Huber K
Universitätsklinik für Innere Medizin II, Universität Wien, Osterreich.
Wien Klin Wochenschr. 2000 Sep 15;112(17):742-8.
Thrombolysis is a milestone in the therapy of acute myocardial infarction due to its ubiquitous availability and ease of application. The recombinant form of tissue-type plasminogen activator (rt-PA) has been proven to be superior over first generation fibrinolytic agents (streptokinase, urokinase, APSAC) with respect to efficacy and side effects and the front-loaded regimen has meanwhile become the "gold"-standard of thrombolytic therapy. Biochemically modified mutants of wild-type t-PA, e.g. r-PA (reteplase), n-PA (lanoteplase), and TNK-t-PA have altered biochemical and pharmacokinetic characteristics which make them more easy to use (as double or single bolus injection) and share a theoretical efficacy benefit. This article describes these specific characteristics focussing on clot-selectivity and PAI-1 resistance of the new mutants of wild-type t-PA and their possible clinical efficiency.
溶栓疗法因其广泛可用性和易于应用，成为急性心肌梗死治疗中的一个里程碑。重组组织型纤溶酶原激活剂（rt-PA）在疗效和副作用方面已被证明优于第一代纤溶药物（链激酶、尿激酶、茴香酰化纤溶酶原链激酶激活剂复合物），同时，加速给药方案已成为溶栓治疗的“金”标准。野生型t-PA的生化修饰突变体，如r-PA（瑞替普酶）、n-PA（兰替普酶）和TNK-t-PA，具有改变的生化和药代动力学特性，这使得它们更易于使用（可单次或两次静脉推注），并在理论上具有疗效优势。本文描述了这些特殊特性，重点关注野生型t-PA新突变体的凝块选择性和对纤溶酶原激活物抑制剂-1（PAI-1）的抗性及其可能的临床疗效。
