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Bosentan and Sildenafil
Bosentan blocks endothelin-1 receptors while sildenafil inhibits phosphodiesterase-5, together reducing pulmonary vascular resistance and improving right ventricular function.
Bosentan blocks endothelin-1 receptors while sildenafil inhibits phosphodiesterase-5, together reducing pulmonary vascular resistance and improving right ventricular function. Used for Pulmonary arterial hypertension.
At a glance
| Generic name | Bosentan and Sildenafil |
|---|---|
| Sponsor | Rigshospitalet, Denmark |
| Drug class | Endothelin receptor antagonist and phosphodiesterase-5 inhibitor combination |
| Target | Endothelin receptors (ETA/ETB) and phosphodiesterase-5 |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
Bosentan is an endothelin receptor antagonist that blocks the vasoconstrictive effects of endothelin-1 in pulmonary vessels. Sildenafil is a phosphodiesterase-5 inhibitor that increases cyclic GMP levels, promoting vasodilation. The combination targets complementary pathways in pulmonary hypertension pathophysiology to achieve synergistic hemodynamic improvement.
Approved indications
- Pulmonary arterial hypertension
Common side effects
- Headache
- Flushing
- Dyspepsia
- Peripheral edema
- Hepatotoxicity
Key clinical trials
- Mono vs. Dual Therapy for Pediatric Pulmonary Arterial Hypertension (PHASE3)
- Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM) - PDE5
- Combination Therapy in Pulmonary Arterial Hypertension (PHASE4)
- Effects of the Combination of Bosentan and Sildenafil Versus Sildenafil Monotherapy on Pulmonary Arterial Hypertension (PAH) (PHASE4)
- The "VISION" Trial: Ventavis Inhalation With Sildenafil to Improve and Optimize Pulmonary Arterial Hypertension (PHASE3)
- Initial Triple Therapy Including Parenteral Treprostinil vs Initial Double Oral Therapy in PAH Group I Patients (PHASE4)
- Vascular Dysfunction in Black Individuals: Roles of Nitric Oxide and Endothelin-1 (EARLY_PHASE1)
- Chronic Thrombo-embolic Pulmonary Hypertension: Classification and Long Term Outcome
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:
- Bosentan and Sildenafil CI brief — competitive landscape report
- Bosentan and Sildenafil updates RSS · CI watch RSS
- Rigshospitalet, Denmark portfolio CI