Medicines
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Discover all available medicines and treatments
Brand: Opsumit
Macitentan is a dual endothelin receptor antagonist indicated for the long-term treatment of pulmonary arterial hypertension (PAH) in adults. It belongs to the class of endothelin receptor antagonists and works by blocking the effects of endothelin, a peptide that causes blood vessel constriction and promotes vascular remodeling. By inhibiting endothelin, macitentan helps to relax the pulmonary arteries, reduce pulmonary vascular resistance, and improve exercise capacity in patients with PAH.
For the long-term treatment of pulmonary arterial hypertension (PAH) in adults.
Macitentan is contraindicated in pregnancy due to its potential to cause embryo-fetal toxicity. Females of reproductive potential must have a negative pregnancy test before starting treatment and monthly thereafter. Effective contraception is required during treatment and for one month after discontinuation.
Outcome:
Decreased macitentan levels
Mechanism:
Increased metabolism
Outcome:
Decreased macitentan levels
Mechanism:
Increased metabolism
Outcome:
May slightly increase macitentan levels
Mechanism:
CYP3A4 inhibition
Most likely new formulation: extended-release formulation (Year 2026, 70% confidence)
Based on current usage trends and clinical trial data, there is a 90% likelihood that macitentan will maintain its current regulatory status for PAH treatment over the next 5 years.
Endothelin Receptor Antagonist
Pyrimidinone