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Tracleer®
Tracleer blocks endothelin-1 receptors on vascular smooth muscle cells, preventing vasoconstriction and reducing pulmonary vascular resistance.
Tracleer blocks endothelin-1 receptors on vascular smooth muscle cells, preventing vasoconstriction and reducing pulmonary vascular resistance. Used for Pulmonary arterial hypertension (PAH), WHO Group 1, Pulmonary hypertension associated with connective tissue disease.
At a glance
| Generic name | Tracleer® |
|---|---|
| Also known as | Bosentan |
| Sponsor | Actelion |
| Drug class | Endothelin receptor antagonist |
| Target | Endothelin receptor A (ETA) and Endothelin receptor B (ETB) |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
Endothelin-1 is a potent vasoconstrictor that plays a key role in pulmonary hypertension pathophysiology. Tracleer is a non-selective endothelin receptor antagonist (blocking both ETA and ETB receptors) that inhibits endothelin-mediated vasoconstriction and smooth muscle proliferation in the pulmonary vasculature. This leads to improved hemodynamics and exercise capacity in patients with pulmonary arterial hypertension.
Approved indications
- Pulmonary arterial hypertension (PAH), WHO Group 1
- Pulmonary hypertension associated with connective tissue disease
Common side effects
- Headache
- Flushing
- Edema/fluid retention
- Palpitations
- Liver enzyme elevation
- Anemia
Key clinical trials
- A Study in Healthy Men to Test Whether Bosentan Influences the Amount of BI 425809 in the Blood (PHASE1)
- The Effect of Tracleer® on Male Fertility (PHASE4)
- Bioequivalence Study to Compare Bosentan 32 mg Dispersible Tablets Versus Tracleer® 32 mg Tablets (PHASE1)
- Effect of BIA 5-1058 400 mg on the Steady State Pharmacokinetics of Bosentan (PHASE1)
- Bioequivalence Study of Bosentan 125 mg Tablets Immediate Release (IR) Versus Tracleer® 125 mg Tablets IR In Healthy Subjects (PHASE1)
- Crossover Study From Macitentan or Bosentan Over to Ambrisentan (PHASE4)
- BREATHE 5-OL: Tracleer (Bosentan) in Patients With Pulmonary Arterial Hypertension Related to Eisenmenger Physiology (PHASE4)
- Study of Incidence of Respiratory Tract AEs in Patients Treated With Tyvaso® Compared to Other FDA Approved PAH Therapies
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 |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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
- Actelion portfolio CI