Abuan Irene, Wong Kristine H, Bolinske Benjamin, Hale Katherine S
Kadlec Regional Medical Center, Richland, WA, USA.
J Pharm Technol. 2019 Jun;35(3):119-125. doi: 10.1177/8755122519839437. Epub 2019 Mar 28.
To review the pharmacology, safety, and efficacy of andexanet alfa (andexanet), a recombinant modified human factor Xa protein for reversal of factor Xa inhibitors. English-language articles were obtained from MEDLINE (1966 to February 2019) using the following key words: andexanet, andexanet alfa, AndexXa, factor Xa, antidote, and reversal. Citations from selected articles were used to identify additional sources. Available published articles reporting results of human studies of andexanet alfa were reviewed for inclusion. Prescribing information was used to obtain additional information regarding pharmacology, adverse events, contraindications, and precautions. Andexanet is a recombinant modified human factor Xa protein indicated for reversal of rivaroxaban and apixaban in patients with life-threatening or uncontrolled bleeding. Onset of action is rapid and sustained throughout bolus and infusion administration. Medication effects subside 1 to 3 hours postadministration. Andexanet is administered as a bolus followed by a 120-minute continuous infusion. Anti-factor Xa activity was reduced by 95% and 92% in apixaban and rivaroxaban groups, respectively, on infusion completion. Thrombin regeneration occurred within 2 to 5 minutes in up to 96% of patients. Minor infusion reactions and gastrointestinal upset were reported most. A black box warning for thrombotic events, cardiac arrest, ischemia, and sudden death should be noted. Andexanet is effective in reversing rivaroxaban and apixaban anticoagulation due to reduction of anti-factor Xa activity in healthy patients and those with acute major bleeds. Safety concerns, including thrombotic risks, exist and should be assessed against individual patient factors.
为了评估andexanet alfa（andexanet）——一种用于逆转Xa因子抑制剂作用的重组修饰人Xa因子蛋白——的药理学、安全性和有效性。使用以下关键词从MEDLINE（1966年至2019年2月）获取英文文章：andexanet、andexanet alfa、AndexXa、Xa因子、解毒剂和逆转。利用所选文章的参考文献来识别其他来源。对已发表的报告andexanet alfa人体研究结果的文章进行综述以确定是否纳入。使用处方信息获取有关药理学、不良事件、禁忌证和注意事项的更多信息。Andexanet是一种重组修饰人Xa因子蛋白，用于有危及生命或难以控制的出血的患者中逆转利伐沙班和阿哌沙班的作用。起效迅速，在推注和输注给药全过程中作用持续。给药后1至3小时药物作用消退。Andexanet以推注给药，随后进行120分钟的持续输注。输注结束时，阿哌沙班组和利伐沙班组的抗Xa因子活性分别降低了95%和92%。高达96% 的患者在2至5分钟内发生凝血酶再生。报告最多的是轻微的输注反应和胃肠道不适。应注意关于血栓形成事件、心脏骤停、缺血和猝死的黑框警告。由于可降低健康患者和急性大出血患者的抗Xa因子活性，Andexanet在逆转利伐沙班和阿哌沙班抗凝方面有效。存在包括血栓形成风险在内的安全问题，应根据个体患者因素进行评估。
