Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is found to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 µM, respectively [1]. Lesinurad (RDEA594) functions as a URAT1 and OAT inhibitor, leading to increased proximal renal tubule urate excretion [2]. Lesinurad (RDEA594) serves as a potential uric acid-lowering agent by inhibiting uric acid reuptake. It also demonstrates favorable p450 profiles, inhibiting CYP2C9 and CYP2C8 with IC50 values of 14.4 μM and 16.2 μM, respectively. IC50 values for Lesinurad exceed 100 µM for CYP1A2, CYP2C19, and CYP2D6 [3].
体内研究
Lesinurad (RDEA594) exhibits superior pharmacokinetics compared to its pro-drug RDEA806. A 100 mg dose of Lesinurad produces a pharmacological effect comparable to that of single doses of RDEA806 ranging from 300 mg to 800 mg [3].
体外研究
Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is found to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 µM, respectively [1].
Lesinurad (RDEA594) functions as a URAT1 and OAT inhibitor, leading to increased proximal renal tubule urate excretion [2].
Lesinurad (RDEA594) serves as a potential uric acid-lowering agent by inhibiting uric acid reuptake. It also demonstrates favorable p450 profiles, inhibiting CYP2C9 and CYP2C8 with IC50 values of 14.4 μM and 16.2 μM, respectively. IC50 values for Lesinurad exceed 100 µM for CYP1A2, CYP2C19, and CYP2D6 [3].
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