Bosentan
Bosentan is an oral endothelin receptor antagonist used primarily to treat pulmonary arterial hypertension (PAH) and digital ulcers in patients with systemic sclerosis. It works by blocking endothelin-1, a potent vasoconstrictor, thereby reducing pulmonary vascular resistance and improving exercise capacity. This medication is typically prescribed when other treatments have not been adequate.
Bosentan is an antihypertensive medication that treats pulmonary arterial hypertension by blocking endothelin receptors to relax blood vessels.
Key facts at a glance
- ATC
- C02KX01
- RxNorm
- 75207
- Generic
- Bosentan
- Class
- atc-c02
- Brands
- Tracleer
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Pulmonary arterial hypertension (PAH) to improve exercise capacity and delay clinical worsening; digital ulcers in systemic sclerosis (scleroderma) to reduce ulcer incidence
Dual endothelin receptor antagonist that blocks endothelin-1 receptors (ETA and ETB) on vascular smooth muscle and endothelium, preventing vasoconstriction and vascular remodeling, which reduces pulmonary vascular resistance and lowers blood pressure
Requires monthly liver function monitoring due to hepatotoxicity risk; contraindicated in pregnancy (teratogenic); may cause fluid retention and anemia; significant drug interactions with cyclosporine, glyburide, and hormonal contraceptives; only available through restricted distribution program
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy