Comparative Pharmacology
Head-to-head clinical analysis: AMBRISENTAN versus BOSENTAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMBRISENTAN versus BOSENTAN.
AMBRISENTAN vs BOSENTAN
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; blocks endothelin-1 (ET-1) from binding to ETA and ETB receptors, inhibiting vasoconstriction and 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.
62.5 mg orally twice daily for 4 weeks, then increase to maintenance dose of 125 mg twice daily.
MODERATE Risk
MODERATE Risk
Clinical Note
moderateBosentan + Digoxin
"The serum concentration of Digoxin can be decreased when it is combined with Bosentan."
Clinical Note
moderateBosentan + Digitoxin
"The serum concentration of Digitoxin can be decreased when it is combined with Bosentan."
Clinical Note
moderateBosentan + Torasemide
"Bosentan may increase the hypotensive activities of Torasemide."
Clinical Note
moderateBosentan + Estrone sulfate
Terminal elimination half-life is approximately 9 hours (range 4–20 hours) in healthy subjects; no significant accumulation is observed with once-daily dosing.
Terminal elimination half-life is approximately 5 hours in healthy adults, but prolonged in patients with hepatic impairment (up to 21 hours in Child-Pugh Class A and B).
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).
Primarily biliary excretion (≥50% as unchanged drug) with fecal elimination; renal excretion accounts for <3% of unchanged drug.
Category C
Category D/X
Endothelin Receptor Antagonist
Endothelin Receptor Antagonist
"The serum concentration of Estrone sulfate can be decreased when it is combined with Bosentan."