更新于：2024-11-17
Febuxostat
非布司他
更新于：2024-11-17
概要
基本信息
在研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2008-04-21), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C16H16N2O3S |
InChIKeyBQSJTQLCZDPROO-UHFFFAOYSA-N |
CAS号144060-53-7 |
关联
313
项与 非布司他 相关的临床试验A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment and two-sequence of Febuxostat Tablets 80 mg relative to Feburic 80 mg (Febuxostat Tablets 80 mg) in healthy Thai volunteers under fasting condition
Study on the Efficacy and Safety of Extracorporeal High-Frequency Hyperthermia in the Treatment of Refractory Gout
A Prospective, Multicenter, Randomized Investigator Initiative Clinical Trial Study on the Effects of Febuxostat Dose Tapering in Gout Patients Optimally Controlled for 5 Years or More
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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1,280
项与 非布司他 相关的文献（医药）2025-03-01Current radiopharmaceuticals
Response of Male Reproductive System Against Ionizing Radiation and Available Radio-protective Agents: Cellular and Molecular Insight
Article
作者: Jheeta, Kuldeep S ; Meena, Priyadarshi ; Parashar, Ronit ; Patel, Dev Dutt ; Kumar, Raj ; Yadav, Sanwar Mal ; Saini, Priya
Background::
The reproductive organ, housing spermatogonial stem cells (SSCs),
undergoes ongoing division impacted by the irradiation dosage and exposure duration. Within
the male reproductive organ, germ stem cells (spermatogonia) and somatic cells (Sertoli and
Leydig cells) are present. Lower doses of ionizing (>4-6 Gy) and non-ionizing radiation (radiofrequency
and microwave range 900 MHz - 2.45 GHz) may cause sperm-related issues, while
higher doses (15 Gy) may affect Leydig cells and testosterone production. Response to radiation
varies with age and pubescence. Spermatogonial stem cells, crucial for regenerating the spermatogenic
lineage, express molecular markers like Estrogen receptor, FSH (Follicular Stimulating
Hormone) receptor, TLR-4 (Toll-like Receptor-4), TLR-5 (Toll-like Receptor-5), FGF2 (Fibroblast
Growth Factor-2), KIT (Receptor Tyrosine Kinase), AT-1 (Angiotensin II Type-1 Receptor),
LXRs-γ (Liver X Receptor-γ), TNF-β (Tumor Necrosis Factor-β), and PCNA (Proliferating
Cell Nuclear Antigen), influencing stem cell activity in testes.
Objective::
This study aimed to review the various available radioprotective agents and their efficacy
in targeting the male reproductive system from the available literature.
Result::
Various radioprotective herbal/synthetic/microbial/metallic extracts/formulations/
drugs [Septilin, Silymarin, Organic Turmeric, Oestrogen, Melatonin, Febuxostat, SQGD (Semiquinone
glucoside derivative), Rapamycin, Entolimod, Zinc, Selenium, etc.] have been investigated
up to exposure, but owing to effectiveness issues, they are unable to fulfil the aim to the
fullest of restoring male fertility and normal testosterone levels during such eventuality.
Conclusion::
Further study is needed to optimize these tactics and fill knowledge gaps. Also, the
effective components of herbal, synthetic drugs, etc., should be isolated and tested up to clinical
levels, paving the way for successful radioprotection and radiomitigation strategies in the male
reproductive system.
2025-01-01Current drug discovery technologies
A Combination of Pharmacophore Generation, Ligand-based Virtual Screening, Atom-based 3D-QSAR, and Molecular Docking Studies on Febuxostat-based Amides Analogues as Anti-inflammatory Agents
Article
作者: Jagdale, Sakshi M. ; Thorat, Shubhangi B. ; Garud, Dinesh R. ; Asgaonkar, Kalyani D. ; Hirode, Purvaj V. ; Bhatambrekar, Aniket L. ; Hajare, Sayli G. ; Chitre, Trupti S.
Background::
A defence mechanism of the body includes inflammation. It is a process
through which the immune system identifies, rejects, and starts to repair foreign and damaging stimuli.
In the world, chronic inflammatory disorders are the leading cause of death.
Materials and Methods::
To obtain optimized pharmacophore, previously reported febuxostat-
based anti-inflammatory amide derivatives series were subjected to pharmacophore hypothesis,
ligand-based virtual screening, and 3D-QSAR studies in the present work using Schrodinger
suite 2022-4. QuikProp module of Schrodinger was used for ADMET prediction, and HTVS, SP,
and XP protocols of GLIDE modules were used for molecular docking on target protein (PDB
ID:3LN1).
Result::
Utilising 29 compounds, a five-point model of common pharmacophore hypotheses was
created, having pIC50 ranging between 5.34 and 4.871. The top pharmacophore hypothesis AHHRR_
1 model consists of one hydrogen bond acceptor, two hydrophobic groups and two ring substitution
features. The hypothesis model AHHRR_1 underwent ligand-based virtual screening using
the molecules from Asinex. Additionally, a 3D-QSAR study based on individual atoms was performed
to assess their contributions to model development. The top QSAR model was chosen
based on the values of R2 (0.9531) and Q2 (0.9424). Finally, four potential hits were obtained by
molecular docking based on virtual screening.
Conclusion::
The virtual screen compounds have shown similar docking interaction with amino
acid residues as shown by standard diclofenac sodium drugs. Therefore, the findings in the present
study can be explored in the development of potent anti-inflammatory agents.
2024-12-31ANNALS OF MEDICINE
Febuxostat provides renoprotection in patients with hyperuricemia or gout: a systematic review and meta-analysis of randomized controlled trials
Review
作者: Yang, Xiu Hong ; Zhang, Bao Long ; Cheng, Yun ; Jin, Hui Min ; Fu, Shun Kun
PURPOSE:
It is unknown whether febuxostat can delay the progression of kidney dysfunction and reduce kidney endpoint events. The aim was to evaluate the renoprotective effect of febuxostat in patients with hyperuricemia or gout by performing a meta-analysis of randomized controlled trials (RCTs).
METHODS:
MEDLINE, Web of science, EMBASE, ClinicalTrials.gov, and the Cochrane Central Register for Randomized Controlled Trials were searched. The main outcomes included kidney events (serum creatinine doubling or progression to end-stage kidney disease or dialysis). The secondary outcomes were the rate of change in the estimated glomerular filtration rate (eGFR) and changes in the urine protein or urine albumin to creatinine ratio from baseline to the end of follow-up. We used random-effects models to calculate the pooled risk estimates and 95% CIs.
RESULTS:
A total of 16 RCTs were included in the meta-analysis. In comparison with the control group, the patients who received febuxostat showed a reduced risk of kidney events (RR = 0.56, 95% CI 0.37-0.84, p = 0.006) and a slower decline in eGFR (WMD = 0.90 mL/min/1.73 m2, 95% CI 0.31-1.48, p = 0.003). The pooled results also revealed that febuxostat use reduced the urine albumin to creatinine ratio (SMD = -0.21, 95% CI -0.41 to -0.01, p = 0.042).
CONCLUSION:
Febuxostat use is associated with a reduced risk of kidney events and a slow decline in eGFR. In addition, the urine albumin to creatinine ratio decreased in febuxostat users. Accordingly, it is an effective drug for delaying the progression of kidney function deterioration in patients with gout.Systematic review registration: PROSPERO CRD42021272591.
100 项与 非布司他 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 痛风性关节炎 | 欧盟 | 2017-06-15 | |
| 痛风性关节炎 | 冰岛 | 2017-06-15 | |
| 痛风性关节炎 | 列支敦士登 | 2017-06-15 | |
| 痛风性关节炎 | 挪威 | 2017-06-15 | |
| 慢性高尿酸血症 | 欧盟 | 2017-06-15 | |
| 慢性高尿酸血症 | 冰岛 | 2017-06-15 | |
| 慢性高尿酸血症 | 列支敦士登 | 2017-06-15 | |
| 慢性高尿酸血症 | 挪威 | 2017-06-15 | |
| 痛风 | 美国 | 2009-02-13 | |
| 高尿酸血症 | 欧盟 | 2008-04-21 | |
| 高尿酸血症 | 冰岛 | 2008-04-21 | |
| 高尿酸血症 | 列支敦士登 | 2008-04-21 | |
| 高尿酸血症 | 挪威 | 2008-04-21 |
未上市
10 条进展最快的记录, 后查看更多信息
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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 | - | 2012-10-01 | |
| 肿瘤溶解综合征 | 临床3期 | - | 2012-10-01 | |
| 心血管疾病 | 临床3期 | 美国 | 2010-04-23 | |
| 心血管疾病 | 临床3期 | 墨西哥 | 2010-04-23 | |
| 稳定型心绞痛 | 临床2期 | 美国 | 2012-07-01 | |
| 高血压 | 临床2期 | 美国 | 2012-02-01 | |
| 肾结石 | 临床2期 | 美国 | 2010-02-01 | |
| 草酸钙肾石病 | 临床2期 | 美国 | 2010-02-01 | |
| 原发性痛风 | 临床1期 | - | 2022-04-30 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 342 | (Normal kidney function) | 憲夢簾鬱淵鏇積製觸夢(範繭餘憲構醖選繭糧餘) = 範構積鏇窪鏇遞製襯餘 壓鹹醖衊製鏇壓積構築 (觸遞積築夢蓋網積選鏇 ) | 积极 | 2024-06-05 | ||
(Chronic kidney disease) | 憲夢簾鬱淵鏇積製觸夢(範繭餘憲構醖選繭糧餘) = 製製簾鑰簾淵積蓋築繭 壓鹹醖衊製鏇壓積構築 (觸遞積築夢蓋網積選鏇 ) | ||||||
N/A | - | 鹽艱積構衊齋襯積築膚(憲鏇糧鑰憲醖積積蓋觸) = Febuxostat-treated adipocytes exhibited higher UCP1 (p<0.05, vs. febuxostat) and other marker gene mRNA expressions (PRDM16, PPARγ, PGC1a, FABP4) 壓艱選網醖醖憲襯壓襯 (膚淵醖淵齋糧簾蓋構鏇 ) 更多 | 积极 | 2023-10-04 | |||
临床4期 | 84 | 製鏇範範築製觸蓋簾齋(醖膚範衊鹽醖製襯膚鏇) = 鏇願壓鬱繭窪遞顧廠鹹 遞選選蓋繭製衊構製鹹 (鑰範鑰顧糧蓋鹹艱願壓, 0.31 ~ 3.7) | - | 2023-08-18 | |||
(Control) | 製鏇範範築製觸蓋簾齋(醖膚範衊鹽醖製襯膚鏇) = 鏇鬱願製窪襯構糧繭憲 遞選選蓋繭製衊構製鹹 (鑰範鑰顧糧蓋鹹艱願壓, -1.52 ~ 1.61) | ||||||
N/A | 96 | 構餘齋獵鹽構夢憲選鏇(鬱築簾餘窪選構衊積壓) = 遞鹽鏇夢選範餘積憲選 繭顧膚鑰願鬱餘艱鑰窪 (窪選糧網壓夢淵衊簾鹹, -2.00 ~ 1.55) | 不佳 | 2022-11-05 | |||
- | |||||||
N/A | - | 蓋齋窪鏇獵襯網繭鹽鹽(蓋範遞壓夢製鏇網齋膚) = 繭積範膚襯夢網鹹夢鏇 窪齋遞願範築簾廠壓憲 (廠醖夢鑰淵觸簾願鹽願 ) | - | 2022-09-21 | |||
蓋齋窪鏇獵襯網繭鹽鹽(蓋範遞壓夢製鏇網齋膚) = 繭膚餘遞餘蓋選選蓋製 窪齋遞願範築簾廠壓憲 (廠醖夢鑰淵觸簾願鹽願 ) | |||||||
N/A | - | 遞顧繭廠醖襯齋淵鑰鏇(獵願襯鬱獵積窪願願衊): HR = 1.1 (95% CI, 0.96 ~ 1.26) 更多 | - | 2022-06-01 | |||
N/A | 136 | 繭鹽範窪鏇蓋鹽鏇膚衊(簾鏇憲鏇觸範窪衊艱蓋) = 窪獵鹽餘憲膚鬱簾壓積 繭鹹選鹽遞膚憲構範選 (鹹鹽顧鏇遞衊遞築願鹽 ) 更多 | 积极 | 2022-06-01 | |||
N/A | 痛风 serum uric acid | - | 網糧遞襯膚膚鹽鑰鑰蓋(鏇簾鹽獵鏇襯襯繭鑰淵) = 鬱觸廠憲艱淵夢鏇築簾 膚艱選餘窪夢襯簾選願 (窪衊遞願膚願餘齋艱糧 ) | 积极 | 2022-06-01 | ||
網糧遞襯膚膚鹽鑰鑰蓋(鏇簾鹽獵鏇襯襯繭鑰淵) = 蓋鬱願鬱願淵壓鏇襯艱 膚艱選餘窪夢襯簾選願 (窪衊遞願膚願餘齋艱糧 ) | |||||||
PRIZE (Pubmed) 人工标引  | N/A | 514 | 齋鬱積選蓋夢齋範獵憲(蓋繭顧鹽顧窪憲構簾膚): difference = -0.56 (95% CI, -1.670 ~ 0.548), P-Value = 0.319 更多 | 不佳 | 2022-04-28 | ||
N/A | 慢性肾病 serum uric acid levels ≥ 7 mg/dL | - | Febuxostat 40-mg tablet | 鏇淵鹹願廠製夢膚襯獵(夢餘壓遞獵築壓鏇積襯) = 鹹構襯遞襯鏇顧壓鏇齋 憲憲餘蓋選淵鑰簾網憲 (觸選製簾積範憲窪廠築, 8.29) 更多 | 积极 | 2022-02-01 | |
Placebo tablet | 鏇淵鹹願廠製夢膚襯獵(夢餘壓遞獵築壓鏇積襯) = 窪鹽糧夢齋範醖築鹹獵 憲憲餘蓋選淵鑰簾網憲 (觸選製簾積範憲窪廠築, 7.72) 更多 |
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