摘要
尿激酶原或尿激酶型纤溶酶原激活剂具有特异性溶解血栓作用，引起人们的极大兴趣。西方国家1986年开始进行临床研究，A-74187或Sp2／0表达的糖基化尿激酶原以及大肠杆菌表达的非糖基化尿激酶原治疗急性心肌梗死阻塞相关血管开通率为70％-80％。德国Grllnenthal公司用大肠杆菌表达的非糖基化尿激酶原（Saruplase）治疗急性心肌梗死研究采用20mg推注，60mg／60min滴注，分别与重组组织型纤溶酶原激活剂、尿激酶、链激酶进行比较，并做了1698名心肌梗死患者的开放性临床试验，梗塞相关血管的开通率达到70％～80％。Saruplase与链激酶在104个临床研究中心，入组3089名急性心肌梗死患者进行大规模临床试验。结果表明，Saruplase对阻塞相关血管开通率、30天死亡率、出血合并症等副作用与链激酶没有明显差异，而出血性中风发生率高于链激酶，欧盟未批准Saru．plase上市。国产重组人尿激酶原也进行了探索研究，用于治疗急性心肌梗死给药剂量为30～60mg，给药时间为30或60min，阻塞相关血管开通率为63．4％～80．0％，而尿激酶为52．2％～66．7％（平均58．0％）。此外，国外用重组人尿激酶原治疗深层静脉血栓和缺血性中风进行了探索研究，但病例数较少，尚须进一步研究。
Prourokinase（urokinasetype plasminogen activator） is a specific thrombolytic agent and cuases a world of interest. In 1986, Western countries began carry out clinical studies. When the glycosylated prourokinase （A74187） and expressed in mouse myeloma cell（Sp2/0） or nonglyslated prourokinase in E.coli was used to treat cute myocardial infraction, the patency rate of related artery of infarction was 70%80%. The prourokinase ex pressed in E.coli in Germany, Saruplase, was used to treat cute myocardial infraction. First 20 mg of Saruplase was bolus followed by 60 mg of the agents infusion over 60 minutes, and was compared to tissue plasminogen acti vator, urokinase, and streptokinase, respectively, the patency rate of related artery of infarction was 70%80%. The Saruplase was carried out open trial of 3089 patients in 104 center of clinical studies, The results showed, that Saruplase and streptokinase was not difference in patency rate of related artery of infarction, motality in 30 days, and bleeding complication etc., but the incidence rate of stroke was higher than streptokinase. The Saruplase was not approved to go on the market in European Union. The recombinant human prourokinase（rhproUK） made in China was yet carried out clinical studies. The rhproUK was used to treat cute myocardial infarction with ad ministration of dosage from 30 to 60 mg in 30 or 60 minutes and compared with urokinase, patency rate of relat ed artery of infarction was from 63.4% to 80.0%, the patency rate of urokinase was from 52.2% to 66.7% （mean 58.0% ）. In addition in Western countries recombinant human prourokinase was used to treat deep vein thrombsis and stroke, but the patients was miner and still want to explore.
出处
《生物技术通讯》
CAS
2012年第2期294-299,共6页
Letters in Biotechnology
