Comparative Pharmacology
Head-to-head clinical analysis: MACITENTAN versus TRACLEER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MACITENTAN versus TRACLEER.
MACITENTAN vs TRACLEER
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Endothelin receptor antagonist (ERA) that blocks the binding of endothelin-1 (ET-1) to ETA and ETB receptors, thereby inhibiting vasoconstriction and smooth muscle proliferation.
Bosentan is a dual endothelin receptor antagonist (ERA) that blocks endothelin-1 (ET-1) from binding to ETA and ETB receptors in pulmonary vascular smooth muscle and endothelium, reducing vasoconstriction and cell proliferation.
10 mg orally once daily.
Initial: 62.5 mg twice daily orally for 4 weeks, then increase to maintenance: 125 mg twice daily orally.
None Documented
None Documented
Terminal elimination half-life is 11–22 hours in healthy subjects; in pulmonary arterial hypertension patients, mean half-life is approximately 13 hours.
Clinical Note
moderateMacitentan + Methylphenidate
"Macitentan may decrease the antihypertensive activities of Methylphenidate."
Clinical Note
moderateMacitentan + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Macitentan."
Clinical Note
moderateMacitentan + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Macitentan."
Clinical Note
moderateMacitentan + Cyclosporine
Terminal elimination half-life is approximately 4-5 hours in healthy adults. In patients with pulmonary arterial hypertension, half-life may be slightly prolonged (up to 6-8 hours) due to reduced clearance.
Biliary/fecal (major, 93% as metabolites) and renal (3% unchanged, <5% of dose in urine).
Primarily hepatic metabolism (CYP2C9 and CYP3A4) with biliary excretion of unchanged drug and metabolites. Renal excretion of unchanged drug is negligible (<1%). Fecal excretion accounts for ~75% of total clearance, with ~25% excreted in urine as metabolites.
Category D/X
Category C
Endothelin Receptor Antagonist
Endothelin Receptor Antagonist
"The metabolism of Cyclosporine can be decreased when combined with Macitentan."