lesinurad   Click here for help

GtoPdb Ligand ID: 7673

Synonyms: RDEA-594 | RDEA594 | Zurampic®
Approved drug
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].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 5
Topological polar surface area 92.79
Molecular weight 403
XLogP 5.93
No. Lipinski's rules broken 1
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Canonical SMILES OC(=O)CSc1nnc(n1c1ccc(c2c1cccc2)C1CC1)Br
Isomeric SMILES OC(=O)CSc1nnc(n1c1ccc(c2c1cccc2)C1CC1)Br
InChI InChI=1S/C17H14BrN3O2S/c18-16-19-20-17(24-9-15(22)23)21(16)14-8-7-11(10-5-6-10)12-3-1-2-4-13(12)14/h1-4,7-8,10H,5-6,9H2,(H,22,23)
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Summary of Clinical Use Click here for help
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 Click here for help
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.
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