradation products increased acutely post treatment indicating systemic fibrinolytic activation. The degree of this activation was variable but was profound in some. It appeared to be dose related and modified by the presence of streptokinase antibodies. BRL 26921 appears less "selectively" thrombolytic in patients than had been expected from animal models.
BRL 26921是链激酶-人纤溶酶原初级复合物的对茴香酰衍生物,其中酰基特异性地位于酶的催化中心。对12例急性心肌梗死患者静脉内或冠状动脉内给予剂量范围为5毫克至25毫克的BRL 26921。该复合物耐受性良好,未产生严重出血。3例患者经血管造影证实冠状动脉再灌注。在大多数患者中,治疗后纤维蛋白原、纤溶酶原、α2抗纤溶酶和α2巨球蛋白水平下降,纤维蛋白原降解产物水平急剧升高,表明全身纤溶激活。这种激活程度各不相同,但在一些患者中很显著。它似乎与剂量相关,并受链激酶抗体的存在影响。BRL 26921在患者中的溶栓作用似乎不如动物模型所预期的那样“具有选择性”。