Comparative Pharmacology
Head-to-head clinical analysis: FILSPARI versus MACITENTAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FILSPARI versus MACITENTAN.
FILSPARI vs MACITENTAN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
FILSPARI (sparsentan) is an endothelin receptor antagonist (ERA) and angiotensin II receptor blocker (ARB) with high affinity for the endothelin type A (ETA) receptor and angiotensin II type 1 (AT1) receptor. It reduces proteinuria in IgA nephropathy by inhibiting endothelin-1 mediated vasoconstriction, inflammation, and fibrosis, and by blocking angiotensin II mediated effects.
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.
200 mg orally once daily, with or without food.
10 mg orally once daily.
None Documented
None Documented
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 half-life ~30 hours in healthy subjects, supporting once-daily dosing.
Terminal elimination half-life is 11–22 hours in healthy subjects; in pulmonary arterial hypertension patients, mean half-life is approximately 13 hours.
Primarily hepatic metabolism; <1% excreted unchanged in urine. ~59% of dose recovered in feces and ~27% in urine 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 / ARB
Endothelin Receptor Antagonist
"The metabolism of Cyclosporine can be decreased when combined with Macitentan."