Macitentan
Chemical compound / From Wikipedia, the free encyclopedia
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Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist (ERA) developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH).[4] The other two ERAs marketed as of 2014 are bosentan and ambrisentan.[4] Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB.[4] However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.[5] The drug received approval from the U.S. Food and Drug Administration (FDA) on 13 October 2013.[6]
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Trade names | Opsumit |
Other names | ACT-064992 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a615033 |
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Routes of administration | By mouth |
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Metabolism | Hydrolysis, oxidation (CYP3A4) |
Excretion | 2/3 urine, 1/3 faeces |
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Formula | C19H20Br2N6O4S |
Molar mass | 588.28 g·mol−1 |
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Macitentan is available as a generic medication in the United States as of April 2021.[7]