verinurad (RDEA3170) / AstraZeneca 
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  • ||||||||||  verinurad (RDEA3170) / AstraZeneca, Zurampic (lesinurad) / AstraZeneca, probenecid / Generic mfg.
    Journal:  Virtual screening and biological evaluation of natural products as urate transporter 1 (URAT1) inhibitors. (Pubmed Central) -  Dec 4, 2025   
    The results showed that the carbonyl group on C-4 and hydroxyl group on C-7, C-4', and C-5' in flavonoids were conducive for URAT1 inhibitory effects. This study facilitates the application of flavonoids in the development of URAT1 inhibitors.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Journal:  Structural Basis for Inhibition of Urate Reabsorption in URAT1. (Pubmed Central) -  Mar 28, 2025   
    The three small molecules reside in the URAT1 central cavity with different binding modes, locking URAT1 in an inward-facing conformation. This study provides mechanistic insights into the drug modulation of URAT1 and sheds light on the rational design of potential URAT1-specific therapeutics for treating hyperuricemia.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Journal, Machine learning:  Crystal structure validation of verinurad via proton-detected ultra-fast MAS NMR and machine learning. (Pubmed Central) -  Sep 22, 2024   
    To do this, we take advantage of 1H resolution improvement at ultra-fast MAS and use solely 1H-detected experiments and machine learning methods to assign all the experimental proton and carbon chemical shifts. This framework provides a new tool for elucidating chemical information from crystalline samples with limited sample volume and yields remarkably faster acquisition times compared to 13C-detected experiments, without the need to employ dynamic nuclear polarization.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Journal:  Verinurad does not prolong QTc interval: A thorough QT study using concentration-QTc modelling. (Pubmed Central) -  Dec 13, 2022   
    P1
    In vivo, isobavachin exhibited powerful urate-lowering and uricosuric effects at 5-20 As the effect on ΔΔQTcF was below the threshold for regulatory concern (10 msec) at the supratherapeutic exposure, it can be concluded that verinurad and allopurinol treatment does not induce QTcF prolongation at the highest clinically relevant exposures.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Journal:  Considerations for Choosing First-Line Urate-Lowering Treatment in Older Patients with Comorbid Conditions. (Pubmed Central) -  Nov 28, 2022   
    The combination therapy of a novel uricosuric, verinurad, plus febuxostat reduced albuminuria in hyperuricemic patients with type 2 diabetes and CKD in a phase 2a trial, and further RCTs are awaited. Finally, the sodium-glucose cotransporter-2 inhibitor class of oral hypoglycemic agents, known to exert beneficial CV and renal effects independent of glycemic control, have shown a uricosuric effect and could be used as adjunctive therapy in older patients with cardiorenal comorbidities.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Urate Regulates Mitochondrial Function in a URAT1 Dependent Manner in Renal Epithelial Cells (Exhibit Hall, Orange County Convention Center, West Building) -  Oct 13, 2022 - Abstract #KIDNEYWEEK2022KIDNEY_WEEK_1857;    
    Both effects were abolished in the presence 0.5μM of verinurad. Conclusion We conclude that increased tubular urate alters intracellular lactate levels and mitochondrial function in a URAT1 dependent manner, providing mechanistic evidence that urate alters cell metabolism in the proximal tubule and may contribute to kidney disease progression.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Trial completion:  AMETHYST: Study of Verinurad in Heart Failure With Preserved Ejection Fraction (clinicaltrials.gov) -  Jun 1, 2022   
    P2,  N=159, Completed, 
    This study will assess the combined clinical effect of verinurad + allopurinol on kidney function in patients with CKD, hyperuricaemia and albuminuria, and whether this combination confers renoprotection beyond standard-of-care. Active, not recruiting --> Completed
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca, Zurampic (lesinurad) / AstraZeneca
    Characterization of the uric acid transporter URAT1 (SLC22A12) in platelets and megakaryocytes (Exhibition) -  May 13, 2022 - Abstract #ISTH2022ISTH_1045;    
    Cell fractionation experiments were consistent with flow cytometry results. Incubation of washed platelets with uric acid (50-100 µg/ml) did not induce spontaneous platelet aggregation, nor did it induce synergistic effects in the presence of low concentrations of classical platelet agonists.
  • ||||||||||  Journal:  What's new on the front-line of gout pharmacotherapy? (Pubmed Central) -  Feb 26, 2022   
    Novel uricosurics are a class for continued drug development; verinurad and arhalofenate are agents with future promise...Its immunogenicity significantly threatens the achievement of sustained urate lowering responses. Abrogating pegloticase's immunogenicity with immunomodulatory co-therapy may lend to sustained efficacy.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca, Urece (dotinurad) / Fuji Yakuhin, Mochida
    Review, Journal:  A historical journey of searching for uricosuric drugs. (Pubmed Central) -  Jan 6, 2022   
    Pharmacotherapeutically, a negative urate balance should be the aim of clinicians and then the rational choice of treatment with uricosurics seems quite logical and promising, but has not had a thorough attention of pharma, researchers nor of clinicians, though most gout patients were and still are low excretors. Here, an overview on the 70-year-old journey mankind has made in a search for uricosurics resulting so far in only 1 registered uricosuric per continent.
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Trial completion date, Trial primary completion date:  AMETHYST: Study of Verinurad in Heart Failure With Preserved Ejection Fraction (clinicaltrials.gov) -  Nov 15, 2021   
    P2,  N=159, Active, not recruiting, 
    Using in vitro systems recommended by regulatory agencies, we determined that, apart from verinurad being a substrate of OATP1B3, the potential for clinically relevant drug-drug interactions involving verinurad and its metabolites M1 and M8 as victims or perpetrators of metabolizing enzymes or drug transporters is considered low. Trial completion date: Nov 2022 --> Apr 2022 | Trial primary completion date: Nov 2022 --> Apr 2022
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Journal:  In Reply to "Verinurad/Febuxostat and Nephrotoxicity". (Pubmed Central) -  Sep 11, 2021   
    Dapagliflozin further reduced sUA without influencing uUA excretion, suggesting that its combination with verinurad and febuxostat at the doses tested does not adversely affect kidney function. No abstract available
  • ||||||||||  verinurad (RDEA3170) / AstraZeneca
    Enrollment change, Trial completion date, Trial initiation date, Trial suspension, Trial primary completion date:  A Study in Healthy Subjects to Assess Drug Availability of 4 Different Formulations of Verinurad and Allopurinol (clinicaltrials.gov) -  Nov 12, 2020   
    P1,  N=48, Suspended, 
    Active, not recruiting --> Completed N=15 --> 48 | Trial completion date: Dec 2020 --> Oct 2021 | Initiation date: Oct 2020 --> Jul 2021 | Not yet recruiting --> Suspended | Trial primary completion date: Dec 2020 --> Oct 2021