Endothelin receptor antagonists

What are endothelin receptor antagonists?

Endothelin receptor antagonists (ERAs) are a type of targeted therapy used to treat people with pulmonary hypertension (PH). Targeted therapies slow the progression of PH and may even reverse some of the damage to the heart and lungs.

There are two types of ERA currently used to treat PH:

  • ambrisentan (Volibris)
  • bosentan (Tracleer)

All ERAs are taken as tablets.

How do endothelin receptor antagonists work?

ERAs work by reducing the amount of a substance called endothelinA chemical produced naturally by the body. In normal amounts, it plays an important role in controlling blood flow. In conditions such as PH, too much endothelin is produced, which tightens and narrows blood vessels and affects the blood pressure in the lungs. in the blood.

Endothelin is made in the layer of cells that line the heart and blood vessels.Something that blood passes through, such as a vein or artery. It causes the blood vessels to constrict (become narrower). In people with PH the body produces too much endothelin. This causes the blood vessels in the lungs to become narrow, increasing the blood pressure in the pulmonary arteries.The blood vessel delivering blood to the lungs from the right side of the heart.

ERAs reduce the amount of endothelin in the blood, therefore limiting the harm an excess of endothelin can cause.

Precautions when taking endothelin receptor antagonists

Liver function tests

If you are taking ambrisentan or bosentan, you will need regular blood tests to make sure your liver is not being harmed. These blood tests can show if your liver will become damaged if you carry on taking the drug.

Your PH specialist team will discuss the risks associated with taking ERAs with you. If you are female, this may include the risks of taking ERAs in pregnancy.

 

Last updated on 9th June 2010
A full list of references used can be obtained by contacting the PHA UK Office