Lesinurad sodium

Description: Lesinurad sodium (formerly known as RDEA594 sodium) is a novel, potent and selective inhibitor of URAT1 (urate transporter 1) and OAT (organic anion transporter), which is also called SURI (selective uric acid reabsorption inhibitor), is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 uM, respectively. It has potential usefulness to treat gout. Lesinurad interacted in vitro with OATP1B1, OCT1, and OAT1/3 transporters. Co-administration of lesinurad 200 mg did not significantly alter plasma exposure (maximum concentration C max and area under the concentration-time curve AUC) of total atorvastatin (atorvastatin + hydroxyl-metabolites) or atorvastatin, while co-administration of lesinurad 400 mg increased the C max of total atorvastatin and atorvastatin by 17-26 %, but had no effect on AUC. Co-administration of lesinurad 400 mg had no effect on the plasma exposure of metformin. Furosemide plasma AUC was reduced by 31 % in the presence of lesinurad 400 mg, but furosemide renal clearance and diuretic activity were unchanged.

References: Ther Adv Musculoskelet Dis. 2016 Aug; 8(4):145-59; Clin Drug Investig. 2016 Jun; 36(6):443-52. 2008 ACR/ARHP Annual Scientific Meeting, 24-29 October 2008, USA.