发明名称 |
THROMBUS-TARGETED COMPLEXES OF PLASMINOGEN ACTIVATOR AND FIBRIN FRAGMENTS. |
摘要 |
<p>Thrombolytic hybrids are formed as covalent or non-covalent complexes of fibrin fragments and plasminogen activator molecules. Native plasmin degradation fragments of fibrin or non-native fibrin fragments are covalently or non-covalently linked to plasminogen activators such as t-PA, scu-PA, urokinase, streptokinase, and the like. Useful native fibrin fragments which may be utilized to form complexes with plasminogen activators include fragments E1, E2, E3, D and DD, and (DD)E complex. The fibrin fragment component targets the hybrid to vascular thrombi, immobilizing the plasminogen activator molecule onto the fibrin surface of the thrombus. Once localized on a thrombus surface, the plasminogen activator component of the hybrid activates only the clot-surface bound plasminogen transported by the fibrin fragment vehicle, without significant systemic activation of plasminogen. The hybrids are strong potentiators of plasminogen activator activity, generating more plasmin from fibrin-surface bound plasminogen than the plasminogen activator molecule alone. The hybrids have a longer half-life in circulation than the corresponding unprotected plasminogen activator molecules.</p> |
申请公布号 |
EP0473689(B1) |
申请公布日期 |
1994.12.14 |
申请号 |
EP19900908772 |
申请日期 |
1990.05.21 |
申请人 |
TEMPLE UNIVERSITY OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION |
发明人 |
BUDZYNSKI, ANDREI, Z.;KNIGHT, LINDA, C.;HASAN, AHMED, AK. |
分类号 |
A61K38/46;A61K38/00;A61K38/49;C07K1/113;C07K14/435;C07K14/75;C07K19/00;C12N9/64;C12N9/72;(IPC1-7):A61K37/54;A61K37/02;C12N9/50;C12N9/70;C07K15/06;A61K37/547 |
主分类号 |
A61K38/46 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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