Macitentan

CAS 441798-33-0

About the API

Systematic name N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide
Trade name(s) Opsumit
Technology Synthetic Organic Chemistry
Molecular Formula C19H20Br2N6O4S
Molecular Weight 588.273 g/mol
Therapeutic category Cardiovascular
Available formulations Oral Solid
Regulations US DMF Flag US DMF

General Information

Macitentan belongs to a class of drugs called endothelin receptor antagonists, which act to relax the arteries connecting the heart to the lungs. It is used to block the progression of pulmonary arterial hypertension (PAH), a chronic, debilitating lung disease. In PAH, high blood pressure in the lungs may cause shortness of breath and physical limitations, and can lead to death or the need for lung transplantation. In a two-year study, treatment with macitentan was shown to significantly reduce the chances for “worsening events” such as death due to respiratory failure, the need for lung transplantation, and other symptoms indicating the significant progression of the disease.

 

Developed by Actelion Pharmaceuticals, macitentan was approved by the FDA in 2013 after receiving orphan drug status in 2009. It is produced through multi-step chemical synthesis.