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تعداد آیتم قابل مشاهده باقیمانده : 3 مورد

Sparsentan: Drug information

Sparsentan: Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Sparsentan: Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Distribution program:

Because of the risks of hepatotoxicity and birth defects, sparsentan is available only through a restricted program called the Filspari REMS. Under the REMS, prescribers, patients, and pharmacies must enroll in the program.

Hepatotoxicity:

Some endothelin receptor antagonists have caused elevations of aminotransferases, hepatotoxicity, and liver failure. In clinical studies, elevations in aminotransferases (ALT or AST) of at least 3 × the ULN have been observed in up to 3.5% of sparsentan-treated patients, including cases confirmed with rechallenge. Measure transaminases and bilirubin before initiating treatment and monthly for the first 12 months, and then every 3 months during treatment. Interrupt treatment and closely monitor patients who develop aminotransferase elevations more than 3 × ULN. Sparsentan should generally be avoided in patients with elevated aminotransferases (>3 × ULN) at baseline because monitoring for hepatotoxicity may be more difficult and these patients may be at increased risk for serious hepatotoxicity.

Embryo-Fetal Toxicity:

Sparsentan can cause major birth defects if used by pregnant patients based on animal data. Therefore, pregnancy testing is required before the initiation of treatment, during treatment, and 1 month after discontinuation of treatment with sparsentan. Patients who can become pregnant must use effective contraception before the initiation of treatment, during treatment, and for 1 month after discontinuation of treatment with sparsentan.

Brand Names: US
  • Filspari
Pharmacologic Category
  • Angiotensin II Receptor Blocker;
  • Endothelin Receptor Antagonist
Dosing: Adult
IgA nephropathy, primary, nonvariant

IgA nephropathy, primary, nonvariant:

Note: May consider as an alternative nonimmunosuppressive therapy in patients at high risk of chronic kidney disease progression (eg, proteinuria >0.75 to 1 g/day) despite receiving optimized therapy (eg, maximally tolerated angiotensin converting enzyme [ACE] inhibitors or angiotensin receptor blockers [ARBs]) for at least 3 to 6 months (Ref). Safety: Prior to initiating therapy, discontinue renin-angiotensin-aldosterone system inhibitors and endothelin receptor antagonists. Consider adjusting or eliminating other medications that may decrease blood pressure in patients at risk for hypotension.

Oral: 200 mg once daily for 14 days, then increase to target dose of 400 mg once daily if tolerated.

Interruption of therapy: Consider restarting at 200 mg once daily after a treatment interruption. After 14 days, increase to target dose of 400 mg once daily if tolerated.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Kidney impairment prior to treatment initiation:

eGFR ≥30 mL/minute/1.73 m2: No dosage adjustments provided in the manufacturer’s labeling; however, need for dosage adjustment unlikely as no clinically significant differences in pharmacokinetics were observed in this population.

eGFR <30 mL/minute/1.73 m2: No dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Acute kidney injury during treatment: Consider withholding or discontinuing in patients who develop a significant decrease in kidney function.

Dosing: Liver Impairment: Adult

Hepatic impairment prior to treatment: Avoid use in patients with any hepatic impairment (Child-Pugh class A to C) due to the potential risk of serious liver injury.

Aminotransferase elevations during treatment:

ALT or AST >3 times and ≤8 times the ULN:

Confirm elevation with a repeat measure. If confirmed, interrupt treatment and monitor aminotransferase levels and bilirubin at least weekly (INR periodically as needed) until levels return to pretreatment values and patient is asymptomatic. Then may consider reinitiating therapy at 200 mg once daily with close monitoring, with reassessment of hepatic enzyme levels and bilirubin within 3 days.

Do not resume treatment if patient has experienced clinical symptoms of hepatotoxicity or the following occurs with no other identifiable cause:

ALT or AST > 3 times ULN and total bilirubin >2 times ULN or INR >1.5.

ALT or AST >3 times ULN with symptoms of fatigue, nausea, vomiting, right upper quadrant pain/tenderness, fever, rash, and/or eosinophilia (>5% eosinophils).

ALT or AST >5 times ULN for more than 2 weeks.

ALT or AST >8 times the ULN: Permanently discontinue treatment if no other cause for elevation identified.

Dosing: Adjustment for Toxicity: Adult

Fluid retention: Determine underlying cause and evaluate potential need to initiate or modify diuretic treatments prior to reducing the dose of sparsentan.

Hyperkalemia: Reducing sparsentan dose or discontinuing sparsentan therapy may be required.

Hypotension (despite elimination or reduction of other antihypertensives): Consider reducing sparsentan dose or interrupting sparsentan therapy. Can consider reinitiating once BP is stabilized.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions (Significant): Considerations
Acute kidney injury

Acute kidney injury (AKI) has been reported with sparsentan. In one clinical study, AKI was defined by decreases in serum creatinine between outpatient visits and rarely led to sparsentan discontinuation (Ref). Increases in serum creatinine secondary to angiotensin II receptor blockers usually stabilize within 20% to 30% from baseline and are expected; additional increases may indicate renal artery stenosis or volume depletion (Ref).

Mechanism: Related to pharmacologic action; angiotensin II receptor blockade inhibits efferent arteriolar vasoconstriction, lowering glomerular filtration pressure which can lead to a modest reduction in glomerular filtration rate (GFR) (Ref).

Onset: Intermediate; initial reduction in GFR generally occurs within 4 weeks of initiation and then stabilizes.

Risk factors:

Volume depletion

Severe congestive heart failure

Concurrent diuretic, renin-angiotensin system inhibitor, and/or nonsteroidal anti-inflammatory use (Ref)

Hypotension (Ref)

Chronic kidney disease

Patients with low renal blood flow (eg, renal artery stenosis) whose GFR is dependent on efferent arteriolar vasoconstriction by angiotensin II (Ref)

Hepatic effects

Increased serum alanine aminotransferase (ALT) and increased serum aspartate aminotransferase (AST) have been reported with sparsentan. Increased ALT and AST were ≥3 times the ULN, asymptomatic, and reversible. Although some endothelin receptor antagonists have caused hepatotoxicity and hepatic failure, there were no reports with sparsentan in clinical trials.

Risk factors:

Elevated transaminases (>3 times the ULN) at baseline

Hyperkalemia

Hyperkalemia has been reported with sparsentan. Most reported cases of hyperkalemia were mild to moderate and did not require therapy discontinuation (Ref).

Mechanism: Related to pharmacologic action; angiotensin II receptor blockade prevents angiotensin II from binding to the adrenal receptor and interferes with generation of angiotensin II within the adrenal cortex, decreasing aldosterone release and impairing kidney potassium excretion (Ref).

Onset: Generally occurs within 1 week of angiotensin receptor blocker initiation (Ref).

Risk factors:

Advanced kidney disease

Baseline elevated potassium (≥5 mmol/L) (Ref)

Older patients (Ref)

Diabetes (Ref)

Concurrent use of medications known to decrease renin and aldosterone (eg, direct renin inhibitors, nonsteroidal anti-inflammatory drugs, cyclosporine, tacrolimus, beta-blockers, sulfamethoxazole/trimethoprim, azole antifungals) (Ref)

Concomitant use of potassium supplements, potassium-sparing diuretics, and/or potassium-containing salt substitutes

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.

>10%:

Cardiovascular: Hypotension (16%; including orthostatic hypotension), peripheral edema (16%)

Endocrine & metabolic: Hyperkalemia (17%) (table 1)

Sparsentan: Adverse Reaction: Hyperkalemia

Drug (Sparsentan)

Comparator (Irbesartan)

Number of Patients (Sparsentan)

Number of Patients (Irbesartan)

17%

13%

202

202

Nervous system: Dizziness (16%)

1% to 10%:

Hematologic & oncologic: Anemia (8%)

Hepatic: Increased serum transaminases (4%; including increased serum alanine aminotransferase and increased serum aspartate aminotransferase >3 × ULN) (table 2)

Sparsentan: Adverse Reaction: Increased Serum Transaminases

Drug (Sparsentan)

Comparator (Irbesartan)

Number of Patients (Sparsentan)

Number of Patients (Irbesartan)

Comments

4%

4%

202

202

Including increased serum alanine aminotransferase and increased serum aspartate aminotransferase >3 × ULN

Renal: Acute kidney injury (6%) (table 3)

Sparsentan: Adverse Reaction: Acute Kidney Injury

Drug (Sparsentan)

Comparator (Irbesartan)

Number of Patients (Sparsentan)

Number of Patients (Irbesartan)

6%

2%

202

202

Frequency not defined: Hepatic: Hepatic failure, hepatotoxicity

Contraindications

Pregnancy; coadministration with angiotensin receptor blockers, endothelin receptor antagonists, or aliskiren.

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Filspari: 200 mg, 400 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Filspari Oral)

200 mg (per each): $497.29

400 mg (per each): $497.29

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Swallow tablets whole with water prior to morning or evening meal. Maintain the same dosing pattern in relationship to meals.

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/216403s000lbl.pdf#page=22, must be dispensed with this medication.

Use: Labeled Indications

IgA nephropathy, primary, nonvariant (alternative agent): To slow kidney function decline in adults with primary IgA nephropathy (IgAN) who are at high risk for disease progression.

Medication Safety Issues
High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).

Metabolism/Transport Effects

Substrate of BCRP, CYP3A4 (Major), P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Induces CYP2B6 (Weak);

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Alfuzosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Aliskiren: Sparsentan may increase adverse/toxic effects of Aliskiren. Risk X: Avoid

Amifostine: Blood Pressure Lowering Agents may increase hypotensive effects of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider Therapy Modification

Amisulpride (Oral): May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Angiotensin II Receptor Blockers: Sparsentan may increase adverse/toxic effects of Angiotensin II Receptor Blockers. Risk X: Avoid

Angiotensin II: Angiotensin II Receptor Blockers may decrease therapeutic effects of Angiotensin II. Risk C: Monitor

Angiotensin-Converting Enzyme Inhibitors: Sparsentan may increase adverse/toxic effects of Angiotensin-Converting Enzyme Inhibitors. Risk X: Avoid

Antacids: May decrease serum concentration of Sparsentan. Management: Administer sparsentan 2 hours before or 2 hours after antacids. Risk D: Consider Therapy Modification

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may increase hypotensive effects of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor

Arginine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Barbiturates: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors): Sparsentan may increase serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid

Benperidol: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Blood Pressure Lowering Agents: May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Brimonidine (Topical): May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Bromperidol: May decrease hypotensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase hypotensive effects of Bromperidol. Risk X: Avoid

BuPROPion: CYP2B6 Inducers (Weak) may decrease serum concentration of BuPROPion. Risk C: Monitor

Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor

CycloSPORINE (Systemic): Sparsentan may increase serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase serum concentration of Sparsentan. Risk X: Avoid

CYP2C9 Substrates (Narrow Therapeutic Index/Sensitive with Inducers): Sparsentan may decrease serum concentration of CYP2C9 Substrates (Narrow Therapeutic Index/Sensitive with Inducers). Risk C: Monitor

CYP3A4 Inducers (Moderate): May decrease serum concentration of Sparsentan. Risk C: Monitor

CYP3A4 Inducers (Strong): May decrease serum concentration of Sparsentan. Risk X: Avoid

CYP3A4 Inhibitors (Moderate): May increase serum concentration of Sparsentan. Risk C: Monitor

CYP3A4 Inhibitors (Strong): May increase serum concentration of Sparsentan. Risk X: Avoid

Dapoxetine: May increase orthostatic hypotensive effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Diazoxide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Dipeptidyl Peptidase-IV Inhibitors: May increase adverse/toxic effects of Angiotensin II Receptor Blockers. Specifically, the risk for angioedema may be increased with this combination. Risk C: Monitor

Drospirenone-Containing Products: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

DULoxetine: Blood Pressure Lowering Agents may increase hypotensive effects of DULoxetine. Risk C: Monitor

Endothelin Receptor Antagonists: Sparsentan may increase adverse/toxic effects of Endothelin Receptor Antagonists. Risk X: Avoid

Finerenone: Angiotensin II Receptor Blockers may increase hyperkalemic effects of Finerenone. Risk C: Monitor

Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification

Grapefruit Juice: May increase serum concentration of Sparsentan. Risk C: Monitor

Heparin: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Heparins (Low Molecular Weight): May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Herbal Products with Blood Pressure Lowering Effects: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Histamine H2 Receptor Antagonists: May decrease serum concentration of Sparsentan. Risk X: Avoid

Hypotension-Associated Agents: Blood Pressure Lowering Agents may increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Iloperidone: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Inhibitors of the Proton Pump (PPIs and PCABs): May decrease serum concentration of Sparsentan. Risk X: Avoid

Lefamulin: Sparsentan may increase serum concentration of Lefamulin. Lefamulin may increase serum concentration of Sparsentan. Specifically, the use of oral lefamulin may increase sparsentan concentrations. Risk X: Avoid

Levodopa-Foslevodopa: Blood Pressure Lowering Agents may increase hypotensive effects of Levodopa-Foslevodopa. Risk C: Monitor

Lithium: Angiotensin II Receptor Blockers may increase serum concentration of Lithium. Management: Initiate lithium at lower doses in patients receiving an angiotensin II receptor blocker (ARB). Consider lithium dose reductions in patients stable on lithium therapy who are initiating an ARB. Monitor lithium concentrations closely when combined. Risk D: Consider Therapy Modification

Loop Diuretics: May increase hypotensive effects of Angiotensin II Receptor Blockers. Loop Diuretics may increase nephrotoxic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Lormetazepam: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Metergoline: May decrease antihypertensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase orthostatic hypotensive effects of Metergoline. Risk C: Monitor

Molsidomine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Naftopidil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nicergoline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nicorandil: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Nicorandil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nitroprusside: Blood Pressure Lowering Agents may increase hypotensive effects of Nitroprusside. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents (Topical): May decrease therapeutic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents: May decrease therapeutic effects of Angiotensin II Receptor Blockers. The combination of these two agents may also significantly decrease glomerular filtration and renal function. Angiotensin II Receptor Blockers may increase adverse/toxic effects of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Risk C: Monitor

Obinutuzumab: May increase hypotensive effects of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider Therapy Modification

P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors): Sparsentan may increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid

Pentoxifylline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Pholcodine: Blood Pressure Lowering Agents may increase hypotensive effects of Pholcodine. Risk C: Monitor

Phosphodiesterase 5 Inhibitors: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Polyethylene Glycol-Electrolyte Solution: Angiotensin II Receptor Blockers may increase nephrotoxic effects of Polyethylene Glycol-Electrolyte Solution. Risk C: Monitor

Potassium Salts: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Potassium-Sparing Diuretics: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Prostacyclin Analogues: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Quinagolide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Ranolazine: May increase adverse/toxic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Sacubitril: Angiotensin II Receptor Blockers may increase adverse/toxic effects of Sacubitril. Risk X: Avoid

Silodosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Sodium Phosphates: Angiotensin II Receptor Blockers may increase nephrotoxic effects of Sodium Phosphates. Specifically, the risk of acute phosphate nephropathy may be enhanced. Risk C: Monitor

Tolvaptan: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Trimethoprim: May increase hyperkalemic effects of Angiotensin II Receptor Blockers. Risk C: Monitor

Reproductive Considerations

Evaluate pregnancy status prior to use; verify the patient is not pregnant prior to treatment initiation in patients who could become pregnant. A negative pregnancy test is required prior to treatment initiation, monthly during treatment, and 1 month after the last dose of sparsentan in patients who could become pregnant. Additional pregnancy testing is also recommended if menses is delayed or whenever pregnancy is suspected.

Patients who could become pregnant should use effective contraception during therapy and for 1 month after the last sparsentan dose. Options for effective birth control include one of the following (also refer to prescribing information):

  • Option 1: Copper IUD, levonorgestrel IUD, tubal sterilization, or progesterone implant.

  • Option 2: Oral estrogen/progestin contraceptive, transdermal estrogen/progesterone patch, vaginal ring, or progesterone injection, and use of a male condom, diaphragm with spermicide or cervical cap with spermicide.

  • Option 3: Diaphragm with spermicide or cervical cap with spermicide and use of a male condom.

  • Option 4: Partner’s vasectomy and use of a male condom, diaphragm with spermicide, cervical cap with spermicide, oral estrogen/progestin contraceptive, transdermal estrogen/progesterone patch, vaginal ring, or progesterone injection.

Pregnancy Considerations

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to sparsentan may cause fetal harm. Use is contraindicated in patients who are pregnant.

Breastfeeding Considerations

It is not known if sparsentan is present in breast milk.

Due to the potential for serious adverse reactions in the breastfed infant (including hypotension), breastfeeding is not recommended by the manufacturer.

Monitoring Parameters

Periodically monitor BP, serum creatinine, serum potassium, signs and symptoms of fluid retention or hepatotoxicity (eg, nausea, vomiting, right upper quadrant pain/tenderness, fatigue, anorexia, jaundice, dark urine, fever, itching).

ALT, AST, and bilirubin: Prior to treatment initiation (do not initiate treatment in patients with ALT or AST >3 times the ULN), monthly for the first 12 months after initiation or restarting after treatment interruption for aminotransferase elevations, and every 3 months thereafter.

Pregnancy testing (in patients who can become pregnant): A negative pregnancy test is required prior to treatment initiation, monthly during treatment, and 1 month after the last dose of sparsentan. Additional pregnancy testing is also recommended if menses is delayed or whenever pregnancy is suspected.

Mechanism of Action

Sparsentan is an endothelin type A receptor (ETAR) and angiotensin II type 1 receptor (AT1R) antagonist. Endothelin-1 and angiotensin II are thought to contribute to the pathogenesis of immunoglobulin A nephropathy (IgAN) via these receptors, and sparsentan has a high affinity for them, with a greater than 500-fold selectivity over the endothelin type B and angiotensin II subtype 2 receptors.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: Vdss: 61.4 L.

Protein binding: >99%.

Metabolism: Cytochrome P450 3A.

Half-life elimination: 9.6 hours.

Time to peak: ~3 hours (range: 2 to 8 hours).

Excretion: Feces: ~80% (9% as unchanged drug); Urine: 2%.

Clearance (steady state): 5.11 L/hour.

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  2. Cattran DC, Appel GB, Coppo R. IgA nephropathy: treatment and prognosis. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed December 13, 2023.
  3. Chapter 10: Immunoglobulin A nephropathy. Kidney Int Suppl (2011). 2012;2(2):209-217. doi:10.1038/kisup.2012.23 [PubMed 25018935]
  4. Filspari (sparsentan) [prescribing information]. San Diego, CA: Travere Therapeutics, Inc; September 2024.
  5. Heerspink HJL, Radhakrishnan J, Alpers CE, et al; PROTECT Investigators. Sparsentan in patients with IgA nephropathy: a prespecified interim analysis from a randomised, double-blind, active-controlled clinical trial. Lancet. 2023;401(10388):1584-1594. doi:10.1016/S0140-6736(23)00569-X [PubMed 37015244]
  6. Kidney Disease: Improving Global Outcomes (KDIGO) Glomerular Diseases Work Group. KDIGO 2021 clinical practice guideline for the management of glomerular diseases. Kidney Int. 2021;100(4S):S1-S276. doi:10.1016/j.kint.2021.05.021 [PubMed 34556256]
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  9. Palmer BF. Managing hyperkalemia caused by inhibitors of the renin-angiotensin-aldosterone system. N Engl J Med. 2004;351(6):585-592. doi:10.1056/NEJMra035279 [PubMed 15295051]
  10. Park IW, Sheen SS, Yoon D, et al. Onset time of hyperkalaemia after angiotensin receptor blocker initiation: when should we start serum potassium monitoring? J Clin Pharm Ther. 2014;39(1):61-68. doi:10.1111/jcpt.12109 [PubMed 24262001]
  11. Raebel MA. Hyperkalemia associated with use of angiotensin-converting enzyme inhibitors and angiotensin receptor blockers. Cardiovasc Ther. 2012;30(3):e156-e166. doi:10.1111/j.1755-5922.2010.00258.x [PubMed 21883995]
  12. Refer to manufacturer's labeling.
  13. Ryan MJ, Tuttle KR. Elevations in serum creatinine with RAAS blockade: why isn't it a sign of kidney injury? Curr Opin Nephrol Hypertens. 2008;17(5):443-449. doi:10.1097/MNH.0b013e32830a9606 [PubMed 18695383]
  14. Schoolwerth AC, Sica DA, Ballermann BJ, Wilcox CS; Council on the Kidney in Cardiovascular Disease and the Council for High Blood Pressure Research of the American Heart Association. Renal considerations in angiotensin converting enzyme inhibitor therapy: a statement for healthcare professionals from the Council on the Kidney in Cardiovascular Disease and the Council for High Blood Pressure Research of the American Heart Association. Circulation. 2001;104(16):1985-1991. doi:10.1161/hc4101.096153 [PubMed 11602506]
  15. Trachtman H, Nelson P, Adler S, et al; DUET Study Group. DUET: A phase 2 study evaluating the efficacy and safety of sparsentan in patients with FSGS. J Am Soc Nephrol. 2018;29(11):2745-2754. doi:10.1681/ASN.2018010091 [PubMed 30361325]
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