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macitentan : ウィキペディア英語版
macitentan

Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH).〔Hong, I.S., Coe, H.V., & Catanzaro, L.M. (2014). Macitentan for the treatment of pulmonary arterial hypertension. ''The Annals of Pharmacotherapy, 48'', 1-10.〕 The other two ERAs marketed as of 2014 are bosentan and ambrisentan.〔 Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB.〔 However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.〔Iglarz, M., Qiu, C., Fischli, W., Morrison, K., Binkert, C., Clozel, M., Hess, P., Capeleto, B., Buchmann, S., Boss, C., Bolli, M.H., Weller, T., Treiber, A., & Gatfield, J. (2008). Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. ''Journal of Pharmacology and Experimental Therapeutics, 327''(3), 736-745.〕 The drug received approval from the U.S. Food and Drug Administration (FDA) on October 13, 2013.〔(Actelion receives us fda approval of Opsumit (macitentan) for the treatment of pulmonary arterial hypertension ). Actelion. Retrieved 22 October 2013.〕
==Mechanism of action==


抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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