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macitentan (ACT-064992)
Macitentan is a dual endothelin receptor antagonist that blocks both ETA and ETB receptors to reduce pulmonary vascular resistance and improve exercise capacity in pulmonary arterial hypertension.
Macitentan is a dual endothelin receptor antagonist that blocks both ETA and ETB receptors to reduce pulmonary vascular resistance and improve exercise capacity in pulmonary arterial hypertension. Used for Pulmonary arterial hypertension (PAH).
At a glance
| Generic name | macitentan (ACT-064992) |
|---|---|
| Sponsor | Actelion |
| Drug class | Endothelin receptor antagonist |
| Target | ETA and ETB receptors |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
Endothelin is a potent vasoconstrictor that plays a key role in the pathophysiology of pulmonary arterial hypertension. By antagonizing both ETA and ETB receptors on vascular smooth muscle and endothelial cells, macitentan reduces vasoconstriction, inhibits cell proliferation, and decreases inflammation in the pulmonary vasculature. This leads to improved hemodynamics and clinical outcomes in PAH patients.
Approved indications
- Pulmonary arterial hypertension (PAH)
Common side effects
- Headache
- Nasopharyngitis
- Anemia
- Peripheral edema
- Flushing
Key clinical trials
- A Study to Assess Whether Macitentan Delays Disease Progression in Children With Pulmonary Arterial Hypertension (PAH) (PHASE3)
- Clinical Study to Compare the Efficacy and Safety of Macitentan and Tadalafil Monotherapies With the Corresponding Fixed-dose Combination Therapy in Subjects With Pulmonary Arterial Hypertension (PAH) (PHASE3)
- A Study of Macitentan in Japanese Pediatric Participants With Pulmonary Arterial Hypertension (PHASE3)
- Effects of Combination Medical Therapy Followed by BPA on Right Ventricular-PA Coupling and Hemodynamics in CTEPH (PHASE3)
- A Study to Evaluate Efficacy and Safety of Macitentan 75 mg in Inoperable or Persistent/Recurrent Chronic Thromboembolic Pulmonary Hypertension (PHASE3)
- A Study to Compare the Macitentan-tadalafil Fixed Dose Combination Tablet Relative to the Concomitant Administration of the Reference Tablets of Macitentan and Tadalafil in Healthy Subjects (PHASE1)
- Clinical Study to Investigate the Effect of Macitentan on the Concentrations of Rosuvastatin in the Blood of Healthy Male Subjects (PHASE1)
- A Clinical Study to Investigate the Long-term Safety of the Drug Macitentan in Patients With Pulmonary Hypertension Who Were Previously Treated With Macitentan in Clinical Studies. (PHASE3)
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:
- macitentan (ACT-064992) CI brief — competitive landscape report
- macitentan (ACT-064992) updates RSS · CI watch RSS
- Actelion portfolio CI