ArticleScientific reports2017
Discovery and characterization of verinurad, a potent and specific inhibitor of URAT1 for the treatment of hyperuricemia and gout.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers, 1 of them a synthesis that pooled it.
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The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
45 citing papers in PubMed, 1 synthesis or guideline pooled it, 112 citations in OpenAlex.
- Impact of lifestyle factors and dietary patterns on serum uric acid levels and disease activity in gout: a systematic review.Journal of health, population, and nutrition · 2025Pooled it
- 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
- Pharmacokinetics, Pharmacodynamics, and Tolerability of Concomitant Administration of Verinurad and Febuxostat in Healthy Male Volunteers.Clinical pharmacology in drug development · 2019Trial
- Pharmacokinetics, Pharmacodynamics, and Tolerability of Concomitant Multiple Dose Administration of Verinurad (RDEA3170) and Allopurinol in Adult Male Subjects With Gout.Journal of clinical pharmacology · 2018Trial
- Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study.Rheumatology (Oxford, England) · 2018Trial
- URAT1 and GLUT9 as drug targets in gout: progress in transporter-directed therapies and delivery technologies.Inflammopharmacology · 2025Review
- Molecular mechanism of drug inhibition of URAT1.Nature communications · 2025Article
- Understanding Renal Tubular Function: Key Mechanisms, Clinical Relevance, and Comprehensive Urine Assessment.Pathophysiology : the official journal of the International Society for Pathophysiology · 2025Review
- Article
- Mechanisms of urate transport and uricosuric drugs inhibition in human URAT1.Nature communications · 2025Article
- Overview of pharmacodynamical research of traditional Chinese medicine on hyperuricemic nephropathy: from the perspective of dual-regulatory effect on the intestines and kidneys.Frontiers in pharmacology · 2025Review
- From Patents to Progress: Unraveling Gout's Journey Through Clinical Trials and Advancements.Reviews on recent clinical trials · 2025Review
- Looping forward: exploring R-loop processing and therapeutic potential.FEBS letters · 2025Review
- Investigating the Role of Food-Derived Peptides in Hyperuricemia: From Mechanisms of Action to Structural Effects.Foods (Basel, Switzerland) · 2024Review
- Transport mechanism and structural pharmacology of human urate transporter URAT1.Cell research · 2024Article
- A System for Discovering Novel Uricosurics Targeting Urate Transporter 1 Based on In Vitro and In Vivo Modeling.Pharmaceutics · 2024Article
- Emerging Urate-Lowering Drugs and Pharmacologic Treatment Strategies for Gout: A Narrative Review.Drugs · 2023Review
- Investigation of the Inhibition Mechanism of Xanthine Oxidoreductase by Oxipurinol: A Computational Study.Journal of chemical information and modeling · 2023Article
- Virtual screening and activity evaluation of human uric acid transporter 1 (hURAT1) inhibitors.RSC advances · 2023Article
- TCM and related active compounds in the treatment of gout: the regulation of signaling pathway and urate transporter.Frontiers in pharmacology · 2023Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gout is caused by elevated serum urate levels, which can be treated using inhibitors of the uric acid transporter, URAT1. Here, we characterize verinurad (RDEA3170), which is currently under evaluation for gout therapy. Verinurad specifically inhibits URAT1 with a potency of 25 nM. High affinity inhibition of uric acid transport requires URAT1 residues Cys-32, Ser-35, Phe-365 and Ile-481. Unlike other available uricosuric agents, the requirement for Cys-32 is unique to verinurad. Two of these residues, Ser-35 and Phe-365, are also important for urate transport kinetics. A URAT1 binding assay using radiolabeled verinurad revealed that distinct URAT1 inhibitors benzbromarone, sulfinpyrazone and probenecid all inhibit verinurad binding via a competitive mechanism. However, mutations made within the predicted transporter substrate channel differentially altered the potency for individual URAT1 inhibitors. Overall, our results suggest that URAT1 inhibitors bind to a common site in the core of the transporter and sterically hinder the transit of uric acid through the substrate channel, albeit with vastly different potencies and with differential interactions with specific URAT1 amino acids.
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