Kholdani Cyrus A, Fares Wassim H, Trow Terence K
Section of Pulmonary, Critical Care and Sleep Medicine, Yale University School of Medicine, New Haven, CT, USA.
Yale Pulmonary Vascular Disease Program, Section of Pulmonary, Critical Care and Sleep Medicine, Department of Internal Medicine, Yale University School of Medicine, New Haven, CT, USA.
Vasc Health Risk Manag. 2014 Nov 25;10:665-73. doi: 10.2147/VHRM.S33904. eCollection 2014.
Macitentan is the most recently approved dual endothelin-receptor antagonist (ERA) for the treatment of symptomatic pulmonary arterial hypertension. Compared to other available ERAs, it demonstrates superior receptor-binding properties, with consequently improved tissue penetration, and a longer duration of action allowing for once-daily dosing. It has a favorable adverse-effect profile, with notably no demonstrable increase in the risk of hepatotoxicity or peripheral edema, but like other ERAs, it is potentially limited by significant anemia. Phase I data have demonstrated a favorable drug-drug interaction profile and no need for dose adjustment with hepatic and renal impairment. In the pivotal SERAPHIN study, treatment of symptomatic pulmonary arterial hypertension patients with macitentan led to statistically significant improvements in functional class, exercise tolerance, and hemodynamic parameters, in addition to a reduction in morbidity in an event-driven long-term trial.
马昔腾坦是最近获批用于治疗症状性肺动脉高压的双重内皮素受体拮抗剂（ERA）。与其他可用的ERA相比，它具有卓越的受体结合特性，从而改善了组织渗透，并具有更长的作用持续时间，允许每日一次给药。它具有良好的不良反应谱，尤其在肝毒性或外周水肿风险方面无明显增加，但与其他ERA一样，它可能受到严重贫血的限制。I期数据显示其具有良好的药物相互作用谱，并且在肝肾功能损害时无需调整剂量。在关键的SERAPHIN研究中，在一项事件驱动的长期试验中，用马昔腾坦治疗症状性肺动脉高压患者除了降低发病率外，还在功能分级、运动耐量和血流动力学参数方面带来了具有统计学意义的改善。
