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Macitentan Tablets
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 Tablets |
|---|---|
| Also known as | OPSUMIT |
| Sponsor | Dr Sudarshan Rajagopal |
| 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 (PAH). By antagonizing both ETA and ETB receptors on vascular smooth muscle and endothelial cells, macitentan reduces vasoconstriction, inhibits smooth muscle 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
- Outcome Study Assessing a 75 Milligrams (mg) Dose of Macitentan in Patients With Pulmonary Arterial Hypertension (PHASE3)
- A Study Providing Treatment Access in Participants With Pulmonary Hypertension Completing a Parent Study and Having no Other Option (PHASE3)
- A Study to Assess Whether Macitentan Delays Disease Progression in Children With Pulmonary Arterial Hypertension (PAH) (PHASE3)
- Efficacy and Mechanisms of Macitentan for Non-Coronary Obstructive Angina (EARLY_PHASE1)
- 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)
- Clinical Trial to Evaluate the Efficacy and Safety in Concomitant Administration of Macitentan and Dapagliflozin in Patients With Heart Failure With Mildly Reduced and Preserved Ejection Fraction (HFmrEF and HFpEF) and Combined Pre- and Post-capillary Pulmonary Hypertension (CpcPH) (PHASE4)
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 Tablets CI brief — competitive landscape report
- Macitentan Tablets updates RSS · CI watch RSS
- Dr Sudarshan Rajagopal portfolio CI