Macitentan

Pulmonary Arterial Hypertension

Treatment

2 FDA approvals

0 Active Studies for Macitentan

What is Macitentan

Macitentan

The Generic name of this drug

Treatment Summary

Macitentan is a medication used to treat pulmonary arterial hypertension (high blood pressure in the lungs). It was approved by the FDA in 2013 and is considered safer than its predecessor due to its lower risk of causing liver damage.

Opsumit

is the brand name

image of different drug pills on a surface

Macitentan Overview & Background

Brand Name

Generic Name

First FDA Approval

How many FDA approvals?

Opsumit

Macitentan

2013

1

Approved as Treatment by the FDA

Macitentan, otherwise called Opsumit, is approved by the FDA for 2 uses such as Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH) and Pulmonary Arterial Hypertension .

Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)

Helps manage Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)

Pulmonary Arterial Hypertension

Helps manage Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)

Effectiveness

How Macitentan Affects Patients

Macitentan works by reducing how much blood vessels constrict and how much cells multiply when there is too much endothelin in the body.

How Macitentan works in the body

Macitentan helps treat pulmonary arterial hypertension (PAH) by blocking signals coming from endothelin-1 and -2, which are molecules released by the vascular endothelium. It does this by binding to two receptors in the body, E<sub>A</sub> and E<sub>B</sub>. When endothelin molecules bind to the E<sub>A</sub> receptor, it causes the cells to release calcium, which makes the cells contract and narrow the blood vessels. This leads to PAH. When endothelin binds to the E<sub>B</sub> receptor, it

When to interrupt dosage

The amount of Macitentan is contingent upon the identified affliction. The measure of dosage differs as per the technique of delivery (e.g. Tablet or Tablet, film coated - Oral), as indicated in the table beneath.

Condition

Dosage

Administration

Pulmonary Arterial Hypertension

, 10.0 mg

, Oral, Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet

Warnings

Macitentan Contraindications

Condition

Risk Level

Notes

Severe Hypersensitivity Reactions

Do Not Combine

Macitentan may interact with Pulse Frequency

There are 20 known major drug interactions with Macitentan.

Common Macitentan Drug Interactions

Drug Name

Risk Level

Description

Amifostine

Major

Macitentan may increase the hypotensive activities of Amifostine.

Acrivastine

Minor

Macitentan may decrease the excretion rate of Acrivastine which could result in a higher serum level.

Albutrepenonacog alfa

Minor

Macitentan may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.

Aliskiren

Minor

Macitentan may increase the hypotensive activities of Aliskiren.

Almasilate

Minor

Macitentan may decrease the excretion rate of Almasilate which could result in a higher serum level.

Macitentan Toxicity & Overdose Risk

Taking too much macitentan may lead to headaches, nausea, and vomiting. If this happens, supportive care is recommended. Macitentan binds to proteins in the blood, so it cannot be removed from the body through dialysis.

image of a doctor in a lab doing drug, clinical research

Macitentan Novel Uses: Which Conditions Have a Clinical Trial Featuring Macitentan?

53 active investigations are currently underway to assess the potential of Macitentan to mitigate Pulmonary Arterial Hypertension.

Condition

Clinical Trials

Trial Phases

Pulmonary Arterial Hypertension

0 Actively Recruiting

Macitentan Reviews: What are patients saying about Macitentan?

2

Patient Review

1/14/2015

Macitentan for Pulmonary Arterial Hypertension

I got worse when I switched from bosentan to macitentan; however, switching back has helped me feel much better.
image of drug pills surrounding a glass of water symbolizing drug consumption

Patient Q&A Section about macitentan

These questions and answers are submitted by anonymous patients, and have not been verified by our internal team.

What is macitentan tablets used for?

"Macitentan is used to manage PAH, which is high blood pressure in the vessels that carry blood to the lungs."

Answered by AI

Is macitentan a controlled substance?

"The product is a Schedule II controlled substance and is subject to FDA Medication Guide requirements. It has a risk evaluation and mitigation strategy to help make sure it is used safely."

Answered by AI

How is macitentan administered?

"Macitentan can be taken orally, with or without food. The recommended dose is 10 mg once daily. The tablets should not be split, crushed, or chewed."

Answered by AI