Otani N, Ouchi M, Mizuta E, Morita A, Fujita T, Anzai N, et al. Dysuricemia-a new concept encompassing hyperuricemia and hypouricemia. Biomedicines. 2023;11:1255.
Article CAS PubMed PubMed Central Google Scholar
Dalbeth N, Gosling AL, Gaffo A, Abhishek A. Gout. Lancet. 2021;397:1843–55.
Article CAS PubMed Google Scholar
Sun L, Zhang M, Zhao JX, Chen W, Wang G, The human gut microbiota and uric acid metabolism: genes, metabolites, and diet. Crit Rev Food Sci Nutr. 2025: 1-21.
Song D, Zhao X, Wang F, Wang G. A brief review of urate transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia and gout: current therapeutic options and potential applications. Eur J Pharm. 2021;907:174291.
Sun ZQ, Zhang XW, Zhao ZA, Li X, Pang J, Chen J. Recent progress and future perspectives on anti-hyperuricemic agents. J Med Chem. 2024;67:19966–87.
Article CAS PubMed Google Scholar
Du L, Zong Y, Li HR, Wang Q, Xie L, Yang B, et al. Hyperuricemia and its related diseases: mechanisms and advances in therapy. Signal Transduct Target Ther. 2024;9:212.
Article CAS PubMed PubMed Central Google Scholar
Perez-Ruiz F, Dalbeth N. Combination urate-lowering therapy in the treatment of gout: What is the evidence?. Semin Arthritis Rheum. 2019;48:658–68.
Article CAS PubMed Google Scholar
Shi XY, Zhao T, da Silva-Júnior EF, Zhang J, Xu S, Gao S, et al. Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2020-present). Expert Opin Ther Pat. 2022;32:1175–84.
Article CAS PubMed Google Scholar
Dalbeth N, Jones G, Terkeltaub R, Khanna D, Kopicko J, Bhakta N, et al. Lesinurad, a selective uric acid reabsorption inhibitor, in combination with febuxostat in patients with tophaceous gout: findings of a phase III clinical trial. Arthritis Rheumatol. 2017;69:1903–13.
Article CAS PubMed PubMed Central Google Scholar
Presa M, Pérez-Ruiz F, Oyagüez I. Second-line treatment with lesinurad and allopurinol versus febuxostat for management of hyperuricemia: a cost-effectiveness analysis for Spanish patients. Clin Rheumatol. 2019;38:3521–8.
Xue X, Sun M, Yan F, Dalbeth N, He Y, Li X, et al. Superiority of low-dose benzbromarone add-on to low-dose febuxostat compared with febuxostat monotherapy in gout with combined-type hyperuricemia. Arthritis Care Res(Hoboken). 2024;76:703–11.
Article CAS PubMed Google Scholar
Terkeltaub R, Lee J, Min J, Shin S, Saag KG. Serum urate-lowering efficacy and safety of tigulixostat in gout patients with hyperuricemia: a randomized, double-blind, placebo-controlled, dose-finding trial. Arthritis Rheumatol. 2023;75:1275–84.
Article CAS PubMed Google Scholar
Otani N, Ouchi M, Kudo H, Tsuruoka S, Hisatome I, Anzai N. Recent approaches to gout drug discovery: an update. Expert Opin Drug Discov. 2020;15:943–54.
Article CAS PubMed Google Scholar
Warrell RP, Klukovits A, Barnes K, Satyanarayana C, Cheeseman C, Piwinski P, et al. Profound hypouricemia induced in human subjects by novel bifunctional inhibitors of xanthine oxidase and URAT1. Arthritis Rheum. 2014;66:S366–S366.
Tonghua Dongbao Pharmaceuticals Completion of Phase IIa Clinical Trial Summary Report for Gout Dual-Target Inhibitor (THDBH151 Tablets) [Online]. Changchun, China: Tonghua Dongbao Pharmaceuticals; 2024. http://www.thdb.com/companynews-show-505.html (accessed July 1, 2024).
Zhu XY, Yang C, Zhang L, Jing L. Identification of novel dual inhibitors targeting XOR and URAT1 via multiple virtual screening methods. J Mol Struct. 2022;1256:132567.
Zhu XY, Chen HM, Zhang L, Qin YX, Li J. Design, synthesis, and evaluation of the in vitro activity of novel dual inhibitors of XOR and URAT1 containing a benzoic acid group. Chem Biol Drug Des. 2023;102:1553–67.
Article CAS PubMed Google Scholar
Jhoti H, Williams G, Rees DC, Murray CW. The ‘rule of three’ for fragment-based drug discovery: where are we now?. Nat Rev Drug Discov. 2013;12:644–5.
Article CAS PubMed Google Scholar
Storer RI, Owen RM, Pike A, Benn CL, Armstrong E, Blakemore DC, et al. The discovery and evaluation of diaryl ether heterocyclic sulfonamides as URAT1 inhibitors for the treatment of gout. Medchemcomm. 2016;7:1587–95.
Cai WQ, Wu JW, Liu W, Xie Y, Liu Y, Zhang S, et al. Systematic Structure-Activity Relationship (SAR) exploration of diarylmethane backbone and discovery of a highly potent novel Uric Acid Transporter 1 (URAT1) inhibitor. Molecules. 2018;23:252.
Article PubMed PubMed Central Google Scholar
Tian H, Liu W, Zhou Z, Shang Q, Liu Y, Xie Y, et al. Discovery of a flexible triazolylbutanoic acid as a highly potent Uric Acid Transporter 1 (URAT1) inhibitor. Molecules. 2016;21:1543.
Article PubMed PubMed Central Google Scholar
Yang XT, Pang XH, Fan L, Li X, Chen Y. Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors. Bioorg Med Chem Lett. 2017;27:1919–22.
Article CAS PubMed Google Scholar
Wu JW, Yin L, Liu YQ, Zhang H, Xie YF, Wang RL, et al. Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout. Bioorg Med Chem Lett. 2019;29:383–8.
Article CAS PubMed Google Scholar
Peng JB, Hu QY, Gu CY, Liu B, Jin F, Yuan J, et al. Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model. Bioorg Med Chem Lett. 2016;26:277–82.
Article CAS PubMed Google Scholar
Li J, Wu FP, Liu XG, Zou Y, Chen H, Li Z. Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors. Eur J Med Chem. 2017;10:20–30.
Zhou HY, Zhong GR, Bai J, Li X, Peng W, Zhang L, et al. Development of a fluorescence-based assay for screening of urate transporter 1 inhibitors using 6-carboxyfluorescein. Anal Biochem. 2021;626:114246.
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