Table 2.
Disadvantages and advantages of endothelin (ET)-receptor antagonists
| Parameters | Ambrisentan (Volibris) | Bosentan (Tracleer) | Macitentan (Opsumit) |
|---|---|---|---|
| Oral administration | Once daily | Twice daily | Once daily |
| Need for monitoring of transaminases | ++− | +++ | −++ |
| Need for hemoglobin monitoring | +++ | +++ | +++ |
| Selectivity ratio for ETA (ETA: ETB) | 200:1 | 20:1 | 50:1 |
| Antagonist for ETA and ETB | − − − | +++ | +++ |
| Prevalent type of elimination | Biliary system | Biliary system | Kidneys |
| Peripheral edema | +++− | ++− | +− − − |
| Drug interactions | +− − − | +++− | ++− − |
| Contraindications | Child–Pugh C, pregnancy, breastfeeding, idiopathic pulmonary fibrosis | Child–Pugh B–C, pregnancy, concomitant cyclosporine A | Child–Pugh C, pregnancy, breastfeeding |
| Results confirmed by trials with composite primary end point (morbidity and mortality) | +++ | − − − | +++ |