Bosentan (Tracleer®)

Tracleer was the first oral medication approved for treatment of PAH. It is a dual endothelin receptor antagonist, meaning that it blocks both endothelin receptors.

Fda approval date
November 20, 2001

Recommended for
PAH patients in WHO (World Health Organization) class II - IV.

How administered
Tracleer is an oral medication taken in a tablet form.  It is available in different strengths and is usually taken twice a day.

Risks/Side Effects
There are important issues that every patient must know:
  • Tracleer may cause liver damage; therefore monitoring liver enzyme levels is necessary. This is done by a blood test every month.
  • Tracleer may cause birth defects; therefore, it is essential that patients on Tracleer are not pregnant and don't become pregnant. Monthly pregnancy tests must be obtained.
  • Oral, injected and implanted contraceptives may not be reliably effective because Tracleer may alter their metabolism in a way that reduces the effectiveness of hormonal contraceptives, so these methods must be supplemented by other methods or barrier methods must be used. Therefore, it is important for patients to consult with a gynecologist or other physician knowledgeable about contraceptives.

Headache, sore throat, and flushing are reported by some users.

Tracleer has been shown to improve exercise ability and decrease the rate of clinical worsening in PAH patients with WHO Class II - IV symptoms. As with any medication, patients who take Tracleer as directed by their physician achieve the optimal benefit.

Tracler has been shown to offer these important benefits to people with PAH:
  • Tracleer can improve symptoms and the ability to perform normal daily activities.
  • Tracleer can improve the worsening of symptoms.
  • Tracleer can lower high blood pressure in the lungs.
  • Tracleer can enable the heart to pump blood more effectively

The involvement of ET-1 as a modulator of increased pulmonary vascular resistance in PAH patients has led to the development of endothelin receptor antagonists as potential therapeutic agents. Bosentan is an orally active, nonpeptide, competitive antagonist of both ET-A and ET-B (endothelin type A and B) receptors, with a slightly higher affinity for the ET-A receptor.

Bosentan costs approximately $30,000 per year.  Because Tracleer is classified as a drug, instead of a treatment, it is covered differently by insurance companies and Medicare.  Co-pay rates have varied widely.   At this time, arrangements with individual insurance companies vary.

Manufactured by
Patheon Inc

Distributed by
Actelion Pharmaceuticals

Additional info
Tracleer is prescribed and dispensed by a specialty pharmacy distributor and is available only through the Tracleer Access Program (TAP), a direct distribution program. Your doctor can give you more information on how Tracleer is distributed.

Visit the FDA Page for this drug/therapy

Visit the Official Drug Company Website

Info Source(s)
Full Prescribing Information

Page Reviewed/Edited: October 2010

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