非布司他(Febuxostat) - 药物靶点：XO_在研适应症：痛风性关节炎，慢性高尿酸血症，痛风_专利_临床

概要

基本信息

药物类型

小分子化药

别名

2-(3-cyano-4-isobutoxyphenyl)-4-methyl- 1,3-thiazole-5-carboxylic acid、Adenuric、Febuxostat (JAN/USAN/INN)

+ [23]

靶点

XO

作用方式

抑制剂

作用机制

XO抑制剂(黄嘌呤脱氢酶抑制剂)

治疗领域

免疫系统疾病遗传病与畸形内分泌与代谢疾病+ [2]

在研适应症

痛风性关节炎慢性高尿酸血症痛风+ [1]

非在研适应症

稳定型心绞痛脑梗塞心血管畸形+ [10]

原研机构

Teijin Pharma Ltd.

在研机构

Viatris Ltd. (New Zealand)

江苏恒瑞医药股份有限公司

Takeda Pharmaceutical Co., Ltd.

+ [8]

非在研机构

Menarini International Operations Luxembourg SA

安斯泰来制药（中国）有限公司

权益机构-

最高研发阶段批准上市

首次获批日期

欧盟 (2008-04-21),

高尿酸血症

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C16H16N2O3S

InChIKeyBQSJTQLCZDPROO-UHFFFAOYSA-N

CAS号144060-53-7

关联

302

项与非布司他相关的临床试验

CTR20252504

/ Active, not recruiting临床1期

HR091506片不同批次制剂在健康受试者中单次给药的药代动力学对比研究

1.评价HR091506片不同批次制剂在健康受试者中单次给药的药代动力学特征。2.评价给药后的安全性。

开始日期2025-07-10

申办/合作机构

江苏恒瑞医药股份有限公司

TCTR20250425001

/ Not yet recruiting临床1期

A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Febuxostat 80 mg Film-coated Tablets and Reference Product (Feburic) in Healthy Thai Volunteers under Fasting Conditions

开始日期2025-07-07

申办/合作机构-

TCTR20241122011

/ Not yet recruiting临床1期

A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Febuxostat 80 mg Film-coated Tablets (INNOXOSTAT) and Reference Product (Feburic 80 mg) in Healthy Thai Volunteers under Fasting Conditions

开始日期2025-07-01

申办/合作机构-

100 项与非布司他相关的临床结果

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100 项与非布司他相关的转化医学

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100 项与非布司他相关的专利（医药）

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2,308

项与非布司他相关的文献（医药）

2025-12-31·RENAL FAILURE

Comparative efficacy and safety of febuxostat and allopurinol in chronic kidney disease stage 3–5 patients with asymptomatic hyperuricemia: a network meta-analysis

Review

作者: Chen, Lu ; Zhang, Yanyun ; Wang, Yinglin ; Chen, Jiaojiao

OBJECTIVE:

This study evaluates and compares the effectiveness and safety of febuxostat and allopurinol in chronic kidney disease (CKD) stages 3-5 patients with asymptomatic hyperuricemia using a network meta-analysis.

METHODS:

A systematic review and network meta-analysis were conducted, adhering to PRISMA-NMA guidelines. Searches included PubMed, Embase, Cochrane Library, and Chinese databases up to June 2024. Randomized controlled trials (RCTs) and cohort studies were assessed for methodological rigor using GRADE.

RESULTS:

A total of 12 RCTs and 4 cohort studies (n = 2,423 participants) were included. Febuxostat was associated with greater improvements in estimated glomerular filtration rate compared to allopurinol (MD, 4.99 mL/min/1.73 m²; 95%CI -0.65 to 10.78; certainty: low) and placebo (MD, 4.72 mL/min/1.73 m²; 95%CI 0.67 to 8.82; low). Serum uric acid reduction was also more pronounced with febuxostat (MD, -0.61 mg/dL; 95%CI -1.15 to -0.05; moderate). Safety outcomes, including major cardiovascular events and adverse events, showed no significant differences between febuxostat and allopurinol. Subgroup analyses revealed enhanced effectiveness of febuxostat at six months of treatment.

CONCLUSIONS:

This analysis provides robust evidence that febuxostat might offers greater improvements in kidney function and uric acid levels compared to allopurinol or placebo in asymptomatic hyperuricemia with CKD stage 3-5 patients, without compromising safety. These findings can guide clinical decision-making and treatment optimization.

2025-10-01·BIOCHEMICAL PHARMACOLOGY

Novel aryl hydrocarbon receptor agonists as potential anti-inflammatory therapeutics: Identification and validation through drug repurposing

Article

作者: Künze, Georg ; Geisslinger, Gerd ; Buchholz, Mirko ; Köhl, Ulrike ; Metzger, Marco ; Schmidt, Johannes R ; Windshügel, Björn ; Haupt, Janine ; Neser, Christina ; Biermann, Melina K ; Neurath, Markus F ; Siegmund, Britta ; Lehmann, Jörg ; Kalkhof, Stefan ; Müller, Claudia ; Claussen, Carsten ; Scholz, Ulrike ; Schiefke, Ingolf ; Wiltzsch, Vivien ; Keminer, Oliver ; Oliveira da Rocha, Gustavo Henrique ; Zdzieblo, Daniela ; Pliushcheuskaya, Palina

The aryl hydrocarbon receptor (AhR) was shown to be an important regulator of inflammatory processes at epithelial barriers, and is thus considered a therapeutic target for several chronic inflammatory diseases, such as inflammatory bowel disease. We aimed to identify and validate new AhR agonists that sustainably attenuate intestinal inflammation. Using a high-throughput luciferase reporter gene assay, 90 AhR ligands were identified out of 7448 approved and investigational drugs. Out of these, 15 AhR ligands were selected based on substance class, half maximal effective concentration, known toxicity and pharmacokinetic/pharmacodynamic profiles, and preclinical/clinical evaluation status for other indications. While Febuxostat, Nitazoxanide, Rabeprazole, 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester, 3-Indolepropionic acid, and Indirubin, were already known as AhR agonists, Nabumetone, Teriflunomide, Timapiprant/OC000459, and Caffeic acid phenylethyl ester have not yet been directly described in this context. Six compounds (Daidzein/Equol, as well as compounds no. 19, 22, 49, and 64, not yet disclosed due to pending patent applications) were newly described as AhR agonists. Hit compounds were studied in silico for their molecular interactions with AhR and in vitro for potential immunotoxicity and their ability to induce interleukin (IL)-10 and/or to suppress IL-1β in murine macrophages without significant cytochrome P450 1A1 induction in Caco-2 cells. Five compounds that met these criteria were functionally tested using organoid-based Transwell®-like models derived from gut biopsies. Five candidates restored the epithelial barrier, as evidenced by increased transepithelial electrical resistance and induction of the tight junction proteins claudin-1/-2 and occludin, while exhibiting anti-inflammatory effects, i.e., decreased expression of toll-like receptor 4. Out of these, one compound was selected for future in vivo preclinical studies.

2025-09-01·EUROPEAN JOURNAL OF PHARMACOLOGY

The potential mitigating effect of febuxostat alone or with donepezil on scopolamine-induced Alzheimer's disease in rats: The role of TXNIP/NLRP3 inflammasome signaling pathway

Article

作者: Yassin, Ahmed I ; Abdin, Amany A ; Taha, Dina E ; Kabel, Ahmed M

BACKGROUND:

Alzheimer's disease (AD) is a pervasive neurodegenerative disorder. Despite extensive research, its multifactorial etiology remains complex and not fully understood. The present study was performed to investigate the potential ameliorative effect of febuxostat and donepezil each alone or in combination on scopolamine-induced AD in male Wistar rats via targeting Thioredoxin-interacting protein (TXNIP)/NOD-like receptor protein-3 (NLRP3) inflammasome pathway.

METHODS:

In a rat model of scopolamine-induced AD, the changes in the behavioral tests, biochemical parameters, and the histopathological picture in the hippocampal and cerebral tissues were assessed.

RESULTS:

Administration of either donepezil or febuxostat to scopolamine-induced AD rats significantly improved the behavioral changes, decremented TXNIP levels with amelioration of the neuroinflammation by decreased NLRP3, and IL-1β levels, restoration of the oxidant/antioxidant balance and inhibition of apoptosis by increasing expression of anti-apoptotic protein Bcl-2 with restoration of ACh levels. Notably, only febuxostat causes normalization of fasting blood glucose levels. These changes were positively reflected on the histopathological picture and scoring in both tissues. These beneficial effects were significantly more evidenced in rats treated with donepezil/febuxostat combination relative to monotherapy by either donepezil or febuxostat. The impact of the tested parameters in the disease outcome was evidenced by their significant correlation and moreover the causality by the significant regression, shedding light particularly for the glycemic state and the neuroinflammatory reactions.

CONCLUSION:

These elaborated data signified the neuroprotective effect of febuxostat and indicated that donepezil/febuxostat combination strengthened each other as they act by different mechanisms to counteract AD.

284

项与非布司他相关的新闻（医药）

2025-07-15

·药事纵横

新型抗痛风药在中国上市，疗效优于非布司他

卫材株式会社7月14日对外宣布，该公司已在中国推出了新型抗痛风物“URECE”（中国商品名：“优乐思”，通用名：dotinurad）。优乐思于2024年12月获得中国国家药品监督管理局（NMPA）批准，用于治疗痛风伴高尿酸血症患者。优乐思是由富士药品株式会社发现的痛风及高尿酸血症治疗新药。该药通过选择性抑制肾脏中与尿酸重吸收相关的尿酸转运蛋白（URAT1），抑制尿酸重吸收，从而降低血尿酸水平。卫材与富士药品株式会社就中国及五个东盟成员国（印度尼西亚、马来西亚、缅甸、菲律宾和泰国）达成了许可协议，获得在这些国家的独家开发和销售权。此次在中国的获批基于卫材在中国开展的一项多中心、活性药物对照、双盲、平行组、随机、3期研究的结果。‘’血清尿酸 (SUA) 水平超过 7.0 mg/dL 的痛风患者入组后按 1:1 的比例随机分配至 dotinurad 组或非布司他组，接受为期 24 周的研究药物治疗（dotinurad 组接受 1 mg/天治疗 4 周，随后 2 mg/天治疗 8 周，再随后 4 mg/天治疗 12 周；而非布司他组则接受 20 mg/天治疗 4 周，随后 40 mg/天治疗 20 周）。主要终点是第 24 周时 SUA ≤ 6.0 mg/dL 的患者比例，次要终点是第 12 周时 SUA ≤ 6.0 mg/dL 的患者比例。试验共入组了451 名患者，其中225 名被分配至 dotinurad 组，226 名被分配至非布司他组。其中441 名患者（dotinurad 组 220 名，非布司他组 221 名）被纳入全分析集 (FAS)。在 24 周时，dotinurad 组SUA ≤ 6.0 mg/dL 的患者比例73.6% [95% 置信区间 (CI): 67.8, 79.5]，而非布司他组为 38.1% [95% CI: 31.6, 44.5]，达到了主要终点，这证实了 dotinurad 4 mg 在统计学上显著优于非布司他 40 mg（比例差异 35.87% [95% CI: 27.36, 44.37, p<0.001]）。另外，第 12 周时，dotinurad 组 SUA ≤ 6.0 mg/dL 的患者比例在为 55.5%，而非布司他组为 50.5%，也达到了次要终点，这证实了 dotinurad 2 mg 在统计学上非劣效于非布司他 40 mg（比例差异 5.24% [95% CI: -3.69, 14.17]）。 Dotinurad 组最常见的不良事件为痛风性关节炎、COVID-19 和肝功能异常，在非布司他组为痛风性关节炎、COVID-19 和丙氨酸氨基转移酶 (ALT) 升高。未观察到与 dotinurad 相关的新的安全性问题。痛风可发生于任何年龄，男性多于女性。痛风的患病率正在上升，据估计目前中国约有2300万痛风患者。急性发作时会引起严重的关节疼痛、肿胀、发红和炎症。疼痛通常会在几天内逐渐缓解，但有时可能持续数周。如果不进行治疗，关节组织可能会遭到破坏和变形，导致日常活动受限。药事纵横投稿须知：稿费已上调，欢迎投稿

临床结果临床3期

2025-07-14

·CPHI制药在线

业绩亏损，股价却连创新高，这三家药企做对了什么？

关注并星标CPHI制药在线随着今年创新药支持政策的大爆发，以及国内创新药企研发实力不断提升，从2025年初至今，创新药板块不断创出新高。其中常山药业、一品红、舒泰神三家创新药概念股行情火爆，这三家药企既不是创新药龙头，而且过去一年业绩仍处于亏损之中。那么，是什么造就了这些药企"业绩走低、股价上涨"的现象？常山药业先看常山药业，其股价短期爆发力惊人，今年5、6月份，短短2个月时间，股价涨幅近300%，若拉长时间线来看，过去两年已经涨了10倍多，成为当之无愧的十倍股。常山药业前身为1993年成立的河北常山生化制药厂，以肝素粗品生产起步。后经历几次技术改进、扩张，2011年8月，常山药业正式登陆创业板。肝素是一种天然存在于哺乳动物肥大细胞与中性粒细胞的黏多糖类物质，在临床主要用于抗凝血和抗血栓。常山药业是国内少数拥有完整肝素产业链的企业，产品涵盖肝素粗品、肝素原料药和肝素制剂药品。凭借肝素原料药和制剂业务，2016-2022年间，公司累计盈利12.4亿元。2023年，受集采冲击，常山药业业绩遭遇"滑铁卢"。在第八批全国药品集中带量采购中，常山药业的那屈肝素钙注射液虽然中标，但价格降幅较大。此外，公司主力品种低分子量肝素钙未纳入全国性集采，导致销售收入较2022年度下降46.51%。最终，2023年，常山药业迎来上市后首年亏损，营收锐减至14.1亿元，归母净利润巨亏12.4亿元。2024年，常山药业继续亏损2.49亿元。在业绩连续两年亏损的情况下，常山药业靠胰高血糖素样肽-1受体（GLP-1R）激动剂艾本那肽，为资本市场带来了想象空间。艾本那肽是在全球首款上市的GLP-1药物艾塞那肽基础上，采用化学修饰技术，将艾塞那肽与重组人血白蛋白结合形成。艾本那肽作为一种长效GLP-1R激动剂，半衰期可达7天。2024年4月，艾本那肽的糖尿病适应症国内上市申请获受理。今年5月，艾本那肽拟用于减重适应症的临床试验申请已获得国家药监局受理。在艾本那肽的加持下，常山药业成为GLP-1风口上的新星，被资本疯抢。曾有公开数据统计，常山药业从2023年以来，区间最大涨幅超1300%。对此，常山药业多次澄清：艾本那肽申请上市适应症为治疗2型糖尿病，不涉及肥胖适应症。即使未来肥胖适应症获批上市，也将面临激烈的市场竞争，盈利存在较大不确定性。可狂欢中的人们根本无暇顾及这些提醒。一品红一品红成立于2002年，以仿制药起家，2017年在深交所上市，一品红主要聚焦于儿童药、慢病药领域，现有 26 个儿童药注册批件和 66 个慢病药注册批件，产品结构丰富。在创新项目上，公司主要聚焦在代谢、炎症、神经等领域，共有15个创新药项目。由于一品红转型较早，前几年实实在在吃到了集采红利，然而由于去年7月，一品红在第七批国家药品集采盐酸溴己新注射液投标中存在违约情形，不仅被要求退还集采销售所得2.66亿元，还被暂停从2024年8月21日至2025年2月20日参与国家组织药品集中采购的资格。这一惩罚使得一品红元气大伤。业绩方面，2024年，实现营收14.5亿元，同比下降42.07%，净利润为-5.40亿元，上市后首次迎来亏损；2025年一季度营收3.77亿元，同比下降39.48%，净利润为5659万元，同比下降43.7%。但是在营收大幅下滑，净利润首亏背景下，一品红的股价还是从开年时的不足20元涨到6月份的57.31元，主要原因就在于公司的一款痛风创新药：氘泊替诺雷。痛风是一种尿酸过度沉积导致的疾病，据《2021中国高尿酸及痛风趋势白皮书》显示，截至2020年全球高尿酸及痛风患病人数为9.3亿人，中国高尿酸血症的患病人数约为1.77亿，痛风患病人数约为1466万，且新发患者逐渐年轻化。可以说，这一领域市场相当可观。与巨大的临床需求相对应的，是有限的治疗选择。目前国内外指南推荐的一线治疗高尿酸/痛风的药物为别嘌醇和非布司他，但别嘌醇有过敏风险，非布司他被FDA黑框警告心血管风险。痛风市场亟待一个安全性与疗效性俱佳的好药。氘泊替诺雷是一款URAT1抑制剂，基于苯溴马隆改造而来。目前，URAT1抑制剂在痛风创新药研发领域深受追捧，国内外在研产品约37个。除了已经上市的多替诺雷和排队等待的恒瑞同靶点药物外，一品红的氘泊替诺雷等已在国内进入III期临床。并且AR882在已完成的全球多中心IIb期临床试验中，展现出显著的疗效和良好的安全性，有望成为潜在的BIC产品，为痛风患者提供一种更安全、更有效的治疗选择。痛风领域之外，一品红还开发了创新药物APH01727，这是一种高活性、高选择性的GLP-1RA，旨在成为每日一次的口服小分子GLP-1R激动剂，用于2型糖尿病的治疗。舒泰神舒泰神成立于2002年8月，这家老药企在成立初期依靠鼠神经生长因子（商品名：苏肽生）带来业绩。鼠神经生长因子能够促进神经生长和修复，巅峰时期，这款药物销售额超过12亿元。但是最终由于疗效存疑，苏肽生于2019年被移除出医保目录，舒泰神业绩受到重创。好在公司的创新药研发进展还算顺利。其注射用STSP-0601的上市申请已获国家药监局受理，适应症为用于伴抑制物的血友病A或B成人患者出血按需治疗。血友病是一种因体内凝血因子缺乏导致凝血障碍的遗传性出血性疾病，根据国家统计局2024年全国人口数14亿计算，全国存量血友病患者人群大约为14万人。目前该病治疗方式国内主要为定期注射凝血因子产品，但这种治疗方式会产生抑制凝血因子的抗体，导致患者受伤后，还是会发生无法止血的现象。STSP-0601通过激活凝血因子X，促进凝血酶生成，在IIb期研究中，STSP-0601达到了预设的主要有效性终点。6月5日，STSP-0601被国家药监局纳入优先审评品种名单，进入药品上市许可优先审评审批程序；并获得FDA用于治疗A型血友病和B型血友病的孤儿药认定。STSP-0601的出色表现，使得舒泰神在不到一个月时间，股价涨了近5倍，达30多元/股，创近几年新高。纵观以上三家药企，股价飙升除了与医药行业景气度提高有关外，主要在于企业自身抓住风口，给出了想象力。这也进一步体现了公司产品规划的前瞻性。接下来，这些"风口创新药"的审批进展与商业化落地将直接影响股价走向。而公司当前的涨幅和市值，是否与其基本面相匹配，见仁见智。主要参考资料： 1、《起底"神药"艾本那肽》，医曜，2025.06.11. 2、Ribatti D. The failed attribution of the Nobel Prize for Medicine or Physiology to Viktor Hamburger for the discovery of Nerve Growth Factor. Brain Res Bull. 2016;124:306-9. doi: 10.1016/j.brainresbull.2016.02.019. 3、《舒泰神，复刻热景和三生制药，悄然崛起？》，生物星海，2025-05-27.END智药研习社近期直播预告来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com▼更多制药资讯，请关注CPHI制药在线▼点击阅读原文，进入智药研习社~

带量采购财报医药出海核酸药物申请上市

2025-07-14

·eisai.com

“URECE®” (Dotinurad) Launched in China as a treatment for Gout

For Print（549KB） July 14, 2025 Eisai Co., Ltd. (Headquarters: Tokyo, CEO: Haruo Naito, “Eisai”) announced today that it has launched “URECE®” (brand name in China: “优乐思®”, generic name: dotinurad) in China as a treatment for Gout. URECE was approved by the National Medical Products Administration in China as a treatment for gout patients with hyperuricemia in December 2024. URECE is a new therapeutic medicine for gout and hyperuricemia discovered by FUJI YAKUHIN. It suppresses uric acid reabsorption and lowers blood uric acid levels by selectively inhibiting the urate transporter (URAT1) related to reabsorption of uric acid in the kidney. Eisai concluded a license agreement with FUJI YAKUHIN for China and five ASEAN member states: Indonesia, Malaysia, Myanmar, the Philippines, and Thailand, granting exclusive development and distribution rights in these countries. This approval in China is based on the results of a multicenter, active-controlled, double-blind, parallel-group, randomized, Phase 3 study of 451 gout patients conducted in China by Eisai.1 The results of this study showed that the proportion of subjects with serum uric acid levels of 6.0 mg/dL or less at 24 weeks, which was the primary endpoint, was 73.6% [95% confidence interval (CI): 67.8, 79.5] in the dotinurad group and 38.1% [95% CI: 31.6, 44.5] in the comparator febuxostat group, confirming the statistical superiority of dotinurad 4 mg over febuxostat 40 mg (difference of proportion 35.87% [95% CI: 27.36, 44.37, p<0.001]) (see “Notes to Editors” section “3. About the Phase 3 Clinical Trial”). Eisai has obtained approval for dotinurad in China, Thailand and the Philippines. Gout can develop at any age, is more common in men than women, and during an acute attack, can cause severe joint pain, swelling, redness, and inflammation. The pain gradually improves over a few days, but can sometimes last for weeks. If left untreated, the joint tissue may become damaged and deformed, leading to restrictions in daily activities and a decrease in quality of life.2 The prevalence of gout is increasing, and it is estimated that there are currently about 23 million patients with gout in China.3 It is expected that the number of patients will further increase in the near future due to changes in lifestyle and dietary preferences in accordance with socioeconomic development. Eisai is committed to providing URECE to more patients with gout in China as a new treatment option, and will contribute to improving the quality of life (QOL) of patients. Media Inquiries: Eisai Co., Ltd. Public Relations Department TEL: +81-(0)3-3817-5120 Chinese Trade name: “优乐思” (URECE) Chinese generic name: 多替诺雷片 (Dotinurad Tablets) Indication for use: It is indicated for gout patients with hyperuricemia. Dosage and administration: For oral use, the usual adult initial dosage is 1 mg of dotinurad once daily. The dose level should then be gradually increased as needed by checking blood uric acid levels. The usual maintenance dosage is 2 mg once daily and may be adjusted according to the patient’s condition, but up to 4 mg once daily. URECE is a therapeutic medicine for gout and hyperuricemia discovered by FUJI YAKUHIN. URECE selectively inhibits URAT1, one of the uric acid transporters, thus preventing reabsorption of uric acid by the kidneys and promoting uric acid excretion in the urine. In addition, URECE has a small effect on other transporters affecting uric acid secretion, so it reduces serum uric acid levels at lower doses. URECE is expected to have a low risk of side effects and drug interactions. In Japan, FUJI YAKUHIN obtained manufacturing and marketing approval for URECE in January 2020 and launched it in May 2020. Eisai concluded a license agreement with FUJI YAKUHIN for China and five ASEAN member states: Indonesia, Malaysia, Myanmar, the Philippines, and Thailand, granting exclusive development and distribution rights in these countries. URECE was approved in Thailand for gout and hyperuricemia in Thailand in September, 2024 and in the Philippines in February, 2025. This was a multicenter, active-controlled, double-blind, parallel-group, randomized, Phase 3 study conducted to confirm the superiority of dotinurad 4 mg over febuxostat 40 mg as the primary endpoint, assess safety, and confirm the non-inferiority of dotinurad 2 mg to febuxostat 40 mg as the secondary endpoint in Chinese patients with gout. Patients with gout and serum uric acid (SUA) levels exceeding 7.0 mg/dL were randomly assigned to either the dotinurad group or the febuxostat group in a 1:1 ratio, investigational product treatment for 24 weeks (the dotinurad group received 1 mg/day for 4 weeks, 2 mg/day for 8 weeks, and 4 mg/day for 12 weeks, while the febuxostat group received 20 mg/day for 4 weeks and 40 mg/day for 20 weeks). The primary endpoint was the proportion of patients with SUA ≤6.0 mg/dL at 24 weeks, and the secondary endpoint was the proportion of patients with SUA ≤6.0 mg/dL at 12 weeks. Of the total 451 patients, 225 were assigned to the dotinurad group and 226 to the febuxostat group. Of these, 441 patients (220 in the dotinurad group and 221 in the febuxostat group) were included in the Full Analysis Set (FAS). For the primary endpoint, the proportion of patients with SUA ≤6.0 mg/dL at 24 weeks was 73.6% [95% confidence interval (CI): 67.8, 79.5] in the dotinurad group and 38.1% [95% CI: 31.6, 44.5] in the febuxostat group, confirming the statistical superiority of dotinurad 4 mg over febuxostat 40 mg (difference of proportion 35.87% [95% CI: 27.36, 44.37, p<0.001]). For the secondary endpoint, the proportion of patients with SUA ≤6.0 mg/dL at 12 weeks was 55.5% in the dotinurad group and 50.5% in the febuxostat group, confirming the statistical non-inferiority of dotinurad 2 mg to febuxostat 40 mg (difference of proportion 5.24% [95% CI: -3.69, 14.17]). The most common adverse events were gouty arthritis, COVID-19, and liver function abnormality in the dotinurad group, and gouty arthritis, COVID-19, and increased alanine aminotransferase (ALT) in the febuxostat group. No new safety concerns with dotinurad were observed. References Full text（549KB）

临床3期引进/卖出临床结果上市批准

100 项与非布司他相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01206	非布司他	M04AA03	DB04854

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
痛风性关节炎	欧盟	Viatris Ltd. (New Zealand)	2017-06-15
痛风性关节炎	冰岛	Viatris Ltd. (New Zealand)	2017-06-15
痛风性关节炎	列支敦士登	Viatris Ltd. (New Zealand)	2017-06-15
痛风性关节炎	挪威	Viatris Ltd. (New Zealand)	2017-06-15
慢性高尿酸血症	欧盟	Viatris Ltd. (New Zealand)	2017-06-15
慢性高尿酸血症	冰岛	Viatris Ltd. (New Zealand)	2017-06-15
慢性高尿酸血症	列支敦士登	Viatris Ltd. (New Zealand)	2017-06-15
慢性高尿酸血症	挪威	Viatris Ltd. (New Zealand)	2017-06-15
痛风	美国	Takeda Pharmaceuticals U.S.A., Inc.	2009-02-13
高尿酸血症	欧盟	Menarini International Operations Luxembourg SA	2008-04-21
高尿酸血症	冰岛	Menarini International Operations Luxembourg SA	2008-04-21
高尿酸血症	列支敦士登	Menarini International Operations Luxembourg SA	2008-04-21
高尿酸血症	挪威	Menarini International Operations Luxembourg SA	2008-04-21

未上市

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适应症	最高研发状态	国家/地区	公司	日期
血液肿瘤	临床3期	-	A. Menarini Industrie Farmaceutiche Riunite Srl	2012-10-01
肿瘤溶解综合征	临床3期	-	A. Menarini Industrie Farmaceutiche Riunite Srl	2012-10-01
心血管畸形	临床3期	美国	Takeda Pharmaceutical Co., Ltd.	2010-04-23
心血管畸形	临床3期	墨西哥	Takeda Pharmaceutical Co., Ltd.	2010-04-23
原发性痛风	临床3期	-	Takeda Pharmaceutical Co., Ltd.	2002-07-01
稳定型心绞痛	临床2期	美国	Takeda Pharmaceutical Co., Ltd.	2012-07-01
高血压	临床2期	美国	Takeda Pharmaceutical Co., Ltd.	2012-02-01
肾结石	临床2期	美国	Takeda Pharmaceutical Co., Ltd.	2010-02-01
草酸钙肾石病	临床2期	美国	Takeda Pharmaceutical Co., Ltd.	2010-02-01
脑梗塞	临床阶段不明	日本	Teijin Pharma Ltd.	2013-11-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05574036 (Pubmed \| Eur J Pharmacol)	临床2期	代谢功能障碍相关的脂肪肝病 NLRP-3 \| TIM-3 \| HOMA-IR ... 更多	-	Febuxostat 80 mg	鹽廠觸衊餘壓窪醖齋餘(積糧齋鹽淵顧願構鏇淵) = 廠觸願積衊艱簾獵淵鑰顧餘艱構憲築艱齋糧鏇 (願壓鹽窪衊觸構壓選願 )	积极	2025-08-01
				Vitamin E 400 mg	鹽廠觸衊餘壓窪醖齋餘(積糧齋鹽淵顧願構鏇淵) = 廠獵齋願膚淵膚蓋範淵顧餘艱構憲築艱齋糧鏇 (願壓鹽窪衊觸構壓選願 )
EULAR2024	N/A	痛风 \| 慢性肾病 serum urate levels	342	Febuxostat (Normal kidney function)	顧襯鹽網齋壓鏇餘遞餘(鑰壓襯鬱鏇選壓淵構鏇) = 窪網艱襯壓鬱鑰積糧繭繭鬱蓋鹹憲構築鹽鬱觸 (網繭糧糧獵遞鏇範衊鏇 )	积极	2024-06-05
				Febuxostat (Chronic kidney disease)	顧襯鹽網齋壓鏇餘遞餘(鑰壓襯鬱鏇選壓淵構鏇) = 淵淵膚糧鑰膚憲繭鬱衊繭鬱蓋鹹憲構築鹽鬱觸 (網繭糧糧獵遞鏇範衊鏇 )
SAT641 (ENDO2023)	N/A	-	12	Febuxostat treated water	艱製餘襯餘積範製糧膚(餘糧夢繭鹹鹹鹽繭積廠) = 繭鑰廠繭憲鹹積獵醖餘遞觸膚遞艱獵鹹衊簾醖 (選鏇觸範廠憲鏇艱蓋鹽, 2.70) 更多	积极	2023-10-05
				Febuxostat (Sham-control)	醖積製醖壓膚鏇網鏇鏇(製衊顧遞鬱選構簾製選) = 範窪醖製艱衊窪廠築衊窪獵夢鹽艱壓窪鏇顧獵 (壓襯觸壓鬱積鹽膚網襯, 0.1) 更多
EASD2023	N/A	眼球运动障碍	-	Febuxostat	積醖憲糧製觸觸衊範觸(壓壓襯蓋醖製醖糧積鏇) = Febuxostat-treated adipocytes exhibited higher UCP1 (p<0.05, vs. febuxostat) and other marker gene mRNA expressions (PRDM16, PPARγ, PGC1a, FABP4) 願衊繭醖鏇觸積醖廠繭 (築夢窪製網鑰膚繭範築 ) 更多	积极	2023-10-04
				febuxostat (Control)
TCTR20210224005 (Pubmed \| Sci Rep)	临床4期	慢性肾病	84	Febuxostat	鬱淵築鑰醖鏇蓋壓蓋蓋(衊築觸範範顧觸願齋鹽) = 窪膚襯築醖鬱選夢範膚齋築獵夢觸衊範膚構鏇 (廠製積願鏇顧觸願醖艱, 0.31 ~ 3.7)	-	2023-08-18
				febuxostat (Control)	鬱淵築鑰醖鏇蓋壓蓋蓋(衊築觸範範顧觸願齋鹽) = 觸鹹醖鬱壓鏇壓積鑰網齋築獵夢觸衊範膚構鏇 (廠製積願鏇顧觸願醖艱, -1.52 ~ 1.61)
WCO_IOF_ESCEO2023	N/A	痛风 \| 2型糖尿病 urate-lowering drugs	78	Allopurinol 100 mg/d	簾襯繭築蓋選觸製鏇憲(襯糧齋積衊淵餘襯願鬱) = 衊繭獵艱餘鬱鑰衊獵鹽繭鑰膚構醖憲餘蓋網範 (餘糧衊鏇築齋鬱鏇製範 )	积极	2023-05-04
				Allopurinol 300 mg/d	簾襯繭築蓋選觸製鏇憲(襯糧齋積衊淵餘襯願鬱) = 鬱蓋餘製蓋築製艱蓋襯繭鑰膚構醖憲餘蓋網範 (餘糧衊鏇築齋鬱鏇製範 )
ASN2022	N/A	高尿酸血症 \| 高血压 \| 慢性肾病 hyperuricemia \| hypertension	96	Febuxostat	鹹網襯獵淵繭夢選淵簾(餘壓繭獵膚餘鑰願衊淵) = 遞鏇鬱鬱構觸衊繭蓋繭願壓製襯齋範鹽選壓蓋 (選願餘顧膚構製衊範餘, -2.00 ~ 1.55)	不佳	2022-11-05
				Benzbromarone	-
NCT04157959 (Pubmed \| J Clin Pharmacol)	N/A	Lesch-Nyhan综合征	-	SHR4640 10 mg	夢夢願顧糧選網鏇醖觸(鹹簾顧窪築範鏇艱鑰範) = 蓋糧齋製繭鑰簾膚觸觸觸蓋壓顧繭願窪鹹網膚 (鑰齋夢夢鬱遞齋遞鬱築 )	-	2022-09-21
				SHR4640 10 mg + Febuxostat 80 mg	夢夢願顧糧選網鏇醖觸(鹹簾顧窪築範鏇艱鑰範) = 構觸窪選膚襯淵衊遞夢觸蓋壓顧繭願窪鹹網膚 (鑰齋夢夢鬱遞齋遞鬱築 )
EULAR2022	N/A	痛风	-	Febuxostat	築築窪膚襯齋獵窪糧糧(顧艱餘顧鑰範選壓鹹願): HR = 1.1 (95% CI, 0.96 ~ 1.26) 更多	-	2022-06-01
				Allopurinol
NCT01101035 (CARES, EULAR2022)	临床3期	痛风 serum uric acid	-	Febuxostat	網積醖壓艱憲遞蓋憲網(襯選廠願糧鹽願鑰憲鑰) = 艱鏇網選壓願餘醖簾壓遞壓鏇艱網觸築製淵選 (鏇獵淵廠選鑰網鏇簾鬱 )	积极	2022-06-01
				Allopurinol	網積醖壓艱憲遞蓋憲網(襯選廠願糧鹽願鑰憲鑰) = 齋窪膚鹽遞憲繭膚醖獵遞壓鏇艱網觸築製淵選 (鏇獵淵廠選鑰網鏇簾鬱 )