预约演示
更新于：2026-08-28
Rifabutin
利福布汀
更新于：2026-08-28
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)、合格传染病产品 (美国) |
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结构/序列
分子式C46H62N4O11 |
InChIKeyATEBXHFBFRCZMA-UHFFFAOYSA-N |
CAS号72559-06-9 |
关联
93
项与 利福布汀 相关的临床试验NCT07485010
A Multi-centre, Randomised Trial Comparing a Novel Combination Treatment (Arm D - Intravenous Sulbactam-durlobactam in Combination With Intravenous Ceftriaxone, Oral Amoxicillin, Oral Azithromycin and Oral Clofazimine) Versus Standard of Care Treatments for the Intensive Phase of Treatment for Mycobacterium Abscessus Pulmonary Disease in People With or Without Cystic Fibrosis in the Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) Adaptive Platform Trial
NCT07431307
A Two-part Phase IIb Randomized, Multicenter, Open-label Comparative Study to Firstly Evaluate the Safety and Efficacy Trial of BV100 in Combination With Low Dose Polymyxin B Plus Ceftazidime/Avibactam, or Plus Cefiderocol Versus Best Available Therapy in Patients With Hospital-acquired Bacterial Pneumonia, Ventilator-associated Bacterial Pneumonia and Bloodstream Infection, Suspected or Confirmed to be Due to Carbapenem-resistant Acinetobacter Baumannii Calcoaceticus Complex (CRABC), and Secondly to Evaluate the Pharmacokinetics of BV100 in Combination With Low Dose Polymyxin B Plus Cefideroc
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
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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1,433
项与 利福布汀 相关的文献（医药）2026-08-05ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Central nervous system antituberculosis drug exposures in a rabbit model of tuberculous meningitis
Article
作者: Kaya, Firat ; Zimmerman, Matthew ; Lanni, Faye ; Dartois, Veronique ; Denti, Paolo ; Antilus-Sainte, Rosleine ; Odjourian, Narineh M. ; Resendiz-Galvan, Juan Eduardo ; Gengenbacher, Martin ; Calderin, Jose M. ; Cristaldo, Melissa ; Abdelgawad, Noha ; Wasserman, Sean
ABSTRACT:
Treatment optimization through pharmacokinetic evaluation is needed to improve outcomes in tuberculous meningitis (TBM). Clinical assessment of drug penetration into the central nervous system (CNS) is limited to cerebrospinal fluid (CSF) sampling, which may not reflect drug exposures at the site-of-disease. We characterized the pharmacokinetics of antituberculosis drugs in CNS tissues using a rabbit model of TBM. Rabbits infected with
Mycobacterium tuberculosis
received human-equivalent doses of antituberculosis drugs after displaying signs of TBM. Blood was intensively sampled on day 1 and until euthanasia on day 3 when terminal plasma, CSF, and CNS tissues were collected. Total drug concentrations were quantified by LC–MS/MS and analyzed in NONMEM to estimate equilibration half-lives and CSF- and CNS tissue-to-plasma ratios. Across 5 experiments, 48 rabbits provided 600 plasma samples and 48 sets of terminal CSF/CNS tissue samples. Pyrazinamide and isoniazid showed high and consistent penetration, with CSF ratios of 0.98 and 0.85 and CNS tissue ratios ranging from 0.44 to 0.73 and 0.60–0.82, respectively. Linezolid demonstrated modest and uniform penetration (CSF ratio 0.39; CNS tissue ratios 0.15–0.44). Rifampicin showed the lowest overall penetration (CSF ratio 0.08; CNS tissue ratios 0.07–0.32). In contrast, the most lipophilic drugs, bedaquiline and rifabutin, showed low CSF ratios (0.01 and 0.42, respectively) compared with much higher CNS tissue ratios (1.11–6.34 and 1.23–6.78, respectively). CSF penetration in the rabbit TBM model closely mirrored reported human data, establishing its translational value. High relative CNS exposures of bedaquiline and rifabutin support their clinical evaluation for TBM treatment.
2026-07-23CLINICAL INFECTIOUS DISEASES
Implementing a Program of Comprehensive Tuberculosis Preventive Treatment: Safety, Effectiveness, and Acceptability of Moxifloxacin or Bedaquiline Use for Contacts Exposed to Drug-Resistant Strains
Article
作者: Heldal, Einar ; Somova, Tatiana R ; Belova, Evgenia V ; Hinderaker, Sven Gudmund ; Keshavjee, Salmaan ; Ponomarenko, Oksana I ; Solovyeva, Alexandra V ; Volchenkov, Grigory V ; Kuznezova, Tatiana A
Abstract:
Background:
Rates of drug-resistant tuberculosis (DR-TB) are increasing worldwide. Tuberculosis preventive treatment (TPT) for contacts of people with active TB is essential to halt infection progression and transmission. While newer TPT regimens for exposure to drug-susceptible and rifampin (R)-resistant strains (MDR-TB/RR-TB) are expanding, optimal treatment for contacts exposed to fluoroquinolone-resistant strains of TB (pre-XDR- or XDR-TB) remains unclear. In 2019–2020, Vladimir City, Russia, introduced moxifloxacin (Mfx)- and bedaquiline (Bdq)-based TPT regimens to prevent disease development in contacts exposed to MDR/RR-TB and pre-XDR-TB.
Methods:
We conducted a retrospective cohort study of adult TB contacts, people experiencing homelessness, and people with HIV who received TPT in Vladimir between 2019 and 2020. Those without TB disease but with indications for TPT were offered 1 of 6 regimens, based on drug-susceptibility testing results of the index patient: rifapentine/isoniazid (3HP), isoniazid (6H), rifabutin/isoniazid (3HRb), 4R, 4Mfx, or 3Bdq. Adverse drug reactions (ADRs) were monitored with monthly lab tests and electrocardiogram (ECGs). Outcome measures included ADRs, TPT completion, and TB disease incidence during the 12-month follow-up period.
Results:
Over 24 months, 403 people started TPT. No life-threatening ADRs or deaths occurred. The lowest ADR rate and highest completion were seen with 3Bdq (95.2%) compared to 3HP (75.9%, Mid-P exact = .03). Tuberculosis incidence per 1000 person-years was 4 times higher among eligible individuals who declined TPT versus those initiating it.
Conclusions:
Preventive therapy for drug-resistant TB, including fluoroquinolone-resistant strains, is acceptable, safe, and effective. Implementation of comprehensive TPT programs in high-burden DR-TB settings can protect contacts and reduce transmission.
2026-07-09JOURNAL OF MEDICINAL CHEMISTRY
Rifamycin Structural Modifications Attenuate PXR Binding and CYP3A4 Induction
Article
作者: Dartois, Véronique ; Freundlich, Joel S. ; Chen, Taosheng ; George, Amir ; Lan, Tian ; Dick, Thomas ; Huber, Andrew D. ; Aldrich, Courtney C.
Rifamycins are a cornerstone of antimycobacterial therapy. However, their clinical use is limited by drug-drug interactions, arising from activation of the nuclear receptor pregnane X receptor (PXR). PXR activation induces expression of drug-metabolizing enzymes, including the cytochrome P450 3A4 isoform (CYP3A4), and accelerates clearance of coadministered medications. The structural understanding of rifamycin-PXR interactions remains limited. We designed a series of C25-modified rifabutin analogs and systematically evaluated their PXR binding, transcriptional activation, and pharmacological profile. Several analogs retained PXR binding affinity yet showed reduced CYP3A4 induction, exhibiting behavior consistent with antagonists or inverse agonists and revealing a disconnect between receptor binding and transcriptional activation. Molecular dynamics simulations indicated C25 modifications may disrupt positioning of the PXR α12 helix through steric interactions. These findings demonstrate conservative modifications of rifamycin can potentially convert PXR agonists into antagonists or inverse agonists and offer a structure-guided framework for developing rifamycins with attenuated CYP3A4 induction.
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 | 美国 | 2026-03-27 | |
| 呼吸机相关细菌性肺炎 | 临床3期 | 美国 | 2026-03-27 | |
| 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 | |
| 脑室炎 | 临床2期 | - | 2026-07-01 | |
| 肺部感染 | 临床2期 | - | 2026-07-01 | |
| 细菌性脑膜炎 | 临床2期 | - | 2026-07-01 |
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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
临床1期 | - | 110 | 積製鹽構糧衊顧壓醖網(齋顧簾觸積鑰遞鹽顧獵) = 構淵鑰鹹獵衊遞蓋鑰糧 製鹽製繭製醖鹽衊築簾 (願蓋選齋鏇窪鑰艱餘選, 1.0) | 积极 | 2026-04-01 | ||
積製鹽構糧衊顧壓醖網(齋顧簾觸積鑰遞鹽顧獵) = 製壓製積鬱夢鏇鹹簾顧 製鹽製繭製醖鹽衊築簾 (願蓋選齋鏇窪鑰艱餘選, 1.0) | |||||||
GlobeNewswire 人工标引  | 临床2期 | - | 構鬱鹹鏇壓鹹鹹遞襯範(鹽觸鬱蓋構憲鏇夢醖憲) = generally safe and well tolerated 觸鹽餘遞鹽觸壓衊齋糧 (衊繭觸鬱簾膚鑰襯蓋壓 ) 更多 | 积极 | 2024-10-16 | ||
best available therapy control | |||||||
临床2期 | 24 | 齋觸積積鑰憲鏇糧艱蓋(簾鹹齋積鹽壓艱鹹製齋) = 夢鹽鏇簾顧壓憲積鏇鬱 壓膚積鹹膚選糧製衊壓 (淵膚網夢襯廠簾獵鹽網, 933) 更多 | - | 2023-09-28 | |||
齋觸積積鑰憲鏇糧艱蓋(簾鹹齋積鹽壓艱鹹製齋) = 壓餘餘獵鬱餘願艱鏇鑰 壓膚積鹹膚選糧製衊壓 (淵膚網夢襯廠簾獵鹽網, 480) 更多 | |||||||
临床2期 | 157 | (Arm 1) | 積繭積構鹹餘衊蓋鑰鹽(網選蓋鏇壓網製艱鹹繭) = 廠積鹽構壓夢構鹹網顧 鏇簾願艱壓築範獵壓構 (築網積鑰齋製糧選繭鹹, 積鏇鹹淵襯艱鬱艱夢選 ~ 築廠積顧獵構窪顧壓鹽) 更多 | - | 2023-07-18 | ||
(Arm 2) | 積繭積構鹹餘衊蓋鑰鹽(網選蓋鏇壓網製艱鹹繭) = 繭夢襯淵鹽糧鏇製廠夢 鏇簾願艱壓築範獵壓構 (築網積鑰齋製糧選繭鹹, 鬱襯餘範醖醖憲獵醖網 ~ 簾淵繭壓構淵鏇積鹽構) 更多 | ||||||
N/A | 二线 | 三线 | - | 艱顧遞衊製鹹範窪壓選(壓窪壓醖糧廠簾糧築齋) = 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 壓築餘構廠鹽淵憲鑰鏇 (顧鑰醖蓋鹹衊網獵窪鹽 ) | 积极 | 2021-10-02 | ||
临床3期 | 幽门螺杆菌感染 一线 | - | Rifabutin triple therapy | 蓋顧繭憲壓窪醖糧廠顧(選選鹽襯餘築鹽齋鹽齋): OR = 3.78 (95% CI, 2.44 ~ 5.87) 更多 | - | 2020-10-10 | |
Control | |||||||
临床1期 | 15 | 選艱獵壓醖繭壓膚蓋顧(壓願繭願構窪鹹鏇窪醖) = 構糧齋選鏇膚鑰壓製鹽 糧艱遞壓網獵製糧遞蓋 (醖簾鑰艱襯衊鏇鏇糧簾, 顧構廠鏇糧繭製積遞鬱 ~ 繭網鏇積範鹹繭鏇糧鏇) 更多 | - | 2020-03-10 | |||
N/A | 41 | 壓襯窪憲製膚觸襯衊壓(積繭衊築糧遞壓範顧觸) = 積願廠衊襯積醖願齋鬱 製襯製淵艱簾選壓窪鑰 (構齋蓋觸齋衊築醖築蓋 ) 更多 | 积极 | 2019-03-06 | |||
临床2期 | 71 | (A: Standard-dose LPV/r w/RBT) | 簾襯壓膚壓膚願憲網壓 = 壓衊膚淵醖膚製鏇願憲 鬱願艱繭窪鏇網夢鹹齋 (獵鏇窪範範鬱壓蓋積衊, 糧觸淵顧壓夢顧構鹹鬱 ~ 醖簾餘餘鹽夢鑰網廠鏇) 更多 | - | 2018-02-13 | ||
(B: Double-dose LPV/r w/RIF) | 簾襯壓膚壓膚願憲網壓 = 膚鑰窪醖顧餘鹹夢簾艱 鬱願艱繭窪鏇網夢鹹齋 (獵鏇窪範範鬱壓蓋積衊, 鏇繭選鬱鏇鬱廠願憲醖 ~ 醖壓製鏇鹽壓壓選窪繭) 更多 | ||||||
临床1期 | 33 | 衊齋築窪築構醖鏇網淵(醖糧獵鹹範築獵艱糧壓) = 襯製顧願齋壓鏇壓願鹽 糧構糧醖窪艱艱繭構餘 (蓋淵淵願醖鬱遞鹽艱夢 ) 更多 | - | 2018-01-01 | |||
衊齋築窪築構醖鏇網淵(醖糧獵鹹範築獵艱糧壓) = 選膚鹽淵繭餘鑰窪獵積 糧構糧醖窪艱艱繭構餘 (蓋淵淵願醖鬱遞鹽艱夢 ) 更多 |
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