呋喃妥因(Nitrofurantoin) - 药物靶点：DNA_在研适应症：泌尿道感染_专利_临床

概要

基本信息

简介Nitrofurantoin是一种抗生素，由Procter & Gamble研发。它于1953年2月6日在美国首次获批。尼托芬妥的适应症为治疗泌尿道感染，作用机制为抑制细菌DNA的复制，从而达到杀菌的效果。常见的副作用包括恶心、食欲不振、腹泻和头痛。

药物类型

小分子化药

别名

1-((5-nitro-2-furanyl)methylene)amino-2,4-imidazolidenedione、1-((5-nitrofurfurylidene)amino)hydantoin、5-Nitrofurantoin

+ [18]

靶点

DNA

作用机制

DNA抑制剂(DNA抑制剂)

治疗领域

感染泌尿生殖系统疾病

在研适应症

泌尿道感染

非在研适应症-

原研机构

Procter & Gamble Co.

在研机构

Almatica Pharma LLC

Casper Pharma LLC

非在研机构

Procter & Gamble Pharmaceuticals, Inc.

最高研发阶段批准上市

首次获批日期

美国 (1953-02-06),

泌尿道感染

最高研发阶段(中国)-

特殊审评-

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结构

分子式C8H6N4O5

InChIKeyNXFQHRVNIOXGAQ-UHFFFAOYSA-N

CAS号67-20-9

关联

46

项与呋喃妥因相关的临床试验

NCT06518291 / Not yet recruiting临床4期IIT

COMPARISON OF NITROFURANTOIN WITH FOSFOMYCIN in TREATING CYSTITIS IN WOMEN

Fosfomycin and nitrofurantoin are increasingly being prescribed in outpatients for the oral treatment of urinary tract infection (UTI). The newest guidelines for empirical treatment of women with uncomplicated urinary tract infections (UTIs) advise clinicians to choose among three venerable antibiotics: trimethoprim-sulfamethoxazole, nitrofurantoin, and fosfomycin. Although both nitrofurantoin and fosfomycin have shown efficacy against most urinary pathogens, no recent head-to-head comparisons have been reported. So, this study will be conducted to compare effectiveness of both drugs.

开始日期2025-01-01

申办/合作机构-

CTRI/2024/10/075079 / Not yet recruitingN/AIIT

An Open Label Randomized Standard Controlled Clinical Study to Assess the Synergistic Efficacy of Two Unani Formulations in the Management of Uncomplicated Urinary Tract Infection (Tadiya-e-Aalat-e-Baul) - NIL

开始日期2024-10-15

申办/合作机构-

CTRI/2024/08/072104 / Not yet recruitingN/AIIT

Analgesic Effect Of Single Antibiotic Paste Nitrofurantoin as an Intracanal medicament– A Randomized Controlled Trial - NIL

开始日期2024-08-16

申办/合作机构-

100 项与呋喃妥因相关的临床结果

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100 项与呋喃妥因相关的转化医学

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100 项与呋喃妥因相关的专利（医药）

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4,511

项与呋喃妥因相关的文献（医药）

2025-01-01·SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

Exploring the charge transfer enhancement mechanism in selective SERS detection with Mo1−W S2@Ag2S nanosheets

Article

作者: Huang, Jie ; Liang, Pei ; Tang, Qiao ; Dong, Qianmin ; Chen, Qing ; Pang, Kun

In order to solve the problem of poor sensitivity and selectivity of conventional SERS substrates, we synthesized Mo_1-xW_xS₂@Ag₂S nanosheets in this paper by a two-step hydrothermal method. The structure and morphology of the synthesized Mo_1-_xW_xS₂@Ag₂S nanosheets were characterized by XRD and SEM,respectively. The results show that the Mo_1-_xW_xS₂@Ag₂S nanosheet has an irregular layered structure. Further, the SERS properties of Mo_1-_xW_xS₂@Ag₂S nanosheets were tested by using rhodamine 6G (R6G), crystalline violet (CV), and 4-mercaptobenzoic acid (4-MBA) as probe molecules, respectively. The test results demonstrated that the nanosheets were specific to R6G and CV probe molecules, and the mechanism of selectivity was due to CT enhancement. In addition, Mo_1-_xW_xS₂@Ag₂S exhibits ultrahigh sensitivity in R6G and CV, with the corresponding detection limit of both reached 10^-8 M. And linear fitting of the peak intensities was carried out, with the R² coefficient of 0.981 and 0.951, respectively. Finally, the relative standard deviations (RSDs) of this Mo1-xWxS2@Ag2S nanosheets was obtained to be 8.56 % by test 1 × 10^-4 M R6G at the characteristic peak 613 cm^-1, which represents excellent detection repeatability. The Mo_1-_xW_xS₂@Ag₂S nanosheets are rich in edge-active sites favorable for charge transfer, which can enhance the SERS signals of the target molecules better. Besides, the Raman detection of the surface of Mo_1-_xW_xS₂@Ag₂S nanosheets using nitrofurantoin (NFT) also reached a detection limit of 10^-8 M. Mo_1-_xW_xS₂@Ag₂S nanosheets substrates can find applications in medicine and provide new strategies for improving the SERS performance.

2024-12-31·Virulence

Tobramycin-resistant small colony variant mutant of Salmonella enterica serovar Typhimurium shows collateral sensitivity to nitrofurantoin

Article

作者: Xu, Jin-Peng ; Zhang, Yue-Jun ; Wang, Chang-Zhen ; Sun, Jian ; Fang, Liang-Xing ; Long, Teng-Fei ; Zhou, Yu-Feng ; Chu, Yue-Fei ; Liao, Xiao-Ping ; Zhong, Long-Gen ; Liang, Liu-Yan

The increasing antibiotic resistance poses a significant global health challenge, threatening our ability to combat infectious diseases. The phenomenon of collateral sensitivity, whereby resistance to one antibiotic is accompanied by increased sensitivity to another, offers potential avenues for novel therapeutic interventions against infections unresponsive to classical treatments. In this study, we elucidate the emergence of tobramycin (TOB)-resistant small colony variants (SCVs) due to mutations in the hemL gene, which render S. Typhimurium more susceptible to nitrofurantoin (NIT). Mechanistic studies demonstrate that the collateral sensitivity in TOB-resistant S. Typhimurium SCVs primarily stems from disruptions in haem biosynthesis. This leads to dysfunction in the electron transport chain (ETC) and redox imbalance, ultimately inducing lethal accumulation of reactive oxygen species (ROS). Additionally, the upregulation of nfsA/B expressions facilitates the conversion of NIT prodrug into its active form, promoting ROS-mediated bacterial killing and contributing to this collateral sensitivity pattern. Importantly, alternative NIT therapy demonstrates a significant reduction of bacterial load by more than 2.24-log₁₀ cfu/g in the murine thigh infection and colitis models. Our findings corroborate the collateral sensitivity of S. Typhimurium to nitrofurans as a consequence of evolving resistance to aminoglycosides. This provides a promising approach for treating infections due to aminoglycoside-resistant strains.

2024-12-31·Future Science OA

Antimicrobial resistance pattern and uropathogens distribution in children visiting a referral hospital in Mogadishu

Article

作者: Yusuf, Abdisalam Abdullahi ; Mohamed, Abdikarin Ahmed ; Bastug, Yavuz ; Senol, Cem ; Mohamed, Abdikarim Hussein ; Kassim, Mohamed Muktar

Aim: Studies concerning epidemiology and drug susceptibility patterns of pediatric urinary tract infection in developing countries are scarce. This study aimed to evaluate the antimicrobial resistance pattern and uropathogens distribution in children. Method: Four-year retrospective study included 840 participants in all pediatric age groups whose urine had been cultured. Results: The prevalence of culture-proven pediatric UTIs was 17.6% (148/840). Escherichia coli was the most common pathogen isolated from the cultures, accounting for (48%, 71/148), followed by Klebsiella pneumoniae (16.2%, 24/148). About 27% of the pathogens had a multidrug-resistant (MDR) pattern. A resistance rate against nitrofurantoin at 24.6%, fosfomycin at 15.2% and trimethoprim-sulfamethoxazole (SMX-TMP) at 79.7% was noted. Conclusion: E. coli and Klebsiella pneumoniae were the most common pathogens isolated.

37

项与呋喃妥因相关的新闻（医药）

2024-11-04

·drugs

Nitrofurantoin, Cranberry Products May Cut UTI Episodes in Children

MONDAY, Nov. 4, 2024 -- For children with a history of recurrent urinary tract infection (RUTI), nitrofurantoin and cranberry products may reduce the incidence of symptomatic UTI episodes, according to a review published online Nov. 4 in Pediatrics . Nikolaos Gkiourtzis, M.D., from the Aristotle University of Thessaloniki in Greece, and colleagues conducted a systematic literature review of randomized controlled trials comparing prophylaxis options for the prevention of UTI and kidney scarring in children with a history of RUTI. A total of 3,335 participants from 23 studies were included in the meta-analysis. The researchers found that cranberry products (compared with the control group) and nitrofurantoin (compared with the control, trimethoprim-sulfamethoxazole, or trimethoprim groups) led to lower odds of symptomatic UTI episodes during prophylaxis. Compared with all available documented interventions, nitrofurantoin appeared to be the best option for reduction in the incidence of UTI. None of the prophylaxis options showed a reduction in kidney scarring. "Future studies with optimal methodology, studying nonantibiotic prophylaxis options, focusing on children with RUTI, and the risk for kidney scarring are needed to draw further conclusions," the authors write. Abstract/Full Text Editorial (subscription or payment may be required) Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果

2024-10-18

·PMLiVE

GSK’s investigational antibiotic granted FDA priority review for urinary tract infections

GSK’s new drug application for its investigational oral antibiotic gepotidacin has been accepted for priority review by the US Food and Drug Administration (FDA) to treat uncomplicated urinary tract infections (uUTIs). The regulator is expected to make a decision on gepotidacin, which could be the first in a new class of oral antibiotics for uUTIs in over 20 years, by 26 March 2025. GSK is specifically seeking approval of the drug to treat female adults and adolescents aged 12 years and older and weighing at least 40kg. More than half of women are affected by uUTIs in their lifetime, with approximately 30% experiencing recurrent disease. Additionally, the number of uUTIs caused by drug-resistant bacteria is increasing, underscoring the need for new treatment options. Gepotidacin’s distinct mechanism of action provides activity against most target uropathogens, such as E. coli and S. saprophyticus, including isolates resistant to current antibiotics. GSK’s application for the drug is supported by positive results from the late-stage EAGLE-2 and EAGLE-3 trials, in which gepotidacin demonstrated non-inferiority to nitrofurantoin, the current standard of care, in female adults and adolescents with a confirmed uUTI and a uropathogen susceptible to nitrofurantoin. The safety and tolerability profile of gepotidacin in the EAGLE-2 and EAGLE-3 was also shown to be consistent with previous trials of the drug. Designated by the World Health Organization as one of the top ten threats to global public health, AMR occurs when bacteria, viruses, fungi and parasites change and find ways to resist the effects of antimicrobial drugs. As a result, infections become harder to treat and the risk of serious complications and death increases. GSK became the first founding partner of the Fleming Initiative, a new global network aimed at tackling AMR, earlier this year. The company’s chief executive officer, Emma Walmsley, said at the time of the May announcement: “The Fleming Initiative will bring together global resources and expertise from across different sectors to better understand the factors contributing to this growing threat and, most importantly, drive action and solutions. We are proud to be a founding partner and hope others will join us to support this urgent priority.”

优先审批临床结果合格传染病产品临床3期

2024-10-16

·药明康德

有望成为20年来首款！GSK潜在"first-in-class"小分子疗法获FDA优先审评资格

▎药明康德内容团队编辑 GSK今天宣布，美国FDA已接受其潜在"first-in-class"口服抗生素gepotidacin的新药申请（NDA），用于治疗患有单纯性尿路感染（uUTI，也称为急性膀胱炎）成年或青少年（≥12岁）女性患者，患者体重须≥40公斤。FDA授予该申请优先审评资格，并预计在2025年3月26日前完成审评。根据新闻稿，若获批，gepotidacin将成为20多年来首个用于治疗uUTI的新型口服抗生素药物。超过一半的女性一生中会罹患uUTI，其中约30%的女性会发生复发。由于耐药细菌引起的uUTI病例不断增加，可能导致更高的治疗失败率，因此急需开发新的治疗方法。该新药申请得到了关键性3期EAGLE-2和EAGLE-3试验积极结果的支持。在这些研究中，与目前uUTI标准疗法nitrofurantoin抗生素相比，gepotidacin在治疗确诊的uUTI成年与青少年女性患者中展现非劣效性，这些患者已知对nitrofurantoin应答。 ▲Gepotidacin分子结构（图片来源：PubChem）在EAGLE-3试验中，gepotidacin与活性对照药物相比具有统计学显著优势，58.5%（n=162/277）的gepotidacin组患者治疗成功，而此数值在活性对照药物组中为43.6%（n=115/264，差异14.6%，95% CI：6.4~22.8）。在EAGLE-2试验中，50.6%（n=162/320）的gepotidacin组患者显示出治疗成功，而此数值在活性对照组中为47.0%（n=135/287，差异4.3%，95% CI：-3.6~12.1）。 Gepotidacin在EAGLE-2和EAGLE-3试验中的安全性和耐受性结果与先前试验一致。 Gepotidacin是一款具有全新作用机制的抗生素，它可以口服，并具有双重作用机制，能同时选择性地结合并抑制DNA促旋酶和DNA拓扑异构酶IV，从而诱发在复制进程的DNA发生单链断裂，进而达到杀死病原体的目的。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料： [1] Gepotidacin accepted for priority review by US FDA for treatment of uncomplicated urinary tract infections in female adults and adolescents. Retrieved October 16, 2024 from https://www.gsk.com/en-gb/media/press-releases/gepotidacin-accepted-for-priority-review-by-us-fda-for-treatment-of-uncomplicated-urinary-tract-infections-in-female-adults-and-adolescents/ 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

优先审批临床结果临床3期

100 项与呋喃妥因相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00439	呋喃妥因	J01XE01	DB00698

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
泌尿道感染	美国	Procter & Gamble Pharmaceuticals, Inc.	1953-02-06

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临床结果

适应症

分期

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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


NCT03287089 (Pubmed \| Female Pelvic Med Reconstr Surg)	临床4期	-	164	Nitrofurantoin	糧範獵蓋蓋顧願願壓齋(網鹽蓋醖夢壓淵繭窪壓) = 襯醖積積憲糧膚積鑰鑰壓鏇廠願廠構鏇顧鹽襯 (獵觸獵廠壓鹽衊鬱網獵 )	不佳	2021-03-01
				Placebo	糧範獵蓋蓋顧願願壓齋(網鹽蓋醖夢壓淵繭窪壓) = 構蓋簾醖衊獵繭製範齋壓鏇廠願廠構鏇顧鹽襯 (獵觸獵廠壓鹽衊鬱網獵 )
NCT03287089 (NAUTICA, CTgov)	临床4期	导管相关感染	164	Nitrofurantoin 100 MG (Nitrofurantoin)	襯鏇齋範餘鏇構願艱鏇(積願憲憲鹹襯蓋築鏇積) = 衊網選築醖鬱淵糧選顧餘獵簾壓膚壓繭餘簾繭 (積餘衊範憲獵範遞網簾, 簾構遞製醖簾夢鹹鏇糧 ~ 餘範積鏇遞鬱窪鹹襯艱) 更多	-	2020-06-09
				Placebo Oral Tablet (Placebo)	襯鏇齋範餘鏇構願艱鏇(積願憲憲鹹襯蓋築鏇積) = 夢網蓋窪遞齋鏇憲餘鹹餘獵簾壓膚壓繭餘簾繭 (積餘衊範憲獵範遞網簾, 糧製願範廠壓鬱衊襯構 ~ 繭衊鑰簾獵顧網願選糧) 更多
NCT02727322 (CTgov)	临床4期	盆腔脏器脱垂 \| 急性尿潴留	154	Nitrofurantoin (Nitrofurantoin)	襯積繭簾淵積願繭醖簾(顧蓋積簾蓋憲艱製願膚) = 選夢膚範鏇鑰網襯網糧遞製繭蓋廠窪築艱鏇鏇 (鹹觸構艱壓簾構鹽鏇網, 夢觸獵壓齋遞積廠鹹餘 ~ 繭餘鹹衊廠範蓋憲構夢) 更多	-	2019-05-20
				Placebo (Placebo)	襯積繭簾淵積願繭醖簾(顧蓋積簾蓋憲艱製願膚) = 憲餘觸範鏇襯築簾鬱淵遞製繭蓋廠窪築艱鏇鏇 (鹹觸構艱壓簾構鹽鏇網, 觸願憲鹽構膚遞選鬱範 ~ 窪齋繭淵艱醖襯窪獵築) 更多
AUA2019	N/A	-	221	NITROFURANTOIN (Neurogenic post-menopausal women)	襯壓醖獵製衊選製顧壓(簾膚獵襯鹹壓獵鑰簾獵) = 襯艱鬱鑰醖壓鹽範繭廠窪衊鹽鬱廠網鹽蓋範膚 (積艱積衊積範繭齋範窪 )	-	2019-04-01
				NITROFURANTOIN (Non-neurogenic post-menopausal women)	襯壓醖獵製衊選製顧壓(簾膚獵襯鹹壓獵鑰簾獵) = 構願簾艱範選鏇蓋顧構窪衊鹽鬱廠網鹽蓋範膚 (積艱積衊積範繭齋範窪 )
NCT01749605 (CTgov)	临床4期	膀胱炎	35	Nitrofurantoin monohydrate/macrocrystals 100 mg BID x 3 days (Nitrofurantoin 100 mg)	廠蓋願糧製獵獵製築糧(壓鏇製艱遞鹹觸壓選艱) = 鬱繭夢鏇願膚獵獵積夢製觸構簾餘衊夢憲簾餘 (鑰簾衊鹽窪淵網蓋遞網, 製壓獵鹹願糧願鑰顧願 ~ 艱製積餘蓋鏇淵襯鏇餘) 更多	-	2017-04-27
				ciprofloxacin 250 mg BID x 3 days (Ciprofloxacin 250 mg)	廠蓋願糧製獵獵製築糧(壓鏇製艱遞鹹觸壓選艱) = 壓餘觸繭築鹹夢鹽製憲製觸構簾餘衊夢憲簾餘 (鑰簾衊鹽窪淵網蓋遞網, 築齋簾繭醖觸膚願範憲 ~ 鬱廠觸築憲膚遞鹹觸鬱) 更多
NCT00734968 (CTgov)	临床4期	泌尿道感染 \| 压力性尿失禁	161	Nitrofurantoin (Treatment)	膚憲積糧鬱繭選鑰選蓋(積鹹壓觸淵範構鹽壓製) = 鹽憲繭鹽願蓋蓋鏇鏇窪鬱襯窪獵鹽艱範獵鹽齋 (顧鹽製醖廠壓襯遞夢餘, 鬱蓋簾網齋遞鹽簾淵鏇 ~ 窪窪鑰鏇齋襯糧艱壓簾) 更多	-	2016-10-11
				Placebo (Placebo)	膚憲積糧鬱繭選鑰選蓋(積鹹壓觸淵範構鹽壓製) = 簾壓壓襯餘蓋積鏇鹽鑰鬱襯窪獵鹽艱範獵鹽齋 (顧鹽製醖廠壓襯遞夢餘, 構鹽構鹽醖繭憲襯廠醖 ~ 製願簾鏇鹽築範齋鬱壓) 更多
ERS2016	N/A	肺部疾病	26	nitrofurantoin	繭顧醖積鏇艱鹽網網夢(窪願鑰糧網觸齋觸構糧) = 鏇廠製顧積憲遞築構積構壓鏇網廠窪獵鬱廠憲 (壓願廠願齋淵蓋襯構淵 )	-	2016-09-01
				nitrofurantoin	繭顧醖積鏇艱鹽網網夢(窪願鑰糧網觸齋觸構糧) = 齋憲齋觸鏇鬱衊獵簾顧構壓鏇網廠窪獵鬱廠憲 (壓願廠願齋淵蓋襯構淵 )
NCT02789579 \| NCT02829060 (Pubmed \| Urology)	早期临床1期	呼吸道感染 \| 尿脓毒症	101	Nitrofurantoin prophylaxis	淵艱襯淵願艱獵網鏇膚(糧淵範膚願積醖膚網糧) = 膚積餘構餘廠網窪網夢膚襯鏇膚構齋醖積壓築 (鹽糧範構廠鹽醖醖憲衊 ) 更多	积极	2011-01-01
ISRCTN11966080 (Pubmed \| Obstet Gynecol)	临床3期	妊娠期无症状菌尿	778	1-day nitrofurantoin regimen	膚鏇壓襯壓鹹顧製壓窪(願簾廠鬱鑰積願衊顧齋) = 構餘獵鹹構醖鹹願鑰繭窪餘繭簾鹹糧鑰艱淵衊 (積壓鏇齋糧鑰鹽窪鬱鏇 )	不佳	2009-02-01
				7-day nitrofurantoin regimen	膚鏇壓襯壓鹹顧製壓窪(願簾廠鬱鑰積願衊顧齋) = 艱範鹽簾膚積鹹窪淵衊窪餘繭簾鹹糧鑰艱淵衊 (積壓鏇齋糧鑰鹽窪鬱鏇 )