Luciseta tablets contain the active ingredient Sparsentan, a novel dual-acting receptor antagonist used for the treatment of certain rare kidney diseases associated with proteinuria.

Sparsentan works by simultaneously blocking the endothelin type A (ETA) receptor and the angiotensin II type 1 (AT1) receptor, both of which play a key role in kidney damage and protein leakage in urine.

Luciseta is an endothelin and angiotensin II receptor antagonist indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy (IgAN) at risk of rapid disease progression, generally a urine protein-to-creatinine ratio (UPCR) ≥1.5 g/g.

This indication is approved under accelerated approval based on reduction of proteinuria. It has not been established whether Luciseta slows kidney function decline in patients with IgAN. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory clinical trial.

Sparsentan is indicated for the treatment of the following:

• IgA nephropathy (IgAN) in patients at risk of rapid disease progression.
• Proteinuria associated with chronic kidney disease (as per clinical guidance).

This therapy helps reduce proteinuria and slow progression of kidney damage.

Sparsentan acts as a dual endothelin and angiotensin receptor antagonist.

It works by:

• Blocking endothelin-mediated vasoconstriction and inflammation.
• Inhibiting angiotensin II–mediated kidney damage.
• Reducing protein leakage in urine (proteinuria).
• Slowing progression of chronic kidney disease.

Clinical studies have shown significant reduction in proteinuria compared to standard therapies.

• Prior to initiating treatment with Luciseta, discontinue use of renin-angiotensin-aldosterone system (RAAS) inhibitors, endothelin receptor antagonists (ERAs), or aliskiren.

• Initiate treatment with Luciseta at 200 mg orally once daily. After 14 days, increase to the recommended dose of 400 mg once daily, as tolerated. When resuming treatment with Luciseta after an interruption, consider titration of Luciseta, starting at 200 mg once daily. After 14 days, increase to the recommended dose of 400 mg once daily.

• Taken once daily or as prescribed by a healthcare professional to swallow tablets whole with water prior to the morning or evening meal. Swallow whole with water; do not crush or chew.

• Follow the prescribed dosing schedule strictly.

Common side effects include:

• Hypotension
• Edema (fluid retention)
• Dizziness
• Elevated liver enzymes
• Hyperkalemia

Serious side effects may include liver toxicity and fluid overload.

Patients should inform their healthcare provider about all medications they are taking.

Sparsentan may interact with the following:

• ACE inhibitors and ARBs (avoid combined use)
• Strong CYP3A inhibitors or inducers
• Diuretics (may increase risk of hypotension)

These interactions may affect safety and effectiveness.

• Renin-Angiotensin System (RAS) inhibitors and ERAs: Contraindicated. Increased risk of hypotension and hyperkalemia.

• Strong CYP3A inhibitors: Avoid concomitant use. Increased sparsentan exposure.

• Moderate CYP3A inhibitors: Monitor adverse reactions. Increased sparsentan exposure.

• Strong CYP3A inducers: Avoid concomitant use. Decreased sparsentan exposure.

• Antacids: Avoid use within 2 hours before or after use of sparsentan. May decrease exposure to sparsentan.

• Acid-reducing agents: Avoid concomitant use. May decrease exposure to sparsentan.

• Nonsteroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase (COX-2) inhibitors: Monitor for signs of worsening renal function. Increased risk of kidney injury.

• CYP2B6, 2C9, and 2C19 substrates: Monitor for the efficacy of the concurrently administered substrates. Decreased exposure of these substrates.

• Sensitive P-gp and BCRP substrates: Avoid concomitant use. Increased exposure to substrates.

• Agents Increasing Serum Potassium: Increased risk of hyperkalemia; monitor serum potassium frequently.

• Store at 20°C–25°C (68°F–77°F)
• Keep in original packaging to protect from moisture.
• Keep out of reach of children.

• Regular monitoring of kidney function, liver enzymes, and potassium levels is recommended.
• Avoid use with other RAAS inhibitors unless advised.
• Monitor blood pressure regularly.
• Use effective contraception during treatment.
• Do not discontinue therapy without consulting your doctor.