Sipasentan, as the first non immunosuppressive therapy, provides a novel treatment option for IgAN patients.

1、 Drug name and main ingredients

1. Common name: Sparsentan

2. Product Name: FILSPARI ™

3. Dosage form: Oral film coated tablets

4. Main ingredients: Each tablet contains 200mg or 400mg of Sipasentan (in the form of dihydrochloride salt)

2、 Indications

1. IgA nephropathy (IgAN): Used to reduce proteinuria in adult patients with primary IgA nephropathy (urinary protein creatinine ratio ≥ 1.5g/g) and rapid disease progression risk.

2. Limitations: This indication is based on accelerated approval of proteinuria reduction and has not yet been proven to have a delaying effect on renal function decline.

3、 Specifications and characteristics

1. Specifications:

200mg tablets: White to off white oval shaped film coated tablets, with "105" engraved on one side.

400mg tablets: white to off white oval shaped film coated tablets, with "021" engraved on one side.

2. Packaging: 30 tablets per bottle, child safety bottle cap.

4、 Usage and dosage

1. Initial dose: 200mg once daily, taken on an empty stomach or with meals, whole tablet swallowed. Increase to 400mg once daily after 14 days.

2. Omission treatment: If missed for more than 6 hours, skip the dose; No need to take additional medication after vomiting.

3. Dose adjustment:

(1) Liver injury: Moderate (Child Pugh B) reduced to 200mg/day, severe (Child Pugh C) prohibited.

(2) Abnormal liver function: Discontinue treatment when ALT/AST>3 times the upper limit of normal (ULN), and titrate again from 200mg after recovery.

5、 Medication precautions

1. Monitoring requirements:

Monitor ALT/AST and bilirubin levels monthly before and during treatment (for the first 12 months), and every 3 months thereafter.

Women of childbearing age need to undergo monthly pregnancy testing.

2. Diet: Avoid high-fat meals (which may increase absorption) and avoid grapefruit juice.

3. Drug interactions:

(1) Prohibited combination therapy: angiotensin receptor blockers (ARBs), endothelin receptor antagonists (ERAs), and aliskiren.

(2) Be cautious when using in combination: Strong CYP3A inhibitors (such as itraconazole) should be discontinued with Sipasentan; NSAIDs may exacerbate kidney damage.

6、 Medication for special populations

1. Pregnant women: Absolute contraindication (animals showing teratogenicity).

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within one week after discontinuation of medication.

3. Children: Safety has not been established.

4. Elderly: No need to adjust dosage, but liver and kidney function needs to be monitored.

7、 Adverse reactions

1. Common (≥ 5%): peripheral edema (14%), hypotension (14%), dizziness (13%), hyperkalemia (13%), anemia (5%).

2. Severe but rare: hepatotoxicity (ALT/AST increase), acute renal injury, fluid retention.

8、 Contraindications

1. Pregnant or planned pregnant women.

2. Combination use of ARB, ERA, or Alikiren.

3. Severe liver injury (Child Pugh C).

9、 Drug interactions

1. CYP3A effects: Strong inhibitors increase the exposure to Sipasentan by 174%, while strong inducers reduce it by 47%.

2. P-gp/BCRP substrates: may increase the concentration of drugs such as digoxin, and should be avoided in combination.

3. Antacids: Take them every 2 hours to avoid reducing their effectiveness.

10、 Storage method

Store at room temperature (20-25 ° C) and keep the original bottle away from light and moisture.

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