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更新于：2026-01-28
Rifabutin
利福布汀
更新于：2026-01-28
概要
基本信息
药物类型 小分子化药 |
别名 1,4-Dihydro-1-deoxy-1',4-didehydro-5'-(2-methylpropyl)-1-oxorifamycin XIV、4-Deoxo-3,4-(2-spiro(N-isobutyl-4-piperidyl)-2,5-dihydro-1H-imidazo)-rifamycin S、4-N-isobutylspiropiperidylrifamycin S + [12] |
靶点 |
作用方式 抑制剂 |
作用机制 RNAP抑制剂(细菌DNA指导的RNA聚合酶复合体抑制剂) |
在研适应症 |
非在研适应症 |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1992-12-23), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C46H62N4O11 |
InChIKeyATEBXHFBFRCZMA-UHFFFAOYSA-N |
CAS号72559-06-9 |
关联
83
项与 利福布汀 相关的临床试验NCT07326540
A Phase 3 Prospective, Randomized, Multicenter, Active-controlled Study to Evaluate the Efficacy and Safety of BV100 Plus Low-dose Polymyxin B Compared With Colistin Plus High-dose Ampicillin/Sulbactam in the Treatment of Adult Patients With Hospital-acquired Bacterial Pneumonia and Ventilator-associated Bacterial Pneumonia Caused by Carbapenem-resistant Acinetobacter Baumannii-calcoaceticus Complex
NCT07199452
An Open-Label Clinical Study to Evaluate the Effects of Multiple Oral Doses of Rifabutin on the Single-Dose Pharmacokinetics of MK-4646 in Healthy Participants
NCT07066722
A Phase 1, Open-Label Study to Evaluate the Relative Bioavailability and the Effect of Food on VH4524184 Tablet Formulations, and to Evaluate the Potential for VH4524184 Drug-Drug-Interactions in Healthy Adult Participants
100 项与 利福布汀 相关的临床结果
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100 项与 利福布汀 相关的转化医学
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100 项与 利福布汀 相关的专利（医药）
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1,331
项与 利福布汀 相关的文献（医药）2026-01-22JOURNAL OF MEDICINAL CHEMISTRY
Design, Synthesis, and Biological Evaluation of Acid-Responsive Bifunctional Molecules with Dual Anti-
Helicobacter pylori
and Acid Suppression Activities
Article
作者: Xing, Gang ; Yang, Jianuo ; Zhang, Rong ; Cheng, Maosheng ; Yang, Huali ; Xia, Mingyu ; Hu, Xingqi ; Li, Hao ; Xu, Hanqing ; Wang, Ting ; Wen, Rui ; Ding, Canyao ; Zheng, Jiang ; Liu, Yang
The increasing antibiotic resistance of Helicobacter pylori necessitates novel therapeutics. Although rifabutin demonstrates potent anti-H. pylori activity and low resistance rates, its clinical use is limited by myelosuppressive risk. Clinical evidence indicates that vonoprazan acts synergistically with rifabutin, allowing a reduced dosage and duration while maintaining efficacy. We developed acid-responsive bifunctional molecules conjugating both drugs for coordinated gastric release and enhanced local synergy, enabling reduced-dose or shorter-duration therapy with minimal adverse effects. Compound 10, incorporating acid-labile silyl ether and self-immolative linkers, demonstrated potent anti-H. pylori activity (MIC ≤ 0.125 μg/mL) and strong acid suppression (>85% inhibition at 2 mg/kg). In murine models, compound 10 exhibited antiulcer efficacy comparable to vonoprazan at half the dose, with pharmacokinetic analysis revealing minimal systemic exposure to rifabutin, thereby substantially reducing the risk of myelosuppression. This strategy provides a promising approach for effective and safe H. pylori therapy.
2026-01-15Gut and Liver
Establishing Epidemiological Cutoff Values for
Helicobacter pylori
Strains in Korea: A Model-Based Analysis of Antibiotic Resistance Patterns
Article
作者: Ahn, Ji Yong ; Gong, Eun Jeong ; Lee, Sun Mi ; Jung, Hwoon-Yong ; Jeon, Seong Woo ; Kwon, Yong Hwan ; Choi, Kee Don ; Lee, Jeong Hoon ; Noh, Jin Hee ; Kim, Jung Mogg
Background/Aims:
The absence of standardized clinical minimum inhibitory concentration (MIC) breakpoints for Helicobacter pylori infection has resulted in inconsistent resistance definitions, even within the same research group in Korea. Therefore, establishing epidemiological cutoff values (ECOFFs) is essential for standardization.
Methods:
The MIC distributions for antibiotics commonly used against H. pylori infection in South Korea were analyzed from 2015 to 2023. A total of 5,925 primary H. pylori isolates were collected from five data sources, and MIC values were determined using the serial 2-fold agar dilution method. The ECOFFinder program was used to establish ECOFFs for six antibiotics.
Results:
The tentative ECOFFs for amoxicillin and clarithromycin were 0.125 μg/mL. The ECOFFs for levofloxacin, metronidazole, and tetracycline were 0.5, 8.0, and 0.25 μg/mL, respectively. The ECOFF for rifabutin could not be determined due to insufficient data. On the basis of these ECOFFs, the resistance rate was 17.9% for amoxicillin, 31.9% for clarithromycin, 40.9% for levofloxacin, 24.7% for metronidazole, and 11.5% for tetracycline.
Conclusions:
This comprehensive analysis defined regional antibiotic resistance patterns and established Korea-specific ECOFFs, providing a foundation for determining clinical breakpoints and optimizing H. pylori eradication strategies.
2026-01-15Gut and Liver
Superior Efficacy of Bismuth-Containing Rifabutin Quadruple Therapy over Rifabutin Triple Therapy as Salvage Treatment
Article
作者: Kwon, Kwang An ; Lee, Hannah ; Chung, Jun-Won ; Kim, Jung Ho ; Kim, Kyoung Oh
Background/Aims:
Helicobacter pylori is a pathogen that causes chronic gastritis and peptic ulcer diseases and is a carcinogen responsible for the development of malignancies, including gastric cancer. In the current era of high antimicrobial resistance, rifabutin-based triple therapy is recommended as a salvage therapy. Bismuth has not only a strong bacteriostatic effect but also a synergic effect when combined with antibiotics. Our study aimed to compare and evaluate the eradication rates between rifabutin-based triple therapy and rifabutin with bismuth-containing quadruple therapy as salvage treatments.
Methods:
In this single-center study, patients who received rifabutin-based triple therapy and rifabutin with bismuth-containing quadruple therapy after failure of conventional therapy, including first- and second-line treatment, between January 2016 and July 2024, were retrospectively investigated. A total of 53 patients who received rifabutin-based triple therapy and 50 who received bismuth-containing quadruple therapy were included.
Results:
In the rifabutin-based triple therapy group, eradication was achieved in 32 out of 53 patients (60.4%; 95% confidence interval [CI], 46.8% to 74.0%). In the bismuth-containing quadruple therapy group, eradication was achieved in 40 out of 50 patients (80.0%; 95% CI, 68.5% to 91.5%), demonstrating significant therapeutic benefit (p=0.030). Adverse events, including nausea, epigastric discomfort, and lethargy, were significantly more frequent in the bismuth-containing quadruple therapy group (p=0.007), but they were mild and tolerable enough not to affect compliance (p=0.329).
Conclusions:
Rifabutin with bismuth-containing quadruple regimen as a salvage treatment achieved significantly superior eradication efficacy over the rifabutin-based triple regimen. Further multicenter prospective studies are needed to provide additional supporting evidence.
100 项与 利福布汀 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 |
|---|---|---|---|
| 细胞内鸟分枝杆菌感染 | 日本 | 2008-07-16 | |
| 耐多药结核病 | 中国 | 2007-12-28 | |
| 非结核分枝杆菌感染 | 美国 | 1992-12-23 |
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 |
|---|---|---|---|---|
| 医院获得性细菌性肺炎 | 临床3期 | - | 2026-03-20 | |
| 呼吸机相关细菌性肺炎 | 临床3期 | - | 2026-03-20 | |
| 获得性免疫缺陷综合征 | 临床3期 | 美国 | 2001-08-31 | |
| 菌血症 | 临床3期 | 美国 | 2001-08-31 | |
| HIV感染 | 临床3期 | 美国 | 2001-08-31 | |
| 真菌病 | 临床3期 | 美国 | 2001-08-31 | |
| 结核 | 临床3期 | 美国 | 1984-06-01 | |
| 鲍氏不动杆菌感染 | 临床1期 | 中国 | 2025-10-21 | |
| 鲍氏不动杆菌感染 | 临床1期 | 中国 | 2025-10-21 | |
| 脓毒症 | 临床1期 | 中国 | 2025-10-21 |
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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
GlobeNewswire 人工标引  | 临床2期 | - | 廠夢齋廠願衊遞窪鏇膚(醖遞齋範範鬱壓淵積觸) = generally safe and well tolerated 醖蓋餘夢簾淵積齋網齋 (憲蓋壓鬱選網憲餘簾繭 ) 更多 | 积极 | 2024-10-16 | ||
best available therapy control | |||||||
临床2期 | 24 | 願顧夢遞憲壓簾網憲願(窪醖鑰襯繭齋願觸選壓) = 鏇構蓋積膚鏇膚鏇糧齋 艱觸廠獵鑰淵糧鏇艱鑰 (膚糧壓選鹽鬱觸糧窪衊, 933) 更多 | - | 2023-09-28 | |||
願顧夢遞憲壓簾網憲願(窪醖鑰襯繭齋願觸選壓) = 壓顧壓艱廠膚積繭願鑰 艱觸廠獵鑰淵糧鏇艱鑰 (膚糧壓選鹽鬱觸糧窪衊, 480) 更多 | |||||||
临床2期 | 157 | (Arm 1) | 鹽網遞醖選鹽憲遞製鏇(選選鹽顧繭齋製觸鹽顧) = 範鏇觸鏇膚築夢憲遞鹹 鏇鑰鏇網築膚遞築顧願 (範衊壓獵選築獵築鹹網, 鹽廠鑰壓遞襯網鹹製艱 ~ 鑰鏇鑰廠糧鬱艱網鹽繭) 更多 | - | 2023-07-18 | ||
(Arm 2) | 鹽網遞醖選鹽憲遞製鏇(選選鹽顧繭齋製觸鹽顧) = 壓網醖製醖積繭構夢艱 鏇鑰鏇網築膚遞築顧願 (範衊壓獵選築獵築鹹網, 鑰憲築艱窪遞願鏇顧鹽 ~ 衊範鏇範淵鬱鬱餘簾鬱) 更多 | ||||||
N/A | 二线 | 三线 | - | 壓積網繭鬱鏇簾襯鹽獵(醖製製糧蓋淵鬱糧夢觸) = At least one adverse event was registered in 28% of the patients (most frequently nausea and asthenia) and one serious adverse event (0.2%) was reported in one patient with leucopenia and thrombopenia with fever requiring hospitalisation 簾衊餘壓簾顧顧遞淵夢 (鏇壓範壓糧繭鏇壓憲醖 ) | 积极 | 2021-10-02 | ||
临床3期 | 幽门螺杆菌感染 一线 | - | Rifabutin triple therapy | 艱壓襯糧鹹鏇鹽膚餘鑰(夢襯膚鹹醖製顧憲醖鑰): OR = 3.78 (95% CI, 2.44 ~ 5.87) 更多 | - | 2020-10-10 | |
Control | |||||||
临床1期 | 15 | 夢鹹鬱餘醖衊範鑰鬱膚(蓋憲製窪淵壓糧製憲顧) = 遞範鏇觸廠顧憲膚鹽鬱 淵構築醖衊積製夢範遞 (糧顧繭鏇糧選鏇觸顧蓋, 醖鹽壓積鏇壓鬱廠製鬱 ~ 鏇構遞憲簾廠繭觸憲築) 更多 | - | 2020-03-10 | |||
临床2期 | 71 | (A: Standard-dose LPV/r w/RBT) | 醖選獵鹽廠鹽構壓蓋壓 = 憲膚構範鹹鑰壓願觸餘 窪築夢鏇膚艱夢繭遞遞 (鬱鏇鑰鹽膚糧範淵衊蓋, 鹽築網構製積網糧顧鹹 ~ 鏇顧觸憲顧築壓夢鹽衊) 更多 | - | 2018-02-13 | ||
(B: Double-dose LPV/r w/RIF) | 醖選獵鹽廠鹽構壓蓋壓 = 簾選窪衊選鹽艱範選窪 窪築夢鏇膚艱夢繭遞遞 (鬱鏇鑰鹽膚糧範淵衊蓋, 衊夢鑰遞夢顧選觸淵淵 ~ 範憲糧膚積鏇網遞憲鹽) 更多 | ||||||
临床1期 | 33 | 鏇蓋構衊網憲遞鏇襯鏇(艱鬱鹹艱遞鹽積築衊獵) = 鹽觸積壓廠構鹹選鏇網 糧餘網觸鬱餘衊鹹積餘 (範願獵鏇繭鏇積鬱築願 ) 更多 | - | 2018-01-01 | |||
鏇蓋構衊網憲遞鏇襯鏇(艱鬱鹹艱遞鹽積築衊獵) = 窪廠醖觸鏇網夢壓鏇膚 糧餘網觸鬱餘衊鹹積餘 (範願獵鏇繭鏇積鬱築願 ) 更多 | |||||||
临床2期 | 12 | (Rifabutin) | 淵鏇鹽獵艱壓夢遞餘壓 = 繭構壓襯製顧壓憲廠觸 鑰蓋淵範襯鹹繭願簾觸 (壓積築憲壓壓糧構醖襯, 網鑰鏇構壓糧獵醖窪蓋 ~ 襯簾餘願糧糧衊鏇鬱範) 更多 | - | 2014-04-21 | ||
淵鏇鹽獵艱壓夢遞餘壓 = 願醖鏇繭醖鬱窪簾鏇顧 鑰蓋淵範襯鹹繭願簾觸 (壓積築憲壓壓糧構醖襯, 糧蓋壓餘選糧夢鹹廠鬱 ~ 遞鹹窪齋構衊構餘構構) 更多 | |||||||
临床3期 | - | 襯夢衊積艱齋蓋艱獵齋(壓築製選獵築構淵願鹹) = 鹹醖構鹽顧醖壓遞選鹹 衊鹹鹹構膚範觸齋膚淵 (餘齋淵選窪淵憲艱襯齋, 92.1 ~ 101) | - | 2006-02-15 | |||
襯夢衊積艱齋蓋艱獵齋(壓築製選獵築構淵願鹹) = 積蓋簾選積網鏇顧範願 衊鹹鹹構膚範觸齋膚淵 (餘齋淵選窪淵憲艱襯齋, 82 ~ 98.6) |
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