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Tracleer (BOSENTAN)
Tracleer (bosentan) is a small molecule endothelin receptor antagonist developed by Actelion, targeting the endothelin-1 receptor to treat pulmonary arterial hypertension, pulmonary hypertension, and systemic sclerosis. It was FDA-approved in 2001 and is now off-patent with multiple generic manufacturers. Tracleer works by blocking the action of endothelin-1, a potent vasoconstrictor, to improve blood flow and reduce pressure in the lungs. As an off-patent medication, Tracleer is widely available in generic forms. Key safety considerations include potential liver enzyme elevations and teratogenic effects.
At a glance
| Generic name | BOSENTAN |
|---|---|
| Sponsor | AstraZeneca |
| Drug class | Endothelin Receptor Antagonist |
| Target | Endothelin-1 receptor |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 2001 |
Approved indications
- Pulmonary arterial hypertension
- Pulmonary hypertension
- Systemic sclerosis
Common side effects
- Abnormal liver function
- Marked decreases in hemoglobin (>15% decrease from baseline resulting in values <11 g/dL)
- Decline in sperm count of at least 50%
Serious adverse events
- Hepatotoxicity/Abnormal liver function (treatment discontinuation)
- Marked oligospermia
Drug interactions
- ciclosporin
- ethinylestradiol
- fluconazole
- glibenclamide
- itraconazole
- ketoconazole
- norethisterone
- sildenafil
- voriconazole
- warfarin
Key clinical trials
- Outcome Study Assessing a 75 Milligrams (mg) Dose of Macitentan in Patients With Pulmonary Arterial Hypertension (PHASE3)
- Mono vs. Dual Therapy for Pediatric Pulmonary Arterial Hypertension (PHASE3)
- Endothelin-1 Receptor Blockade in Resistant Hypertension (PHASE2)
- Dapagliflozin and Endothelin Receptor Antagonism in Large Vessel Vasculitis (DERAIL-LVV) (PHASE2)
- Pharmacokinetics of Drugs Administered to Children
- Preventive Effects of Bosentan on the Systemic Cardiovascular Consequence of Sleep Apnea (PHASE2)
- A Study in Healthy Men to Test Whether Bosentan Influences the Amount of BI 425809 in the Blood (PHASE1)
- A Study in Healthy Men to Test How Bosentan Influences the Amount of Nerandomilast in the Blood (PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
| 8309126 | 2026-05-15 | Formulation |
| 7959945 | 2027-12-28 | Formulation |
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Tracleer CI brief — competitive landscape report
- Tracleer updates RSS · CI watch RSS
- AstraZeneca portfolio CI