Zurampic (lesinurad) / AstraZeneca 
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 10 Diseases   0 Trials   0 Trials   273 News 


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  • ||||||||||  Zurampic (lesinurad) / AstraZeneca, Uriadec (topiroxostat) / Fuji Yakuhin, Suzuken
    Preclinical, Journal:  Evaluation of the inhibitory effects of antigout drugs on human carboxylesterases in vitro. (Pubmed Central) -  Jun 4, 2024   
    In silico docking showed that hydrogen bonds and hydrophobic interactions contributed to the intermolecular interactions of antigout drugs on CESs. Therefore, vigilant monitoring of potential drug-drug interactions (DDIs) is imperative when co-administering antigout drugs in clinical practice.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    Journal:  Proline-derived quinoline formamide compounds as human urate transporter 1 inhibitors with potent uric acid-lowering activities. (Pubmed Central) -  Apr 8, 2024   
    Structure-activity relationship studies reveal that the replacement of the carboxyl group on the polar fragment with trifluoromethanesulfonamide and substituent modification at the 6-position of the quinoline ring greatly improve URAT1 inhibitory activity compared with lesinurad...Notably, 21c also exhibits moderate anti-inflammatory activity related to the gout inflammatory pathway. Compounds 21c and 23a with superior druggability are potential candidates for the treatment of hyperuricemia and gout.
  • ||||||||||  AR882 / Arthrosi
    AR882, a Potent Uricosuric Agent, Shows Favorable Uric Acid Excretion Profile Following Multiple Doses (Poster Hall; in person) -  Sep 23, 2023 - Abstract #ACRConvergence2023ACR_Convergence_3228;    
    With its unique, slower elimination in PK, AR882 maintains a smooth intra-day uric acid excretion profile that was similar to baseline or to that in placebo patients, resulting in a lasting inhibitory effect without any high concentration of uric acid influx in the kidney tubules. The lack of daily transient increase in uric acid excretion confirms AR882, as a new uricosuric agent, possessing a favorable and safe renal profile over existing and other approved uricosuric agents.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    Journal:  Novel (sulfated) thyroid hormone transporters in the solute carrier 22 family. (Pubmed Central) -  Jun 16, 2023   
    Our results demonstrated that members of the OAT clade of the SLC22 family constitute a novel, evolutionary conserved group of transporters for (sulfated) iodothyronines. Future studies should reveal the relevance of these transporters in TH homeostasis and physiology.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    PK/PD data, Journal:  Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents. (Pubmed Central) -  Sep 21, 2022   
    Importantly, JNS4 displayed higher in vivo urate-lowering effects at doses of 1-4 mg/kg in a mouse model of hyperuricemia, as compared to BM and lesinurad...Moreover, JNS4 demonstrated benign toxicity profiles (no cytotoxicities against HepG2 and HK2 cells; no hepatic and renal toxicities observed in vivo). Collectively, these results suggest that JNS4 represents a novel, safe and selective URAT1 inhibitor with excellent druggabilities and is worthy of further investigation as an anti-hyperuricemic agent.
  • ||||||||||  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.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca, Krystexxa (pegloticase) / Horizon Therapeutics
    Clinical, Review, Journal:  Interventions for tophi in gout. (Pubmed Central) -  Sep 19, 2021   
    Lesinurad (400 mg or 200 mg) plus allopurinol is probably not beneficial for tophi resolution, and there was no difference in adverse events between these groups. RCTs on interventions for managing tophi in gout are needed, and the lack of trial data is surprising given that allopurinol is a well-established treatment for gout.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca, Krystexxa (pegloticase) / Horizon Therapeutics
    Review, Journal:  Changing paradigms in the management of gout. (Pubmed Central) -  Jul 30, 2021   
    Advances in understanding the physiology and genetic control of urate transport in the kidney and gut have led to novel, more selective uricosuric drugs, and basic research on mediators of urate crystal-induced inflammation has pointed to alternative therapeutic targets for treating and preventing gout flares. Current guidelines for the management of gout and indications for the use of some more recently introduced drugs; febuxostat, lesinurad, pegloticase and interleukin-1 antagonists are also briefly reviewed.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    Enrollment change, Trial completion date, Trial withdrawal, Trial primary completion date:  SATURATES: Post-Authorisation Safety Study of Lesinurad (clinicaltrials.gov) -  Apr 22, 2021   
    P=N/A,  N=0, Withdrawn, 
    Quantitative assay of the two drugs in Duzallo® tablet was successfully done and the data obtained was statistically compared with the results of another published HPLC quantitative analytical method. N=32800 --> 0 | Trial completion date: Sep 2021 --> Jun 2023 | Not yet recruiting --> Withdrawn | Trial primary completion date: Sep 2021 --> Jun 2023
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca, Krystexxa (pegloticase) / Horizon Therapeutics, Uriadec (topiroxostat) / Fuji Yakuhin, Medca Japan
    Retrospective data, Review, Journal:  Evaluation of urate-lowering therapy in hyperuricemia patients: a systematic review and Bayesian network meta-analysis of randomized controlled trials. (Pubmed Central) -  Feb 2, 2021   
    The new findings were as follows: (i) dual-agent ULTs were superior to febuxostat alone, and further surveillance on the adverse effects when lesinurad is uptitrated is needed, and (ii) terminalia bellerica 500 mg/day, a novel xanthine oxidase inhibitor (XOI) made of natural fruit extracts, and topiroxostat ≥ 80 mg/day, an XOI used mostly in Japan, could be new effective options for lowering the occurrence of adherence attrition events. Evidence from RCTs regarding second-line agents, such as probenecid and pegloticase, remains insufficient for clinical decision-making.Key Points• Dual-agent ULTs were superior to febuxostat alone, and further surveillance on the adverse-effects when lesinurad is uptitrated is needed.• Terminalia bellerica 500 mg/day, a novel xanthine oxidase inhibitor (XOI) made of natural fruit extracts, and topiroxostat 80 mg/day, an XOI used mostly in Japan, could be new effective options for lowering the occurrence of adherence attrition events.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    Review, Journal:  Therapeutic Strategies for the Treatment of Chronic Hyperuricemia: An Evidence-Based Update. (Pubmed Central) -  Jan 21, 2021   
    Xanthine oxidase inhibitors are the safest and most effective uric acid lowering drugs for the management of chronic hyperuricemia, while the efficacy of uricosuric agents is strongly modulated by pharmacogenetics. Emergent drugs (lesinurad, peglotidase) were found to be more effective for the acute management of refractory hyperuricemia, but their use is supported by a relatively small number of clinical trials so that further well-designed clinical research is needed to deepen their efficacy and safety profile.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    Journal:  Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability. (Pubmed Central) -  Jan 9, 2021   
    Lesinurad, a human urate transporter 1 (URAT1) inhibitor approved as a medication for the treatment of hyperuricemia associated with gout in 2015, can cause liver and renal toxicity...Furthermore, we also preliminarily explored the effect of chirality on the potency of the promising derivatives 44 and 54. Compounds 44, 54 and 83 showed favorable drug-like pharmacokinetics, and appear to be promising candidates for the treatment of hyperuricemia and gout.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca, Uriadec (topiroxostat) / Fuji Yakuhin, Sanwa Kagaku Kenkyusho
    Review, Journal:  Dotinurad: a novel selective urate reabsorption inhibitor as a future therapeutic option for hyperuricemia. (Pubmed Central) -  Nov 28, 2020   
    Of note, after the approval of lesinurad, which is a urate transporter-1 (URAT-1) inhibitor, in the United States in 2015, dotinurad (Fig. 1), a novel promising drug with selective UA reabsorption inhibitory property, was recently developed in Japan in 2018...A series of studies included in this supplemental review indicate that dotinurad reduces serum UA levels, and its efficacy and safety are similar to those of other UA-lowering agents currently used even in hyperuricemic patients with various clinical conditions. Moreover, two exploratory studies with a small sample size were conducted to compare PK parameters between patients with overproduction- and underexcretion-type hyperuricemia, and results showed that the effects of UA-lowering agents were comparable between the two subtype groups.Fig. 1Chemical structural formula of dotinurad.
  • ||||||||||  Triglide (fenofibrate) / Vectura, Shionogi
    Biomarker, Review, Journal:  Hypouricemia: what the practicing rheumatologist should know about this condition. (Pubmed Central) -  Nov 12, 2020   
    The rheumatologist is considered an expert in the metabolism of urate and its associated pathological conditions. Therefore, specialists must recognize hypouricemia as a biomarker of various pathological and potentially harmful conditions, highlighting the importance of conducting a deeper clinical investigation to reach a more accurate diagnosis and treatment.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    Preclinical, Journal:  Impact of Lesinurad and allopurinol on experimental Hyperuricemia in mice: biochemical, molecular and Immunohistochemical study. (Pubmed Central) -  Nov 7, 2020   
    Therefore, specialists must recognize hypouricemia as a biomarker of various pathological and potentially harmful conditions, highlighting the importance of conducting a deeper clinical investigation to reach a more accurate diagnosis and treatment. This study confirmed synergistic ameliorative hypouricemic impact of both lesinurad and allopurinol in the treatment of hyperuricemia in mice at the biochemical, molecular and cellular levels.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca, warfarin / Generic mfg.
    Clinical, PK/PD data, Journal:  Lesinurad: Evaluation of Pharmacokinetic and Pharmacodynamic Interactions With Warfarin in Healthy Volunteers. (Pubmed Central) -  Jul 16, 2020   
    Lesinurad had no meaningful clinical impact on anticoagulation activity as measured by prothrombin time, activated partial thromboplastin time, and international normalized ratio of prothrombin time and Factor VII clotting activity. Overall, the administration of warfarin in the presence of multiple-dose lesinurad was devoid of clinically significant drug-drug interaction.
  • ||||||||||  allopurinol / Generic mfg.
    Clinical, PK/PD data, Journal:  The effects of special patient population plasma on pharmacokinetic quantifications using LC-MS/MS. (Pubmed Central) -  May 19, 2020   
    Special population plasma did not affect quantitation of drugs with a wide range of plasma protein binding levels in human plasma. With the confirmation that there is no impact on quantification from the matrix, the bioanalytical method can be used to support the pharmacokinetic evaluations for clinical studies in special populations.
  • ||||||||||  Zurampic (lesinurad) / AstraZeneca
    PK/PD data, Journal:  Indirect pharmacodynamic models for responses with circadian removal. (Pubmed Central) -  May 9, 2020   
    The model was able to capture the chronobiology and pharmacodynamics of applicable drug responses, including the uricosuric effects of lesinurad in humans, suppression of the beta amyloid (Aβ) peptide by a gamma-secretase inhibitor in mouse brain, and the modulation of extracellular dopamine by a dopamine transporter inhibitor in rat brain. This type of model has a mechanistic basis and shows utility for capturing drug responses displaying nonstationary baselines controlled by removal mechanism(s).