Comparative Pharmacology
Head-to-head clinical analysis: FILSPARI versus LOSARTAN POTASSIUM.
Head-to-head clinical analysis: FILSPARI versus LOSARTAN POTASSIUM.
FILSPARI vs LOSARTAN POTASSIUM
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.
Angiotensin II receptor antagonist. Blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle and adrenal gland, resulting in vasodilation and reduced aldosterone secretion.
200 mg orally once daily, with or without food.
50 mg orally once daily; may increase to 100 mg once daily based on blood pressure response.
None Documented
None Documented
Terminal half-life ~30 hours in healthy subjects, supporting once-daily dosing.
Terminal elimination half-life: losartan ~2 hours; active metabolite E-3174 ~6-9 hours. Clinically, the long half-life of E-3174 allows once-daily dosing.
Primarily hepatic metabolism; <1% excreted unchanged in urine. ~59% of dose recovered in feces and ~27% in urine as metabolites.
Losartan and its active metabolite E-3174 are eliminated via renal (35% of dose) and biliary/fecal (60% of dose) routes. Approximately 4% of an oral dose is excreted unchanged in urine, while 6% is excreted as E-3174 in urine.
Category C
Category D/X
Endothelin Receptor Antagonist / ARB
ARB