Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery
Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery
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DOI：
10.1517/14712598.8.8.1187
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发表时间：
2008-08-01
影响因子：
4.6
通讯作者：
Lehmann, Andreas
中科院分区：
文献类型：
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作者：
Lehmann, Andreas
背景：血浆激肽释放酶在接触性(激肽释放酶-激动素)级联反应中起主要作用。缓激肽是一种血管扩张剂，可以增加血管通透性，激活炎症，产生疼痛。血浆激肽释放酶也与凝血系统和补体级联反应有关。目的：依卡兰特(DX-88)是一种高效、特异的血浆激肽释放酶抑制剂。Ecalantide是一种基于人类组织因子途径抑制物的第一个kunitz结构域的重组生产和工程的小蛋白。通过噬菌体展示技术对其进行鉴定。方法：应用计算机检索Pubmed/Medline、临床试验和Google数据库，检索词“ecallantide”、“TX-88”和“遗传性血管性水肿”。结果/结论：目前，该药正在研究两个主要适应症。首先，遗传性血管性水肿的治疗结果是有希望的。第二，一项关于减少体外循环心胸外科手术中失血量的前瞻性随机多中心试验将于2008年10月终止。
Background: Plasma kallikrein plays a major role in the contact (kallikrein-kinin) cascade producing bradykinin. Bradykinin is a vasodilator, which increases vascular permeability, activates inflammation and produces pain. Plasma kallikrein is also crosslinked to the coagulation system and the complement cascade. Objective: Ecallantide (DX-88) is a potent and specific inhibitor of plasma kallikrein. Ecallantide is a recombinantly produced and engineered small protein based on the first Kunitz domain of human tissue factor pathway inhibitor. It was identified through phage display technology. Methods: The search terms 'ecallantide', TX-88' and 'hereditary angioedema' were entered into Pubmed/Medline, ClinicalTrials and Google. Results/conclusion: At present, the drug is being studied for two major indications. First, the results for the treatment of hereditary angioedema are promising. Second, a prospective randomised multi-centre trial for the reduction of blood loss during on-pump cardiothoracic surgery will be terminated in October 2008.