Opsumit Uses, Dosage, Side Effects, Food Interaction and all others data.

Opsumit was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Opsumit is an antagonist/blocker of endothelin receptors on blood vessels and smooth muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction. Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age.

Opsumit blocks simulators of hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction.

Trade Name Opsumit
Availability Prescription only
Generic Macitentan
Macitentan Other Names Macitentán, Macitentan, Macitentanum
Related Drugs sildenafil, tadalafil, Revatio, Adempas, Opsumit, ambrisentan
Weight 10mg,
Type Tablet, Oral Tablet
Formula C19H20Br2N6O4S
Weight Average: 588.273
Monoisotopic: 585.963349142
Protein binding

Macitentan is >99% bound to plasma proteins, which are mainly albumin

Groups Approved
Therapeutic Class
Manufacturer Janssen-Cilag Ltd
Available Country Australia, Canada, United Kingdom, United States,
Last Updated: September 19, 2023 at 7:00 am


Opsumit is an endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.

Opsumit is indicated for patients with pulmonary arterial hypertension.

Opsumit is also used to associated treatment for these conditions: Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)

How Opsumit works

Opsumit is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Opsumit binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating the ETA and ETB receptors.


Opsumit has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.

Food Interaction

  • Take with or without food.

Volume of Distribution

Opsumit has a volume of distribution of 50L.

Elimination Route

Opsumit is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.

Half Life

The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours.


Clearance data was not found.

Elimination Route

Eliminated 50% through urine and 24% through feces.

Innovators Monograph

You find simplified version here Opsumit

*** Taking medicines without doctor's advice can cause long-term problems.