近日，美国FDA在加速批准程序下批准 Praxbind（idarucizumab）在服用抗凝药物达比加群酯患者遇到紧急情况而需要逆转达比加群酯血液稀释作用时使用。
FDA药品评价和研究中心血液学和肿瘤产品室主任Richard Pazdur，M.D.说：“Pradaxa的抗凝剂作用对有些患者是重要和挽救生命，但其中也有情况逆转药物作用是医疗上必要的，” “今天的批准为医学社会提供一个重要工具为在紧急或危及生命情况当出血不能控制时处理用Pradaxa。” 加快批准程序
批准日期：2015年10月16日；公司：Boehringer Ingelheim Pharmaceuticals，Inc.
PRAXBIND（达比加群酯[idarucizumab]）注射液，用于静脉注射
美国最初批准：2015年
最近的重大变化
剂量和用法，准备：4/2018
作用机制
Idarucizumab是一个对达比加群特异性逆转剂。它是一个人源化单克隆抗体片段(Fab)与达比加群及其酰基葡萄糖醛酸苷代谢物结合亲和力比达比加群与凝血酶的结合亲和力有更高，中和它们的抗凝剂效应。
适应症和用法
PRAXBIND是一种人源化单克隆抗体片段（Fab），适用于需要逆转达比加群的抗凝血作用的Pradaxa®患者：紧急手术/紧急手术用于危及生命或不受控制的出血
剂量和给药
仅限静脉注射。
PRAXBIND的推荐剂量为5g，作为两个单独的小瓶提供，每个小瓶含有2.5g/50mL idarucizumab。
有限的数据支持额外的5克PRAXBIND的管理。
剂量形式和强度
注射：在单剂量小瓶中的2.5g/50mL溶液
禁忌症
没有
警告和注意事项
血栓栓塞风险：逆转达比加群治疗会使患者暴露于其潜在疾病的血栓形成风险。在医学上适当时立即恢复抗凝治疗。
凝血参数重新升高：对于凝血参数升高和临床相关出血者再次出现需要第二次急诊手术/紧急手术的患者，可考虑额外的5g剂量的PRAXBIND。
过敏反应：停止给药和评估。
山梨醇辅料对遗传性果糖耐受患者严重不良反应的风险：遗传性果糖耐受不良的患者可能有不良反应的风险。
不良反应
在健康志愿者中，≥5％接受idarucizumab治疗的受试者中最常报告的不良反应是头痛。
对于患者，在使用idarucizumab治疗的患者中，最常报告的不良反应≥5％是便秘和恶心。
包装提供/存储和处理
提供
PRAXBIND是一种无菌，无防腐剂，无色至微黄色，透明至微乳白色的溶液，以2个单剂量小瓶供应，每个小瓶含有
2.5克/ 50毫升的艾达鲁单抗。
NDC号0597-0197-05：装有两个2.5克/50毫升小瓶的纸箱。
存储和处理
将PRAXBIND样品瓶放入原装纸箱中2ºC至8ºC（36ºF至46ºF）的冰箱中，以防光照。 不要冻结。 别摇了。
PRAXBIND样品瓶可以在25°C（77°F）的室温下储存，在原装纸箱中保存48小时，以防光照。
PRAXBIND小瓶可以在25°C（77°F）的室温下储存，从纸箱中取出并暴露在光线下但必须在6小时内使用[见剂量和
管理]。
完整说明资料附件：
https://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Praxbind/Praxbind.pdf
PRAXBIND(idarucizumab) injection, for intravenous use
Initial U.S. Approval: 2015
IMPORTANT SAFETY INFORMATION AND INDICATION FOR PRAXBIND
WARNINGS AND PRECAUTIONS
Thromboembolic Risk
Dabigatran-treated patients have underlying diseases predisposing them to thromboembolic events. Reversing dabigatran therapy exposes patients to the thrombotic risk of their underlying disease. To reduce this risk, resumption of anticoagulant therapy should be considered as soon as medically appropriate.
Re-elevation of Coagulation Parameters
Elevated coagulation parameters (e.g., activated partial thromboplastin time or ecarin clotting time) have been observed in a limited number of PRAXBIND-treated patients. If reappearance of clinically relevant bleeding together with elevated coagulation parameters is observed or if patients requiring a second emergency surgery/urgent procedure have elevated coagulation parameters, an additional full dose may be considered.
Hypersensitivity Reactions
There is insufficient clinical experience eva luating risk of hypersensitivity to idarucizumab, but a possible relationship could not be excluded. Risk of hypersensitivity (e.g., anaphylactoid reaction) to idarucizumab or excipients needs to be weighed cautiously against the potential benefit. If serious allergic reaction occurs, immediately discontinue PRAXBIND and institute appropriate treatment.
Risk in Patients with Hereditary Fructose Intolerance
PRAXBIND contains 4 g sorbitol as an excipient. When prescribing PRAXBIND in patients with hereditary fructose intolerance consider the total daily amount of sorbitol/fructose consumption from all sources as serious adverse reactions (e.g. hypoglycemia, hypophosphatemia, metabolic acidosis, increase in uric acid, acute liver failure and death) may occur.
ADVERSE REACTIONS
The most frequently reported adverse reaction in ≥5% of idarucizumab-treated healthy volunteers was headache (12/224). The most frequently reported adverse reactions in ≥5% of patients were hypokalemia (9/123), delirium (9/123), constipation (8/123), pyrexia (7/123) and pneumonia (7/123).
As with all proteins there is a potential for immunogenicity with idarucizumab. In treated patients, treatment-emergent antibodies with low titers were observed (9/224).
USE IN SPECIFIC POPULATIONS
Pregnancy and Nursing Mothers
PRAXBIND should be given to a pregnant or nursing woman only if clearly needed.
INDICATIONS AND USAGE
PRAXBIND is indicated in patients treated with Pradaxa® when reversal of the anticoagulant effects of dabigatran is needed:
For emergency surgery/urgent procedures
In life-threatening or uncontrolled bleeding
This indication is approved under accelerated approval based on a reduction in unbound dabigatran and normalization of coagulation parameters in healthy volunteers. Continued approval for this indication may be contingent upon the results of an ongoing cohort case series study.