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马昔腾坦治疗肺动脉高压。

Macitentan for the treatment of pulmonary arterial hypertension.

机构信息

Massachusetts General Hospital, Division of Pulmonary and Critical Care, 55 Fruit St Boston, MA 02114, USA.

出版信息

Expert Rev Respir Med. 2014 Aug;8(4):393-9. doi: 10.1586/17476348.2014.937708. Epub 2014 Jul 6.

Abstract

Macitentan is a novel dual endothelin receptor antagonist recently approved for the treatment of symptomatic pulmonary arterial hypertension (PAH). Compared to other endothelin receptor antagonists, in vitro and in vivo studies have demonstrated that macitentan has improved tissue targeting, a longer duration of action and an improved safety profile. Macitentan is available as a once daily oral medication and has been well tolerated in clinical trials. The recently published Study with an Endothelin Receptor Antagonist in PAH to Improve cliNical Outcomes (SERAPHIN), which was the first event-driven trial ever done in PAH, also demonstrated the benefit of macitentan on reducing the likelihood of a composite endpoint of morbidity and mortality events without a significant difference in mortality.

摘要

马西替坦是一种新型的双重内皮素受体拮抗剂,最近被批准用于治疗有症状的肺动脉高压(PAH)。与其他内皮素受体拮抗剂相比,体外和体内研究表明,马西替坦具有改善的组织靶向性、更长的作用持续时间和改善的安全性。马西替坦是一种每日一次的口服药物,在临床试验中耐受性良好。最近发表的肺动脉高压中使用内皮素受体拮抗剂改善临床结局的研究(SERAPHIN),这是 PAH 中首次进行的事件驱动试验,也表明马西替坦在降低发病率和死亡率复合终点的可能性方面具有益处,而死亡率没有显著差异。

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