Comparative Pharmacology
Head-to-head clinical analysis: AMBRISENTAN versus MACITENTAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMBRISENTAN versus MACITENTAN.
AMBRISENTAN vs MACITENTAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Endothelin receptor antagonist (ERA) that selectively binds to endothelin type A (ETA) receptors in pulmonary vascular smooth muscle, blocking endothelin-1-mediated vasoconstriction and 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.
10 mg orally once daily, with or without food, for patients not receiving cyclosporine. For patients receiving cyclosporine, reduce dose to 5 mg once daily.
10 mg orally once daily.
MODERATE Risk
MODERATE Risk
Terminal elimination half-life is approximately 9 hours (range 4–20 hours) in healthy subjects; no significant accumulation is observed with once-daily dosing.
Clinical Note
moderateAmbrisentan + Teriflunomide
"The serum concentration of Teriflunomide can be increased when it is combined with Ambrisentan."
Clinical Note
moderateAmbrisentan + Methylphenidate
"Ambrisentan may decrease the antihypertensive activities of Methylphenidate."
Clinical Note
moderateMacitentan + Methylphenidate
"Macitentan may decrease the antihypertensive activities of Methylphenidate."
Clinical Note
moderateAmbrisentan + Sulfisoxazole
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 nonrenal pathways, with fecal excretion accounting for approximately 77% of a radiolabeled dose (as unchanged drug and metabolites) and renal excretion for about 22% (mostly 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 Sulfisoxazole can be decreased when combined with Ambrisentan."