Macitentan is used to treat high blood pressure in the lungs (pulmonary arterial hypertension). This condition may be caused by high levels of a specific natural substance called endothelin. The treatment blocks the effects of endothelin-1, which helps lessen blood pressure in the lungs, thus slowing down the worsening of symptoms that are caused by the disease, and improving exercise tolerance.
This drug has slower receptor separation than the other drugs that are used to treat this condition. Slow separation leads to the improved pharmacological action of macitentan in pulmonary hypertension than the drugs bosentan and ambrisentan.
The most common side effects are anemia, nasopharyngitis/pharyngitis, bronchitis, migraine, flu, and urinary tract infection. Other uncommon side effects are hepatotoxicity and liver failure, diminished spermatogenesis, and edema.
Changes in liver and kidney tests that are caused by macitentan are not considered clinically significant and do not lead to debilitation in patients. Macitentan is contraindicated in pregnancy. Reproductive-age females are advised to use contraception and have a negative pregnancy test before starting treatment and they should have monthly pregnancy tests from that point on.
The said drug is an orally active, novel, highly potent, and tissue-targeting medication. It shows antihypertensive and anticancer actions. It is used in the long-term treatment of pulmonary arterial hypertension because of its safety profile and is considered to have fewer side effects than the recent treatment choices for the condition.