Tracleer (bosentan)
An approved treatment for Pulmonary Arterial Hypertension.
The same compound appears under different names depending on the context. Here is how to identify Bosentan wherever you encounter it, plus the key facts at a glance.
- Generic name
- Bosentan
- Brand name
- Tracleer
- Development code
- Ro 47-0203
- Drug class
- Endothelin receptor antagonist
- Manufacturer
- Actelion, a Johnson & Johnson company
- How it's taken
- Taken as an oral tablet twice daily.
The first oral endothelin receptor antagonist approved for PAH. Tracleer was a breakthrough as one of the earliest targeted oral therapies, reducing pulmonary artery pressure and improving exercise capacity.
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Where Bosentan fits
First oral endothelin receptor antagonist for PAH. Now available as a cost-effective generic, though newer agents like macitentan may offer improved efficacy.
How Bosentan works
Endothelin-1 is a powerful vasoconstrictor that is overproduced in PAH, causing blood vessels in the lungs to narrow and stiffen. Bosentan blocks both ET-A and ET-B receptors, preventing endothelin-1 from constricting these vessels. This lowers pulmonary artery pressure and reduces the strain on the right side of the heart.
Mechanism: Dual endothelin receptor antagonist (ERA) that blocks ET-A and ET-B receptors to relax and widen pulmonary blood vessels
Side effects and safety
Carries a boxed warning for liver damage and for birth defects. Liver blood tests are required before starting and every month during treatment. Pregnancy must be ruled out before starting, and effective birth control is needed during treatment and for 1 month after stopping. Common side effects include respiratory infections, headache, swelling (edema), flushing, low blood pressure, and anemia. The label also warns about fluid buildup that has sometimes needed a hospital stay for heart failure, drops in red blood cells (hemoglobin should be checked after 1 and 3 months and then every 3 months), lower sperm counts, and fluid in the lungs in people with a rare lung blood vessel disease called pulmonary veno-occlusive disease. Bosentan must not be taken with cyclosporine A or glyburide. Available only through a restricted program (the Bosentan REMS) because of the liver risk.
This is not a complete list of side effects. Talk to your doctor or pharmacist about what to expect and when to seek medical attention.
Taking Bosentan
Taken as an oral tablet twice daily. For patients older than 12, the starting dose is 62.5 mg twice daily for 4 weeks, then 125 mg twice daily for those weighing more than 40 kg. It is approved for adults with PAH and for children 3 years and older with idiopathic or congenital PAH. Children 12 and younger are dosed by weight, and a tablet for oral suspension is available for children. Monthly liver function monitoring is mandatory. Generic versions are now available.
Availability and cost
Generic versions may be available at a lower cost. Ask your pharmacist.
First oral endothelin receptor antagonist for PAH, now available in generic form with multiple manufacturers. Small molecule with established synthesis processes.
Help paying for Tracleer
Pick your insurance to see which help fits. Drugmaker copay cards can't be used with Medicare, Medicaid or TRICARE; charity funds are the usual route there.
- Copay help
Eligible commercially insured patients pay $5 per fill; maximum $20,000 per calendar year. Not valid with government insurance, or in CA or MA.
For: private insurance · source - Insurance and case manager help
Care Coordinators explain insurance coverage and out-of-pocket costs and refer to independent foundations and state programs.
The official page does not say who qualifies. Ask the program. · source
Good to know: Applies to brand TRACLEER only. Generic bosentan is sold by other makers and is not covered. The TRACLEER cost-support page does not mention the J&J Patient Assistance Program (free drug).
- From a charity · HealthWell FoundationPulmonary Hypertension (Medicare Access) fundOpen
Pays for: Copays, premiums or other treatment costs. Medicare patients only.
- From a charity · TotalAssist (formerly PAN Foundation)Pulmonary Hypertension fundOpen
Pays for: Out-of-pocket costs for approved medications, up to $9,500 per year. Requires health insurance (any kind).
- From a charity · The Assistance FundPulmonary Hypertension fundWaitlist
Pays for: Copays, coinsurance, deductibles and other health-related expenses.
The foundation says: “WAITLIST — Accepting Waitlist Patients. TAF is currently accepting requests to join the enrollment waitlist for this program. Waitlists a…”
Clinical trial results
The BREATHE-1 trial demonstrated significant improvement in 6-minute walk distance and WHO functional class compared to placebo. Long-term studies showed sustained hemodynamic and functional benefit.
Development history
Developed by Actelion (now part of Janssen/J&J). Approved November 2001 as a transformative treatment for PAH. Was among the first oral targeted therapies available. Generic versions became available after patent expiration, dramatically improving access.
Explore Pulmonary Arterial Hypertension trials
Other Pulmonary Arterial Hypertension treatments
Common questions about Bosentan
▸What is Bosentan (Tracleer)?
The first oral endothelin receptor antagonist approved for PAH. Tracleer was a breakthrough as one of the earliest targeted oral therapies, reducing pulmonary artery pressure and improving exercise capacity.
▸How does Bosentan work?
Endothelin-1 is a powerful vasoconstrictor that is overproduced in PAH, causing blood vessels in the lungs to narrow and stiffen. Bosentan blocks both ET-A and ET-B receptors, preventing endothelin-1 from constricting these vessels. This lowers pulmonary artery pressure and reduces the strain on the right side of the heart.
▸What are the side effects of Bosentan?
Carries a boxed warning for liver damage and for birth defects. Liver blood tests are required before starting and every month during treatment. Pregnancy must be ruled out before starting, and effective birth control is needed during treatment and for 1 month after stopping. Common side effects include respiratory infections, headache, swelling (edema), flushing, low blood pressure, and anemia. The label also warns about fluid buildup that has sometimes needed a hospital stay for heart failure, drops in red blood cells (hemoglobin should be checked after 1 and 3 months and then every 3 months), lower sperm counts, and fluid in the lungs in people with a rare lung blood vessel disease called pulmonary veno-occlusive disease. Bosentan must not be taken with cyclosporine A or glyburide. Available only through a restricted program (the Bosentan REMS) because of the liver risk.
▸How is Bosentan taken?
Taken as an oral tablet twice daily. For patients older than 12, the starting dose is 62.5 mg twice daily for 4 weeks, then 125 mg twice daily for those weighing more than 40 kg. It is approved for adults with PAH and for children 3 years and older with idiopathic or congenital PAH. Children 12 and younger are dosed by weight, and a tablet for oral suspension is available for children. Monthly liver function monitoring is mandatory. Generic versions are now available.
▸Is Bosentan FDA approved?
Yes, Bosentan (Tracleer) is FDA approved (2001) for the treatment of Pulmonary Arterial Hypertension.
▸Why does bosentan require monthly liver testing?
In clinical studies, about 11% of patients taking bosentan had liver enzyme (ALT or AST) levels rise to at least 3 times the upper limit of normal, compared with 2% on placebo. This is a class effect of endothelin receptor antagonists, though it is most pronounced with bosentan. Monthly liver function tests (ALT/AST) are mandatory for the duration of treatment. If liver enzymes become significantly elevated, the dose may need to be reduced or the drug discontinued.
▸Is generic bosentan available?
Yes. Generic bosentan became available after patent expiration, making it one of the most affordable targeted PAH therapies. Multiple generic manufacturers produce bosentan tablets. The availability of generics has been particularly important for PAH patients in countries where newer, more expensive endothelin receptor antagonists may not be accessible.
▸How does bosentan compare to macitentan?
Both are dual endothelin receptor antagonists, but macitentan (Opsumit) was designed to improve on bosentan in several ways. Macitentan has enhanced tissue penetration, does not require monthly liver function testing (lower hepatotoxicity risk), and demonstrated a reduction in morbidity and mortality events in the SERAPHIN trial. However, bosentan is available as a generic at much lower cost. The choice often involves balancing cost against the improved safety and efficacy profile of macitentan.
▸Can bosentan interact with other medications?
Yes. Bosentan is both a substrate and inducer of CYP450 liver enzymes, leading to numerous drug interactions. It reduces the effectiveness of hormonal contraceptives, requiring patients to use two forms of contraception. It can also interact with certain antifungals, immunosuppressants, and other PAH medications. Your physician and pharmacist should review all medications for potential interactions before starting bosentan.
▸Why is bosentan available only through a restricted program?
Bosentan is available only through the Bosentan REMS program because of its risk of liver damage. Prescribers and pharmacies must be enrolled, patients sign an enrollment form, and liver blood tests are required before starting and every month during treatment. Bosentan can also cause birth defects, so pregnancy must be ruled out before starting and effective birth control is needed during treatment and for 1 month after stopping.