tcsc1389 Lesinurad

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 µM, respectively.

IC50 & Target: Km: 0.85 µM (OAT1), 2 µM (OAT3)^[1]

In Vitro: Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is determined to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with K_m values of 0.85 and 2 µM, respectively^[1]. Lesinurad (RDEA594) is a URAT1 and OAT inhibitor, which increases proximal renal tubule urate excretion^[2]. Lesinurad (RDEA594) is a potential uric acid lowering agent througn inhibition of uric acid reuptake, and exhibits favorable p450 profiles, inhibits CYP2C9 and CYP2C8 with IC₅₀ of 14.4 μM and 16.2 μM, respectively. IC₅₀s of Lesinurad are all above 100 µM for CYP1A2, CYP2C19,and CYP2D6^[3].

In Vivo: Lesinurad (RDEA594) shows better pharmacokinetics than its pro-drug RDEA806. The 100 mg dose of Lesinurad exhibits a phamacological effect in the range of that produced by 300 mg to 800 mg single doses of RDEA806^[3].