司帕生坦(Sparsentan)中文说明书:适应症、用法用量、剂量调整、不良反应、注意事项

Sparsentan, developed by Travere Therapeutics, acts as a dual-receptor antagonist by simultaneously blocking endothelin type A (ETA) and angiotensin I. Type I1 (AT1) receptors significantly reduce proteinuria. The drug received accelerated approval from the FDA for the treatment of IgA nephropathy in 2023 and was upgraded to full approval in 2024. It became the first targeted therapy drug approved to delay the deterioration of renal function in adult patients with primary IgA nephropathy.

Sparsentan Indications

IgA Nephropathy

Sparsentan is indicated for slowing the decline in renal function in adults with primary immunoglobulin A nephropathy (IgAN) who are at risk for disease progression.

Sparsentan usage and dosage

1. Recommended dose

The initial dose of Sparsentan is 200 mg, once a day for 14 days. After 14 days, depending on tolerance, it can be increased to 400 mg once a day.

When resuming sparsentan after an interruption, consider dose titration, starting with 200 mg once daily; after 14 days, increase to 400 mg once daily.

2. Dose adjustment

If patients receiving sparsentan experience an increase in AST or ALT, please adjust monitoring and treatment. Do not resume sparsentan in patients who develop clinical signs of hepatotoxicity or whose liver enzyme and bilirubin levels have not returned to baseline.

Due to limited space, please refer to the original instructions of the drug for details. Please follow the guidance of your doctor for specific medication.

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Adverse reactions of Sparsentan

Common adverse reactions (≥5%)

Common adverse reactions of Sparsentan are peripheral edema, hypotension (including orthostatic hypotension), dizziness, hyperkalemia, anemia, and acute kidney injury.

Due to limited space, please refer to the original instructions of the drug for details. Please follow the guidance of your doctor for specific medication.

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Sparsentan (Sparsentan) Precautions

1. Hepatotoxicity

Sparsentan has reports on hepatotoxicity. Monitor AST, ALT, and total bilirubin before starting sparsentan, monthly during the first year of treatment, and every 3 months thereafter.

2. Fetal/neonatal morbidity and mortality

Based on animal findings, it may cause harm to the fetus and is contraindicated by pregnant women. Perform a pregnancy test before starting sparsentan, once monthly during treatment, and 1 month after stopping sparsentan. Advise females of childbearing potential to use effective contraception before starting sparsentan, during treatment, and for 1 month after discontinuing sparsentan. Inform patients of the potential fetal harm when using sparsentan during pregnancy.

3. Hypotension

There have been reports of hypotension with Sparsentan. Consider eliminating or adjusting other antihypertensive medications and maintaining appropriate volume status in patients at risk for hypotension. If hypotension persists despite elimination or reduction of other antihypertensive medications, consider reducing or interrupting the sparsentan dose. Sparsentan can be resumed after blood pressure stabilizes.

4. Acute kidney injury

Acute kidney injury can occur; patients whose renal function depends in part on the activity of the renin-angiotensin system (e.g., patients with renal artery stenosis, chronic kidney disease, severe congestive heart failure, or volume depletion) may be at increased risk. Monitor kidney function regularly. Consider withholding or discontinuing sparsentan in patients who develop clinically significant decreases in renal function.

5. Hyperkalemia

Patients with end-stage renal disease or those taking potassium-increasing agents (such as potassium supplements, potassium-sparing diuretics, potassium-containing salt substitutes) at increased risk. Monitor serum potassium regularly and treat appropriately. If hyperkalemia occurs, consider reducing the dose or discontinuing sparsentan.

6. Body fluid retention

Fluid retention was reported. Sparsentan has not been studied in patients with heart failure. If clinically significant fluid retention occurs, the underlying cause should be determined and the need for initiation or change of diuretic therapy, and a dose adjustment of sparsentan should be considered.