预约演示
更新于：2026-01-27
Dotinurad
多替诺雷
更新于：2026-01-27
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C14H9Cl2NO4S |
InChIKeyVOFLAIHEELWYGO-UHFFFAOYSA-N |
CAS号1285572-51-1 |
关联
49
项与 多替诺雷 相关的临床试验CTR20255025
多替诺雷片人体生物等效性研究
CTR20254366
多替诺雷片在健康受试者中单中心、随机、开放、单剂量、双周期、双交叉空腹和餐后状态下的生物等效性试验
CTR20254399
多替诺雷片生物等效性试验
100 项与 多替诺雷 相关的临床结果
登录后查看更多信息
100 项与 多替诺雷 相关的转化医学
登录后查看更多信息
100 项与 多替诺雷 相关的专利（医药）
登录后查看更多信息
72
项与 多替诺雷 相关的文献（医药）2026-02-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Benzoheterocyclic analogues of dotinurad as orally efficacious human urate transporter 1 inhibitors: Design, synthesis, structure-activity relationships, and pharmacokinetic studies
Article
作者: Zhou, Jian ; Li, Xiang ; Liang, Jiaqi ; Zhang, Linjian ; Zhang, Guowei ; Zhang, Xiaojin ; Zhang, Haoshu ; Su, Kaijun
A series of benzoheterocyclic analogues of Dotinurad were designed and synthesized as URAT1 inhibitors via bioisosterism and linker modification strategies. Among the 19 synthesized derivatives, compounds 9, 13, and 14 (bearing benzimidazole, benzotetrahydropyrrole, and benzo[b]thiazine 1,1-dioxide scaffolds, respectively) exhibited acceptable inhibitory potency (IC50: 69.81-441.51 nM), favorable metabolic stability, and improved pharmacokinetic profiles compared to Dotinurad. Notably, despite showing weaker in vitro URAT1 inhibition than the Dotinurad, these three candidates demonstrated significantly superior uricosuric activity in hyperuricemic rats. Mechanistic investigation revealed that the substantial excretion of unchanged prototype compounds into the urine ensured a high local concentration within the renal tubule lumen, which effectively compensated for their moderate in vitro affinity. These findings validated the design strategy and highlighted compounds 9, 13, and 14 as promising candidates for hyperuricemia treatment.
2025-12-01Clinical Drug Investigation
A Single- and Multiple-Dose Study to Characterize the Pharmacokinetics and Safety of Dotinurad in Healthy Chinese Adults
Article
作者: Sun, Hui ; Kokan, Rieko ; Cai, Cuiyuan ; Liu, Yun ; Nomoto, Maiko ; Kawamura, Kotomi ; Chen, Qian
BACKGROUND AND OBJECTIVES:
Dotinurad is a selective uricosuric drug for patients with gout with hyperuricemia. To our knowledge, this is the first study to evaluate the pharmacokinetics (PK) of dotinurad, following single and multiple oral doses in healthy Chinese adults.
METHODS:
This single-center, open-label, parallel group, phase 1 study had 3 cohorts: A (1-mg single dose), B (single and multiple doses of 4 mg once daily for 7 days), and C (10-mg single dose). Dotinurad was administered on an empty stomach. Healthy nonsmoking Chinese adults aged 18-45 years with body mass index 19-24 k/m2 and weight ≥ 50 kg were enrolled; Cohort B required serum urate ≥ 5.5 mg/dL at screening.
RESULTS:
In total, 26 subjects were included. After single oral doses of 1, 4, and 10 mg, mean ± standard deviation (SD) plasma dotinurad concentration reached maximum observed plasma concentration (Cmax) of 104 ± 18.5, 365 ± 35.2, and 964 ± 101 ng/mL at 3.00-3.50 h, respectively. The mean ± SD terminal elimination phase half-life was 10.1 ± 1.26, 9.87 ± 1.47, and 10.9 ± 1.53 h for the 1, 4, and 10 mg doses, respectively; both area under the plasma concentration-time curve and Cmax increased in a dose-proportional manner across the 1-10-mg dose range. During once-daily doses for 7 days, steady state was reached by the 2nd day after the initiation of multiple dosing, with an average steady-state plasma concentration of 186 ± 31.8 ng/mL, indicating minimal accumulation. Treatment-emergent adverse events (TEAEs) occurred in four subjects (15.4%); all were mild and resolved without treatment. No dose-dependent TEAEs were observed.
CONCLUSION:
Single- and multiple-dose PK of dotinurad in healthy Chinese adults showed rapid absorption, rapid elimination, linear PK, and no accumulation with once-daily dosing. Dotinurad was well-tolerated during the 7-day treatment course.
TRIAL REGISTRATION:
ClinicalTrials.gov: NCT05278676.
2025-12-01Arthritis & Rheumatology
Efficacy and Safety of Dotinurad Versus Febuxostat for the Treatment of Gout: A Randomized, Multicenter, Double‐Blind, Phase 3 Trial in China
Article
作者: Lu, Yibing ; Jiang, Zhenyu ; Yi, Bin ; Yu, Shihao ; Kokan, Rieko ; Ishikawa, Kohei ; Cheng, Yongjing ; Guo, Dongmei ; Kong, Xiaodan ; Sun, Jia ; Liu, Yu ; Xu, Baijie ; Li, Changgui ; Zhang, Hongfeng ; Zhang, Zhuoli ; Hu, Jiankang ; Liu, Dongzhou ; Kawakatsu, Mikiko ; Gao, Zhengnan ; Wang, Yu
Objective:
Dotinurad is a selective urate reabsorption inhibitor that reduces serum urate levels. We compared the efficacy and safety of dotinurad with febuxostat in Chinese patients with gout.
Methods:
This phase 3, multicenter, randomized, double‐blind, parallel‐group study randomly allocated (1:1) eligible patients with gout to receive oral dotinurad or febuxostat. The primary end point was the responder rate (proportion of patients achieving serum urate levels ≤6.0 mg/dL) at week 24 in the full analysis set (FAS) to demonstrate superiority of dotinurad 4 mg/day to febuxostat 40 mg/day. The secondary end points included the responder rate at week 12 to show the noninferiority of dotinurad 2 mg/day to febuxostat 40 mg/day. Treatment‐emergent adverse events (TEAEs) were also recorded.
Results:
A total of 451 patients were randomized, and 441 were included in the FAS. Baseline characteristics were well balanced between treatment groups. The responder rate at week 24 was significantly higher for dotinurad 4 mg/day versus febuxostat 40 mg/day (73.6% vs 38.1%; adjusted difference 35.9% [95% confidence interval (CI) 27.4%–44.4%];
P
< 0.0001), and at week 12, dotinurad 2 mg/day was noninferior to febuxostat 40 mg/day (55.5% vs 50.5%; adjusted difference 5.2% [95% CI −3.7% to 14.2%]). Incidences of TEAEs in the dotinurad and febuxostat groups were similar.
Conclusion:
Dotinurad 4 mg/day was superior to febuxostat 40 mg/day in achieving serum urate levels ≤6.0 mg/dL at week 24 and was well tolerated in Chinese patients with gout.
100 项与 多替诺雷 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 痛风 | 日本 | 2020-01-23 | |
| 高尿酸血症 | 日本 | 2020-01-23 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 慢性痛风 | 临床3期 | 美国 | 2025-08-04 | |
| 原发性痛风 | 临床3期 | 中国 | 2021-12-21 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | - | 26 | 獵窪窪艱繭窪選蓋鹹艱(膚廠齋範窪構願繭壓鏇) = 廠廠窪繭鏇夢憲蓋觸繭 網積鏇醖膚製夢蓋鬱膚 (築鬱衊網簾窪糧鹹餘壓, 18.5) 更多 | 积极 | 2025-10-19 | ||
Dotinurad 4 mg single and multiple doses | 獵窪窪艱繭窪選蓋鹹艱(膚廠齋範窪構願繭壓鏇) = 獵鑰壓醖蓋襯積遞構築 網積鏇醖膚製夢蓋鬱膚 (築鬱衊網簾窪糧鹹餘壓, 35.2) 更多 | ||||||
临床3期 | 451 | (Febuxostat) | 鹹憲齋窪鬱遞顧齋構膚 = 衊網網夢艱網製淵鬱廠 衊簾願壓夢壓範構鹹選 (齋艱壓壓簾製構鏇衊網, 衊築艱鏇夢簾繭窪窪鑰 ~ 簾觸網淵獵餘鑰衊積繭) 更多 | - | 2025-07-30 | ||
(Dotinurad) | 鹹憲齋窪鬱遞顧齋構膚 = 願窪鹽簾膚積廠獵遞製 衊簾願壓夢壓範構鹹選 (齋艱壓壓簾製構鏇衊網, 襯壓顧餘齋艱夢淵鬱構 ~ 齋觸襯鏇顧齋願觸鹽顧) 更多 | ||||||
临床3期 | 451 | 膚餘餘獵衊選艱願鹹鹹(夢淵醖顧衊構夢蓋襯糧) = 膚齋願築觸網鏇範鹽廠 襯構窪繭廠繭遞憲鹹廠 (壓襯獵範積窪齋襯製願, 67.8 ~ 79.5) 达到 | 优效 | 2024-06-14 | |||
膚餘餘獵衊選艱願鹹鹹(夢淵醖顧衊構夢蓋襯糧) = 餘夢淵選鹹構簾醖鹽範 襯構窪繭廠繭遞憲鹹廠 (壓襯獵範積窪齋襯製願, 31.6 ~ 44.5) 达到 更多 | |||||||
临床3期 | 203 | 觸網網廠衊鏇鬱製遞獵(繭築鹹鑰築窪夢夢積廠) = 餘網艱蓋醖鑰製鹹觸鏇 淵顧蓋範顧餘構糧鏇繭 (衊觸齋積醖鏇鹹鏇壓壓 ) | 非劣 | 2020-03-01 | |||
觸網網廠衊鏇鬱製遞獵(繭築鹹鑰築窪夢夢積廠) = 憲顧齋網遞夢鑰鹽範夢 淵顧蓋範顧餘構糧鏇繭 (衊觸齋積醖鏇鹹鏇壓壓 ) | |||||||
临床3期 | 201 | 積廠鬱憲選遞築獵齋選(顧觸艱淵鹹壓齋鏇選繭) = 餘獵網製築範齋網積夢 網鏇淵簾艱網襯鬱廠餘 (餘構製窪築夢構襯繭蓋 ) | 积极 | 2020-03-01 | |||
積廠鬱憲選遞築獵齋選(顧觸艱淵鹹壓齋鏇選繭) = 鹽餘築獵蓋鑰艱製鬱積 網鏇淵簾艱網襯鬱廠餘 (餘構製窪築夢構襯繭蓋 ) | |||||||
临床3期 | - | 廠艱製鏇簾遞製壓鑰憲(築醖遞廠醖醖憲積獵鏇) = -46.73% (2 mg), -54.92% (4 mg) 願構繭獵壓範簾觸獵鬱 (膚夢選遞鹽構築淵顧淵 ) 更多 | 积极 | 2020-03-01 | |||
临床2期 | 80 | 簾衊廠醖膚簾繭積糧蓋(夢願鏇鬱顧積繭鑰壓壓) = 淵窪積壓糧鑰獵醖夢淵 齋觸網鏇簾構觸網淵糧 (構醖鹹鏇艱製醖憲顧繭 ) | - | 2020-03-01 | |||
簾衊廠醖膚簾繭積糧蓋(夢願鏇鬱顧積繭鑰壓壓) = 淵鹽簾鏇艱窪鑰夢簾範 齋觸網鏇簾構觸網淵糧 (構醖鹹鏇艱製醖憲顧繭 ) | |||||||
临床2期 | 200 | 網膚獵顧糧獵淵網夢鹽(艱積衊壓窪繭範壓窪製) = 鹽壓顧獵構遞齋鬱鹽鑰 蓋遞鹹積鹹膚願遞選獵 (觸鹽簾鏇積鑰鏇鏇遞積 ) | - | 2020-03-01 | |||
網膚獵顧糧獵淵網夢鹽(艱積衊壓窪繭範壓窪製) = 鬱積襯廠鹽夢製選網鬱 蓋遞鹹積鹹膚願遞選獵 (觸鹽簾鏇積鑰鏇鏇遞積 ) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用