Comparative Pharmacology
Head-to-head clinical analysis: LETAIRIS versus MACITENTAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LETAIRIS versus MACITENTAN.
LETAIRIS vs MACITENTAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Ambrisentan is an endothelin receptor antagonist that selectively inhibits endothelin-1 (ET-1) binding to endothelin type A (ETA) receptors in pulmonary vascular smooth muscle cells, reducing vasoconstriction and smooth muscle proliferation.
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.
5 mg orally once daily, with or without food; may increase to 10 mg once daily if tolerated.
10 mg orally once daily.
None Documented
None Documented
Terminal elimination half-life is approximately 9 hours (range 6–12 hours) in healthy adults.
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 11–22 hours in healthy subjects; in pulmonary arterial hypertension patients, mean half-life is approximately 13 hours.
Primarily via biliary/fecal elimination (approximately 80% of metabolites and unchanged drug; ~20% renal as metabolites).
Biliary/fecal (major, 93% as metabolites) and renal (3% unchanged, <5% of dose in urine).
Category C
Category D/X
Endothelin Receptor Antagonist
Endothelin Receptor Antagonist
"The metabolism of Cyclosporine can be decreased when combined with Macitentan."