ArticleArthritis research & therapy2016
Lesinurad, a novel, oral compound for gout, acts to decrease serum uric acid through inhibition of urate transporters in the kidney.
Article in Arthritis research & therapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 61 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
61 citing papers in PubMed, 1 synthesis or guideline pooled it, 124 citations in OpenAlex.
- Efficacy and tolerability ofPharmaceutical biology · 2020Pooled it
- Impact of Renal Impairment on the Pharmacodynamic and Pharmacokinetic Profiles of Epaminurad, a Novel Uric Acid Transporter 1 Inhibitor.Clinical and translational science · 2025Trial
- Effect of Intensive Urate Lowering With Combined Verinurad and Febuxostat on Albuminuria in Patients With Type 2 Diabetes: A Randomized Trial.American journal of kidney diseases : the official journal of the National Kidney Foundation · 2021Trial
- Dotinurad versus benzbromarone in Japanese hyperuricemic patient with or without gout: a randomized, double-blind, parallel-group, phase 3 study.Clinical and experimental nephrology · 2020Trial
- Efficacy and safety during extended treatment of lesinurad in combination with febuxostat in patients with tophaceous gout: CRYSTAL extension study.Arthritis research & therapy · 2019Trial
- A Dose-Escalation Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of HP501 in Male Chinese Gout Patients with Hyperuricemia.Clinical pharmacology in drug development · 2026Article
- ABCG2 transporter: Structural and functional associations with gout (Review).International journal of molecular medicine · 2026Review
- Ginger and Its Purified Major Components Inhibit Clinically Relevant Uptake and Efflux Transporters In Vitro.Pharmaceutics · 2026Article
- Advances in Understanding the Mechanisms of Treatment for Gouty Arthritis: A Comprehensive Review.Physiological research · 2025Review
- Molecular mechanism of drug inhibition of URAT1.Nature communications · 2025Article
- Simultaneous determination of lesinurad and co-administered drugs used in management of gout comorbidities to uncover potential pharmacokinetic interaction in rat plasma.Scientific reports · 2025Article
- Drug-Induced Hypouricemia.Drug safety · 2025Review
- Hyperuricemia-induced complications: dysfunctional macrophages serve as a potential bridge.Frontiers in immunology · 2025Review
- Case report: Gouty renal abscess and gouty sacroiliitis associated with genetic variants of a young woman.Frontiers in medicine · 2025Article
- Transport mechanism and structural pharmacology of human urate transporter URAT1.Cell research · 2024Article
- In vivo study of newly developed albumin-conjugated urate oxidase for gout treatment.Arthritis research & therapy · 2023Article
- Emerging Urate-Lowering Drugs and Pharmacologic Treatment Strategies for Gout: A Narrative Review.Drugs · 2023Review
- Novel (sulfated) thyroid hormone transporters in the solute carrier 22 family.European thyroid journal · 2023Article
- Investigation of the Inhibition Mechanism of Xanthine Oxidoreductase by Oxipurinol: A Computational Study.Journal of chemical information and modeling · 2023Article
- Insoluble Fiber in Barley Leaf Attenuates Hyperuricemic Nephropathy by Modulating Gut Microbiota and Short-Chain Fatty Acids.Foods (Basel, Switzerland) · 2022Article
1 more citing papers are in PubMed but not listed here.
Corrections and comments
- Erratum issued
Authors and funding
13 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundExcess body burden of uric acid promotes gout. Diminished renal clearance of uric acid causes hyperuricemia in most patients with gout, and the renal urate transporter (URAT)1 is important for regulation of serum uric acid (sUA) levels. The URAT1 inhibitors probenecid and benzbromarone are used as gout therapies; however, their use is limited by drug-drug interactions and off-target toxicity, respectively. Here, we define the mechanism of action of lesinurad (Zurampic®; RDEA594), a novel URAT1 inhibitor, recently approved in the USA and Europe for treatment of chronic gout.
methodssUA levels, fractional excretion of uric acid (FE
resultsAfter 6 hours, a single 200-mg dose of lesinurad elevated FE
conclusionThe pharmacodynamic effects and in vitro activity of lesinurad are consistent with inhibition of URAT1 and OAT4, major apical transporters for uric acid. Lesinurad also has a favorable selectivity and safety profile, consistent with an important role in sUA-lowering therapy for patients with gout.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.