新型肺动脉高压治疗药物马西替坦

Macitentan,a novel antagonist of endothlin against pulmonary arterial hypertension

肺动脉高压是严重威胁人类健康的心血管疾病,药物是其主要治疗手段。Actelion公司开发的用于肺动脉高压的新型药物马西替坦(macitentan)是内皮素受体A(ET A)和内皮素受体B(ET B)的双重拮抗剂。临床前研究和临床试验结果表明马西替坦能有效延缓肺动脉高压患者的的疾病进展,延长患者的生存期,改善患者的生活质量,且肝肾毒性低,药物相互作用少。文中对其药理作用、药动学、临床评价及安全性做一综述。

Pulmonary hypertension （PAH） is a serious cardiovascular disease which can threat human health, and drug therapy is its main treatment measure. Macitentan （Opsumit） is a new dual endothelin ETA/ETB receptor antagonist developed by Actelion for pulmonary hypertension treatment. Preclinical studies and clinical tri- als showed that macitentan could effectively delay disease progression, prolong survival, and improve the quality of life, with lower liver and kidney toxicity and fewer drug interactions. The pharmacology, pharmacokinetics, clinical evaluation, and safety of macitentan were reviewed in this paper.