FDA approved Tracleer (bosentan) for Pulmonary Arterial Hypertension in Adults and Pediatric PatientsFDA approved Tracleer for Adults and Children With a Rare Lung Blood Vessel Disease

FDA From the archive Source published September 5, 2017 Summary added October 30, 2026 DOI ↗ Editorial oversight: Dr. Amelia Tan, PhD · Internal Medicine & Chronic Disease

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Key Takeaway

Note: Tracleer requires Bosentan REMS enrollment and monthly liver monitoring due to hepatotoxicity risk.

The U.S. Food and Drug Administration has approved Tracleer (bosentan) for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1). In adults, the indication is to improve exercise ability and to decrease clinical worsening; studies establishing effectiveness included predominantly patients with WHO Functional Class II-IV symptoms and etiologies of idiopathic or heritable PAH (60%), PAH associated with connective tissue diseases (21%), and PAH associated with congenital heart disease with left-to-right shunts (18%). In pediatric patients aged 3 years and older with idiopathic or congenital PAH, the indication is to improve pulmonary vascular resistance (PVR), which is expected to result in an improvement in exercise ability.

Bosentan is an endothelin receptor antagonist. The approval provides a treatment option for both adult and pediatric PAH patients, but it carries a boxed warning for hepatotoxicity and requires prescribers to enroll in the Bosentan REMS and monitor liver aminotransferase levels prior to initiation and monthly thereafter. The label does not include clinical trial data; therefore, trial data are not available in the label.

＋ Clinical Details (Mechanism · Dosing · Trial Data · Warnings)

Mechanism of Action

Bosentan is an endothelin receptor antagonist. The label does not provide further details on the mechanism of action.

Indication & Patient Population

Tracleer is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1): - In adults to improve exercise ability and to decrease clinical worsening. Studies establishing effectiveness included predominantly patients with WHO Functional Class II-IV symptoms and etiologies of idiopathic or heritable PAH (60%), PAH associated with connective tissue diseases (21%), and PAH associated with congenital heart disease with left-to-right shunts (18%). - In pediatric patients aged 3 years and older with idiopathic or congenital PAH to improve pulmonary vascular resistance (PVR), which is expected to result in an improvement in exercise ability.

Dosing & Administration

- Patients older than 12 years of age: initiate at 62.5 mg orally twice daily; for patients weighing greater than 40 kg, increase to 125 mg orally twice daily after 4 weeks. - Patients 12 years of age and younger: dosage is based on weight (see Table 1 in label). - Doses above 125 mg twice daily did not appear to confer additional benefit sufficient to offset the increased risk of hepatotoxicity. - Administration: film-coated tablets and tablets for oral suspension (dispersible tablets) should be administered orally twice daily. Disperse tablets for oral suspension, or dispersible tablet half, in a minimal amount of water immediately before administration. Store divided dispersible tablet pieces at 20 ºC to 25 ºC (68 ºF to 77 ºF) in the opened blister for up to 7 days. - Dosage adjustments for aminotransferase elevations: reduce dose or interrupt treatment for elevations >3 and ≤5 × ULN; stop treatment for elevations >5 and ≤8 × ULN; permanently discontinue for elevations >8 × ULN. Discontinue if elevations are accompanied by clinical symptoms of hepatotoxicity or bilirubin ≥2 × ULN. - Use with ritonavir: in patients on ritonavir for at least 10 days, start Tracleer at the recommended initial dose once daily or every other day based upon individual tolerability. If ritonavir is started in patients on Tracleer, discontinue Tracleer at least 36 hours prior.

Key Clinical Trial Data

Trial data not available in label.

Warnings & Contraindications

- Boxed warning for hepatotoxicity: measure liver aminotransferase levels prior to initiation and monthly thereafter. - Contraindicated in pregnancy: exclude pregnancy before initiating treatment in females of reproductive potential. - Required monitoring: healthcare professionals who prescribe Tracleer must enroll in the Bosentan REMS and comply with required monitoring. - Discontinue if liver aminotransferase elevations are accompanied by clinical symptoms of hepatotoxicity or bilirubin ≥2 × ULN. - There is no experience with reintroduction of Tracleer after permanent discontinuation for aminotransferase elevations >8 × ULN or with clinical symptoms of hepatotoxicity.

Place in Therapy

Tracleer is an endothelin receptor antagonist approved for PAH in adults and pediatric patients aged 3 years and older. Its use requires enrollment in the Bosentan REMS and monthly liver aminotransferase monitoring due to the risk of hepatotoxicity. The label does not provide comparative efficacy data or information on use in combination with other PAH therapies.

Tracleer is a pill called bosentan. It treats pulmonary arterial hypertension, or PAH. In PAH, the blood vessels in the lungs narrow, so the heart has to work harder to push blood through. Tracleer is an endothelin receptor antagonist, which is a drug that blocks a natural substance that tightens those blood vessels.

In adults, the drug is meant to help people exercise more and to lower the chance of their disease getting worse. The studies that showed it works mostly included adults with moderate to severe symptoms. In children aged 3 and older, the goal is to improve blood flow in the lungs, which is expected to help them exercise better.

This approval gives adults and children with PAH another treatment choice. But Tracleer has a serious warning about liver harm. Doctors must enroll in a special safety program, and people taking the drug need blood tests to check their liver before starting and every month after.

The label does not include the details of the clinical trials, so those data are not available there. If you or your child has PAH, talk with your doctor about whether Tracleer fits your situation and about the liver monitoring it requires.

What this means for you:

Tracleer is a new option for adults and children with PAH, but it needs regular liver blood tests.

Study Details

Study typeFda approval

PublishedSep 2017

View Original Abstract ↓

1 INDICATIONS AND USAGE TRACLEER is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1): in adults to improve exercise ability and to decrease clinical worsening. Studies establishing effectiveness included predominantly patients with WHO Functional Class II-IV symptoms and etiologies of idiopathic or heritable PAH (60%), PAH associated with connective tissue diseases (21%), and PAH associated with congenital heart disease with left-to-right shunts (18%) [see Clinical Studies (14.1) ] . in pediatric patients aged 3 years and older with idiopathic or congenital PAH to improve pulmonary vascular resistance (PVR), which is expected to result in an improvement in exercise ability. TRACLEER is an endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1): in adults to improve exercise ability and to decrease clinical worsening. Studies establishing effectiveness included predominantly patients with WHO Functional Class II-IV symptoms and etiologies of idiopathic or heritable PAH (60%), PAH associated with connective tissue diseases (21%), and PAH associated with congenital heart disease with left-to-right shunts (18%) ( 1 ). in pediatric patients aged 3 years and older with idiopathic or congenital PAH to improve pulmonary vascular resistance (PVR), which is expected to result in an improvement in exercise ability ( 1 ).

FDA approved Tracleer (bosentan) for Pulmonary Arterial Hypertension in Adults and Pediatric PatientsFDA approved Tracleer for Adults and Children With a Rare Lung Blood Vessel Disease

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FDA approved Tracleer (bosentan) for Pulmonary Arterial Hypertension in Adults and Pediatric PatientsFDA approved Tracleer for Adults and Children With a Rare Lung Blood Vessel Disease

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