纤溶酶及其衍生物溶栓研究进展

Thrombolysis of plasmin and its derivatives:research advances

当前批准使用的溶栓药物均为纤溶酶原激活剂,其应用受到出血并发症和血栓部位纤溶酶原含量不足的限制。而纤溶酶可被α2-抗纤溶酶迅速中和,避免了出血风险。随着导管输送技术的应用,纤溶酶特有的生化性质使其成为安全有效的直接溶栓药物,小纤溶酶、Δ-纤溶酶、微小纤溶酶等纤溶酶衍生物在临床前及临床试验中亦表现出较高的溶栓效率和较好的止血安全性。本文将对纤溶酶及其衍生物在生化性质、临床前和临床研究等方面取得的进展进行综述。

All of the thrombolytic agents currently approved for use in humans are plasminogen activators, the application of which is limited by bleeding complications at vascular injury sites and plasminogen content in the thrombus. Plasmin is rapidly neutral- ized in the circulation by α2-antiplasmin and tolerated without bleeding. With the application of catheter-based delivery, the unique bio- chemical properties of plasmin make it a safe and effective direct fibrinolytics. Plasmin derivatives, including miniplasmin, △-plasmin and microplsmin, display more thrombolysis efficacy and better hemostatic safety in preclinical study and clinical trials. This review sum- marizes the current information on plasmin and its derivatives, including the advances on biochemical properties, preclinical and clinical trials.