School of Pharmacy, West Virginia University, Morgantown, WV 26506, USA.
Am J Health Syst Pharm. 2012 Apr 15;69(8):651-7. doi: 10.2146/ajhp110227.
The pharmacology, pharmacokinetics, efficacy, safety, dosage, administration, adverse effects, and place in therapy of ecallantide, a kallikrein inhibitor for the treatment of hereditary angioedema (HAE), are reviewed.
Ecallantide is the first member of the kallikrein inhibitor class approved for the treatment of acute attacks of HAE. Ecallantide works by binding to kallikrein, preventing the conversion of kininogen to bradykinin, which reduces vascular permeability, thus reducing the swelling associated with acute attacks of HAE. Ecallantide has been studied for the treatment of HAE in three Phase II studies and two Phase III studies. These studies were collectively known as the EDEMA (Evaluation of DX-88's Effect in Mitigating Angioedema) studies. Phase III clinical trials found that ecallantide is superior to placebo in ameliorating patient symptoms associated with acute attacks of HAE at any anatomical site. Ecallantide has a favorable safety profile, with the most common adverse effects being gastrointestinal effects, headache, and injection site reactions. The most severe adverse effects of ecallantide are the risk of anaphylaxis and the possible development of antiecallantide antibodies. A risk evaluation and mitigation strategy program has been approved by the Food and Drug Administration to help ensure the safety and efficacy of ecallantide use. The recommended dose is 30 mg given as three separate subcutaneous injections.
Ecallantide is a novel agent approved for the treatment of acute attacks of HAE at any anatomical site. It is one of only three medications approved for this indication in the United States, presents a unique mechanism of action, and appears to be safe and effective when used for its labeled indication.
综述 kallikrein 抑制剂 ecallantide 的药理学、药代动力学、疗效、安全性、剂量、给药途径、不良反应以及在遗传性血管性水肿（HAE）治疗中的地位。
ecallantide 是首个获批用于治疗 HAE 急性发作的 kallikrein 抑制剂。ecallantide 通过与 kallikrein 结合，阻止激肽原转化为缓激肽，从而降低血管通透性，减少与 HAE 急性发作相关的肿胀。ecallantide 已在三项 II 期研究和两项 III 期研究中用于 HAE 的治疗。这些研究统称为 EDEMA（评价 DX-88 减轻血管水肿的效果）研究。III 期临床试验发现，ecallantide 在改善 HAE 任何解剖部位急性发作相关症状方面优于安慰剂。ecallantide 具有良好的安全性，最常见的不良反应是胃肠道效应、头痛和注射部位反应。ecallantide 最严重的不良反应是过敏反应的风险和可能产生抗 ecallantide 抗体。美国食品和药物管理局批准了一项风险评估和缓解策略计划，以帮助确保 ecallantide 使用的安全性和疗效。推荐剂量为 30mg，分三次皮下注射。
ecallantide 是一种新型药物，获批用于治疗 HAE 任何解剖部位的急性发作。它是美国仅有的三种获批用于该适应证的药物之一，具有独特的作用机制，在用于其标注适应证时似乎安全有效。
