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Macitentan (ACT-064992, ACT064992)，又称马西替坦，是可口服的、非多肽ETA和ETB（内皮素受体）双拮抗剂，IC₅₀为0.5 nM/391 nM，能阻断内皮素诱导的气管和大动脉中的血管收缩，临床上用于治疗肺动脉高压。

参考文献

1.Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18(1):228.

2.Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Oct 15;91(13-14):658-68.

3.Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78.

4.Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist.Transl Oncol. 2012 Feb;5(1):39-47.

冰袋运输。粉末直接保存于-20℃，有效期3年。建议分装后-20℃干燥保存，避免反复冻融。