Phillips Bradley, Vascimini Angelina, Whitner Chardae, St Onge Erin, Huston Jessica
Department of Pharmacy Education and Practice, College of Pharmacy, University of Florida, Orlando, FL, USA.
Department of Pharmacy Education and Practice, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Ann Pharmacother. 2025 Apr;59(4):364-370. doi: 10.1177/10600280241273218. Epub 2024 Sep 4.
This article reviews the published data including the pharmacology, efficacy, and safety of aprocitentan, a novel endothelin receptor antagonist developed to treat hypertension in conjunction with additional agents.
A literature search was conducted from drug discovery until May 2024 through PubMed, MEDLINE, and National Institutes of Health Clinical Trials Registry utilizing the following search terms: Tryvio, aprocitentan, hypertension, resistant hypertension, endothelin receptor antagonist, and ACT-132577.
All relevant English-language studies, or studies that could be appropriately translated into English, containing the pharmacology, pharmacokinetics, safety, and efficacy of aprocitentan, were selected for review.
In the setting of resistant hypertension, aprocitentan has shown significant reductions in blood pressure in both medical office and 24-hour ambulatory settings at 4 weeks with a sustained effect at 40 weeks. Studies evaluating cardiovascular risk reduction have not been conducted at this time. Fluid retention and edema were the most frequent adverse events reported in clinical studies with aprocitentan. As a class, endothelin receptor antagonists may cause fetal harm; aprocitentan should be used with caution to avoid embryo-fetal toxicity.
Owing to the existent barriers for the treatment of resistant hypertension, aprocitentan presents itself as an effective option when added to traditional antihypertensives. This single-strength, once-daily regimen may serve as an appealing option to both patients and prescribers.
Aprocitentan is a safe and effective medication for the treatment of hypertension when added to other pharmacological therapies.
本文回顾已发表的数据，包括阿曲生坦（一种开发用于联合其他药物治疗高血压的新型内皮素受体拮抗剂）的药理学、疗效和安全性。
从药物研发至2024年5月，通过PubMed、MEDLINE和美国国立卫生研究院临床试验注册库进行文献检索，使用以下检索词：Tryvio、阿曲生坦、高血压、顽固性高血压、内皮素受体拮抗剂和ACT-132577。
选择所有包含阿曲生坦药理学、药代动力学、安全性和疗效的相关英文研究，或可适当翻译成英文的研究进行综述。
在顽固性高血压的背景下，阿曲生坦在4周时在诊室和24小时动态血压监测中均显示血压显著降低，且在40周时仍有持续效果。目前尚未进行评估心血管风险降低的研究。液体潴留和水肿是阿曲生坦临床研究中报告最频繁的不良事件。作为一类药物，内皮素受体拮抗剂可能会对胎儿造成伤害；使用阿曲生坦时应谨慎，以避免胚胎-胎儿毒性。
由于顽固性高血压治疗存在现有障碍，阿曲生坦在与传统抗高血压药物联用时是一种有效的选择。这种单强度、每日一次的给药方案可能对患者和处方医生都具有吸引力。
阿曲生坦在添加到其他药物治疗时是一种安全有效的高血压治疗药物。
