SUNY Downstate Medical Center, Brooklyn, New York.
Semin Neurol. 2021 Feb;41(1):28-38. doi: 10.1055/s-0040-1722722. Epub 2021 Jan 20.
The introduction of thrombolytic therapy in the 1990s has transformed acute ischemic stroke treatment. Thus far, intravenous recombinant tissue plasminogen activator (rt-PA) also known as alteplase is the only thrombolytic proven to be efficacious and approved by the United States Food and Drug Administration. But the thrombolytic agent tenecteplase (TNK) is emerging as a potential replacement for rt-PA. TNK has greater fibrin specificity, slower clearance, and higher resistance to plasminogen activator inhibitor-1 than rt-PA. Hence, TNK has the potential to provide superior lysis with fewer hemorrhagic complications. Also, easier bolus-only administration makes TNK a very practical rt-PA alternative. In several clinical trials, TNK has shown similar efficacy and safety to rt-PA, and the potential to be at least noninferior to rt-PA in some settings. TNK may be superior to rt-PA for reperfusing large vessel occlusions in patients with salvageable penumbra, although this has not yet translated to improved clinical outcomes. Further phase 3 studies are in progress comparing rt-PA with TNK for acute ischemic stroke during the first 4.5 hours. Studies are also in progress to evaluate the use of TNK for extended applications, such as wake-up stroke.
20 世纪 90 年代，溶栓疗法的引入改变了急性缺血性脑卒中的治疗模式。迄今为止，只有静脉注射重组组织型纤溶酶原激活剂（rt-PA），也称为阿替普酶，被证明是有效的，并获得了美国食品和药物管理局的批准。但新型溶栓药替奈普酶（TNK）正在成为 rt-PA 的潜在替代品。TNK 具有更高的纤维蛋白特异性、更慢的清除率和更高的对纤溶酶原激活物抑制剂-1 的抗性，因此，TNK 有可能在减少出血并发症的同时提供更好的溶栓效果。此外，因其易于推注给药，TNK 是一种非常实用的 rt-PA 替代药物。在几项临床试验中，TNK 与 rt-PA 的疗效和安全性相似，并且在某些情况下有至少不劣于 rt-PA 的潜力。TNK 可能优于 rt-PA 用于再通有可挽救半暗带的大血管闭塞患者，但这尚未转化为改善临床结局。目前正在进行比较 rt-PA 与 TNK 在发病 4.5 小时内治疗急性缺血性脑卒中的 3 期研究。此外，还在进行研究以评估 TNK 在扩展应用（如唤醒性脑卒中）中的应用。
