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Synonyms: RDEA-594 | RDEA594 | Zurampic®
lesinurad is an approved drug (FDA (2015), EMA (2016))
Compound class: Synthetic organic
Comment: Lesinurad is an orally available inhibitor of URAT1, the renal transporter that regulates uric acid excretion from the body [1-2].
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.
|Summary of Clinical Use
|Following the completion of successful Phase 3 clinical trials, the US FDA approved lesinurad as a treatment for the hyperuricaemia which causes the symptoms of gout in December 2015. The EMA followed with approval in April 2016.
Click here to view ClinicalTrials.gov's list of current lesinurad trials.
A fixed dose combination of lesinurad and the xanthine dehydrogenase inhibitor allopurinol (Duzallo®) was FDA and EMA approved in 2017 and 2018 respectively, for the treatment of gout that is not controlled by allopurinol alone.
|Mechanism Of Action and Pharmacodynamic Effects
|Lesinurad inhibits the uric acid transporter URAT1 which is expressed in the proximal tubule of the kidney. This reduces re-absorption of uric acid, thereby promoting its renal excretion.
For extended ADME data see the following:
European Medicines Agency (EMA)