Sparsentan CAS# 254740-64-2 4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺

Sparsentan, also known as RE-021, PS433540 and DARA-a, is a dual angiotensin II and endothelin A receptor antagonist. Sparsentan has demonstrated potent antagonism of ETA and AT1 receptors with Ki values in the low nanomolar range (ETA: ~0.8 nM; AT1: ~9 nM), resulting in effective blockade of vasoconstrictive and pro-fibrotic signaling pathways. This dual mechanism leads to reductions in proteinuria and stabilization of renal function, as evidenced in the DUET and PROTECT trials. Pharmacodynamically, sparsentan reduces blood pressure and proteinuria more effectively than angiotensin receptor blockers alone, supporting its superior therapeutic potential in progressive glomerular diseases.