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Brand Name :
Filspari
Synonyms :
sparsentan
Class :
Dual Endothelin Angiotensin Receptor Antagonists (DEARAs)
Brand Name :
Filspari
Synonyms :
sparsentan
Class :
Dual Endothelin Angiotensin Receptor Antagonists (DEARAs)
Dosage Forms & StrengthsÂ
TabletÂ
200 mg orally every Day initially; following 14 days, increase to advised dose of 400 mg every Day
When resuming, start with 200 mg/day and then gradually increase to 400 mg/day after 14 days
Dose Adjustments
Dosage Modifications
ALT/AST >3x to ≤8x ULN
Repeat observations to verify elevation
If confirmed, discontinue medication. Once levels return to pre-treatment values and the patient is asymptomatic, monitor ALT/AST levels, bilirubin levels, and INR at least once a week.
Coadministration of strong CYP3A4 inhibitors
Avoid from coadministration
In case usage cannot be avoided, interrupt sparsentan
Renal impairment
There were no clinically significant variations in the pharmacokinetics of mild-to-moderate (eGFR 30-89 mL/min/1.73 m2) patients.
Unstudied for severe (eGFR 30 mL/min/1.73 m2)
Hepatic impairment
(Child-Pugh A-C) Mild, moderate, or severe Avoid usage as there is a danger of severe liver damage if there is any hepatic impairment.
Dosing Considerations
Before initiating
Check that women who are sexually active are not pregnant and that they are taking effective contraception.
Assess ALT, AST, and bilirubin; avoid from initiating if >3x ULN
Aliskiren, endothelin receptor antagonists, and renin-angiotensin-aldosterone system (RAAS) inhibitors should not be used anymore.
Monitoring
Prior to starting therapy, ALT, AST, and bilirubin should be monitored. For the first 12 months, they should be checked every month.
Check on women who are sexually active every month while they are receiving therapy and for one month after they stop taking the drug.
Safety and efficacy not establishedÂ
Refer to the adult dosing regimenÂ
spironolactone and hydrochlorothiazide
may enhance the potassium levels in the blood when combined with sparsentan.
may enhance the potassium levels in the blood when combined with sparsentan.
may enhance the potassium levels in the blood when combined with sparsentan.
may enhance the potassium levels in the blood when combined with sparsentan.
may enhance the potassium levels in the blood when combined with sparsentan.
may enhance the hypotensive effect when combined with sparsentan
may enhance the hypotensive effect when combined with sparsentan
may enhance the hypotensive effect when combined with sparsentan
may enhance the hypotensive effect when combined with sparsentan
may enhance the hypotensive effect when combined with sparsentan
may diminish the effectiveness of reducing proteinuria when combined with sparsentan
may diminish the effectiveness of reducing proteinuria when combined with sparsentan
may diminish the effectiveness of reducing proteinuria when combined with sparsentan
may diminish the effectiveness of reducing proteinuria when combined with sparsentan
may diminish the effectiveness of reducing proteinuria when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
may increase or decrease the activity of this enzyme when combined with sparsentan
sparsentan: they may diminish the serum concentration of antacids
sparsentan: they may diminish the serum concentration of antacids
sparsentan: they may diminish the serum concentration of antacids
sparsentan: they may diminish the serum concentration of antacids
sparsentan: they may diminish the serum concentration of antacids
sparsentan: they may diminish the serum concentration of antacids
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
may have an increasingly adverse effect when combined with ACE inhibitors
may have an increasingly adverse effect when combined with ACE inhibitors
may have an increasingly adverse effect when combined with ACE inhibitors
it increases the toxicity of angiotensin II receptor blockers
it increases the toxicity of angiotensin II receptor blockers
it increases the toxicity of angiotensin II receptor blockers
it increases the toxicity of angiotensin II receptor blockers
it increases the toxicity of angiotensin II receptor blockers
it increases the toxicity of angiotensin II receptor blockers
it increases the toxicity of angiotensin II receptor blockers
may enhance the serum concentration of P-glycoprotein/ABCB1 Substrates
sparsentan: they may increase the CNS depressant effect of CNS Depressants
sparsentan: they may increase the CNS depressant effect of CNS Depressants
sparsentan: they may increase the CNS depressant effect of CNS Depressants
sparsentan: they may increase the CNS depressant effect of CNS Depressants
sparsentan: they may increase the CNS depressant effect of CNS Depressants
Actions and spectrum:Â
sparsentan is an investigational drug used to treat focal segmental glomerulosclerosis (FSGS) and IgA nephropathy. It is a dual endothelin receptor antagonist (ERA) and angiotensin receptor blocker (ARB), meaning that it blocks both the endothelin and angiotensin receptors in the body.
This combination of mechanisms of action may provide a more comprehensive approach to treating certain kidney diseases. sparsentan is thought to reduce proteinuria, or the excessive excretion of protein in the urine, which is a hallmark feature of FSGS and other kidney diseases.Â
Frequency definedÂ
>10%Â
Dizziness (13%)Â
Hyperkalemia (13%)Â
Hypotension (14%)Â
Peripheral edema (14%)Â Â
1-10%Â
Transaminase elevations (2.5%)Â
Acute kidney injury (4%)Â
Anemia (5%)Â
Contraindication/Caution:Â
Contraindication:Â
Caution:Â
As sparsentan is still investigational and not yet approved for use by the FDA, there are no official cautions available at this time. However, during clinical trials, some common adverse effects were observed, such as dizziness, fatigue, and diarrhea. Additionally, sparsentan may interact with other medications, particularly those that affect the renin-angiotensin system. Â
Comorbidities:Â
Hypertension, hyperlipidemia, diabetes mellitus, and cardiovascular disease.Â
Pregnancy consideration: pregnancy category is unknown.Â
Lactation: safety and efficacy are not established. Â
Pregnancy category:Â
Pharmacology:Â
sparsentan is a dual-acting angiotensin receptor blocker and endothelin receptor antagonist. It selectively inhibits the angiotensin II type 1 receptor (AT1) and the endothelin type A receptor (ETA), both of which are involved in the pathophysiology of kidney disease. By blocking the AT1 receptor, sparsentan reduces the vasoconstrictor and pro-inflammatory effects of angiotensin II, leading to improved blood pressure control and decreased proteinuria.
Additionally, by blocking the ETA receptor, sparsentan reduces the production of endothelin 1, a potent vasoconstrictor, and profibrotic mediator, which can lead to further protection of kidney function. sparsentan has also been shown to have anti-inflammatory and antioxidant effects, which may contribute to its renoprotective effects. Overall, sparsentan is thought to improve kidney function and delay the progression of kidney disease in patients with focal segmental glomerulosclerosis (FSGS) and IgA nephropathy (IgAN).Â
Pharmacodynamics:Â
sparsentan is a dual angiotensin receptor blocker (ARB) and endothelin receptor antagonist (ERA). It works by blocking the action of angiotensin II and endothelin, which are both vasoconstrictors, leading to vasodilation and decreased blood pressure.Â
The drug has been studied for its effectiveness in treating focal segmental glomerulosclerosis (FSGS) and IgA nephropathy, which are both kidney diseases. By blocking both the angiotensin and endothelin pathways, sparsentan may help to reduce proteinuria and slow the progression of kidney damage. Â
Pharmacokinetics:Â
AbsorptionÂ
After oral administration, sparsentan is rapidly absorbed with a median time to maximum plasma concentration (Tmax) of 2 to 3 hours. The absolute bioavailability of sparsentan is approximately 50%.Â
DistributionÂ
The steady-state volume(Vss) of sparsentan is estimated to be 20 to 30 L, suggesting that it is extensively distributed in the body. sparsentan is highly protein-bound (≥99%) to plasma proteins, mainly albumin.Â
MetabolismÂ
sparsentan is mainly metabolized in the liver by cytochrome P450 (CYP) 3A4 and, to a lesser extent, by CYP2C9. The major circulating metabolites are sparsentan M1 (formed by hydroxylation of the parent compound) and sparsentan M2 (formed by hydrolysis of the carboxylic ester bond).Â
Elimination and excretionÂ
The elimination half-life (t1/2) of sparsentan is approximately 14 to 17 hours. sparsentan and its metabolites are primarily excreted in the feces (70-80%) and, to a lesser extent, in the urine (20-30%). sparsentan is eliminated mainly by biliary excretion, with minimal renal elimination.Â
Administration:Â
sparsentan is available in the form of tablets for oral administration. It should be administered with or without food, usually once daily, as directed by the healthcare provider. The tablet should be swallowed whole and not crushed, chewed, or broken.
The dosage may vary based on the patient’s medical condition, treatment, and other medications they may be taking. Patients should follow the instructions provided by their healthcare provider regarding the use of sparsentan.Â
Patient information leafletÂ
Generic Name: sparsentanÂ
Pronounced: (spa-rs-en-tan)Â Â
Why do we use sparsentan?Â
sparsentan is an investigational medication that is evaluated in clinical trials for the treatment of several conditions, including diabetic kidney disease (DKD) and focal segmental glomerulosclerosis (FSGS), both of which are types of kidney disease. If approved, sparsentan could potentially be used to help slow the progression of kidney damage and preserve kidney function in people with these conditions.Â
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