"目錄號(hào): HY-15258A
Membrane Transporter/Ion Channel-
Lesinurad sodium (RDEA594 sodium)是URAT1抑制劑。
相關(guān)產(chǎn)品
生物活性
Description
Lesinurad sodium is aURAT1andOATinhibitor, is determined to be a substrate for the kidney transportersOAT1andOAT3withKmvalues 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 Kmvalues 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 IC50of 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].
Clinical Trial
Ardea Biosciences, Inc.
Healthy
January 2014
Phase 1
Ardea Biosciences, Inc.
Healthy
April 2014
Phase 1
Ardea Biosciences, Inc.
Healthy
July 2013
Phase 1
Ardea Biosciences, Inc.
Healthy
November 2013
Phase 1
Ironwood Pharmaceuticals, Inc.-Medpace, Inc.
Gout-Chronic Kidney Disease (CKD)
July 19, 2017
Phase 4
Ardea Biosciences, Inc.
Gout
February 2013
Phase 3
Ardea Biosciences, Inc.
Gout
March 2013
Phase 3
Ardea Biosciences, Inc.
Gout
August 2012
Phase 3
Ardea Biosciences, Inc.
Gout
January 2012
Phase 3
Ardea Biosciences, Inc.
Healthy
August 30, 2016
Phase 1
Ardea Biosciences, Inc.
Healthy
November 2013
Phase 1
Ardea Biosciences, Inc.
Gout
December 2011
Phase 3
Ardea Biosciences, Inc.
Tophaceous Gout
January 2012
Phase 3
Ardea Biosciences, Inc.
Gout
June 2013
Phase 1
Ardea Biosciences, Inc.
Healthy
October 2015
Phase 1
Ardea Biosciences, Inc.
Gout
December 2012
Phase 1
Ardea Biosciences, Inc.
Gout
January 2012
Phase 3
Ardea Biosciences, Inc.
Healthy
October 2013
Phase 1
Ardea Biosciences, Inc.
Gout
October 2009
Phase 2
Ardea Biosciences, Inc.
Hyperuricemia
July 2009
Phase 2
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References
