內(nèi)皮素受體拮抗劑與內(nèi)皮素受體結(jié)合后，可以抑制由內(nèi)皮素引起的血管收縮，同時(shí)還可減輕由內(nèi)皮素活化造成的血管平滑肌的增殖和纖維化，從而達(dá)到治療與內(nèi)皮素相關(guān)疾病的目的。馬西替坦是由瑞士Actelion公司研發(fā)的新型內(nèi)皮素受體拮抗劑，具有組織靶向性，對ETA受體、ETB受體具有雙重抑制作用，可用于治療肺動(dòng)脈高壓、肺纖維化等疾病，在一系列臨床研究中顯示出良好的治療前景，且安全性及耐受性均較好。

Endothelin receptor antagonists combined with endothelin receptor could inhibit vasoconstriction induced by endothelin, and also could reduce the proliferation and fibrosis which are caused by the activition of endothelin. Macitentan is a new endothelin receptor antagonist developed by Switzerland Actelion Company, which has the organization target with dual inhibitory effects on ETA and ETB receptor. Macitentan could be used for the treatment of pulmonary arterial hypertension, pulmonary fibrosis, and other diseases, and it shows a good prospect in a series of clinical studies with good safety and tolerability.