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更新于：2026-10-17
Tobramycin
妥布霉素
更新于：2026-10-17
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1980-12-12), |
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C18H37N5O9 |
InChIKeyNLVFBUXFDBBNBW-PBSUHMDJSA-N |
CAS号32986-56-4 |
关联
132
项与 妥布霉素 相关的临床试验NCT07856355
Tobramycin Nebulization to Prevent Multidrug-Resistant Ventilator-Associated Pneumonia: A Prospective, Multicenter, Double-Blind, Randomized Controlled Trial
CTIS2024-516232-10-00
Defining Antibiotic Levels in Intensive care patients (DALI-2) protocol - A multi-national pharmacokinetic/pharmacodynamic cohort study to determine whether contemporary antibiotic dosing for critically ill patients achieves therapeutic exposures.
ChiCTR2600120598
Effects of general anesthesia combined with oxybuprocaine hydrochloride eye drops on oculocardiac reflex, agitation and pain during recovery period during strabismus surgery in children
100 项与 妥布霉素 相关的临床结果
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100 项与 妥布霉素 相关的转化医学
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100 项与 妥布霉素 相关的专利（医药）
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12,185
项与 妥布霉素 相关的文献（医药）2026-12-01MOLECULAR BIOLOGY REPORTS
Comparison the effect of Curcumin and methanolic extracts of Fraxinus excelsior L. and glycyrrhiza glabra L. on the expression of MexCD-OprJ and MexEF-OprN efflux pumps in multidrug resistant Pseudomonas aeruginosa clinical isolates
Article
作者: Goli, Hamid Reza ; Gholami, Mehrdad ; Jamal, Zeynab ; Ebrahimzadeh, Mohammad Ali
BACKGROUND:
Pseudomonas aeruginosa is a multidrug-resistant (MDR) pathogen, and efflux pumps such as MexCD-OprJ and MexEF-OprN play a key role in its antibiotic resistance. This study evaluated the putative effects of curcumin and methanolic extracts of F. excelsior L. and G. glabra L. on the expression of these efflux pumps, as well as their role in mediating antibiotic resistance.
METHODS AND RESULTS:
In this study, MDR P. aeruginosa clinical strains were used to determine the minimum inhibitory concentrations (MICs) of tobramycin and ciprofloxacin in the presence and absence of curcumin and selected plant extracts (F. excelsior L. and G. glabra L.) and curcumin. Real-time PCR was used to assess changes in efflux pump gene expression in tested strains. A significant positive correlation was identified between resistance to the tested antibiotics and increased expression of MexCD-OprJ and MexEF-OprN, as determined by Spearman's rank correlation using SPSS (p < 0.05). Treatment with the extracts, individually and in combination, resulted in a reduction in the expression levels of both efflux genes (p < 0.05), with the combined treatment showing the greatest effect. These findings were supported by colony count and turbidity assays, as evidenced by > 80% reduction in viable counts and decreased turbidity in treated groups.
CONCLUSION:
Overexpression of MexCD-OprJ and MexEF-OprN is a key factor contributing to MDR in P. aeruginosa. Treatment with curcumin, F. excelsior L. and G. glabra L. extracts-especially in combination, suggesting potential for suppression of efflux gene expression and enhanced antibiotic efficacy.
2026-12-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
PEGylation modulates the pulmonary behaviour and antibacterial efficacy of tobramycin liposomes in advanced in vitro lung models
Article
作者: Goñi-de-Cerio, Felipe ; de la Iglesia, Endika ; Nafarrate, Ibai ; Carregal-Romero, Susana ; Fernández-Méndez, Laura ; Carrillo-Romero, Juliana ; Sainz, Lourdes
Pulmonary infections caused by P. aeruginosa remain challenging to treat because physiological lung barriers limit antibiotic distribution and local availability at the site of infection. Here, we investigated how PEGylation influences the behaviour and antibacterial performance of tobramycin-loaded liposomes across distinct pulmonary microenvironments. Non-PEGylated (LP-TOB) and PEGylated (LP-PEG-TOB) liposomes were prepared, physicochemically characterised and compared with free tobramycin (TOB) using complementary in vitro assays and advanced alveolar and bronchial air-liquid interface co-culture models. Both liposomal formulations displayed suitable physicochemical properties, high colloidal stability and preserved antibacterial activity against P. aeruginosa. PEGylation significantly altered formulation behaviour by reducing epithelial uptake, increasing mucus-associated localisation and promoting faster tobramycin release. These differences resulted in microenvironment-dependent antibacterial responses following bacterial challenge. LP-PEG-TOB achieved greater control of extracellular bacterial burden than LP-TOB in both pulmonary models, with its distribution within the mucus compartment potentially contributing to its performance in the bronchial model. In contrast, LP-TOB demonstrated superior control of the intracellular bacterial signal in macrophages, consistent with its greater cellular interaction. All formulations were non-cytotoxic and attenuated infection-associated inflammatory responses. High-content imaging further revealed that antibiotic exposure mitigated infection-induced cellular and nuclear morphological alterations in macrophages. Overall, these findings demonstrate that PEGylation is a key determinant of liposome distribution and antibacterial performance across pulmonary microenvironments. This study provides a mechanistic basis for tailoring liposomal surface properties to the intended site of action in inhaled antibiotic therapy.
2026-12-01ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
Computational prioritization of megalin-aminoglycoside recognition and gentamicin-associated cellular stress responses
Article
作者: Millan-Pacheco, Cesar ; Benítez Cardoza, Claudia G ; Zamorano Carrillo, Absalom ; Castañeda-Villa, Norma ; Carrasco Sánchez, Luis Angel ; Lopez-Macay, Ámbar ; Serratos, Iris N ; Pérez-Hernández, Gerardo
BACKGROUND:
Aminoglycosides are effective antibiotics for severe infections, but their clinical use is limited by nephrotoxicity and ototoxicity resulting from drug accumulation in non-infected tissues. Megalin, an endocytic receptor expressed in renal proximal tubules and inner-ear tissues, has been proposed as a mediator of this uptake.
OBJECTIVE:
To evaluate whether the CR10 domain of human megalin constitutes a plausible aminoglycoside-recognition site and to prioritize compounds for experimental testing.
METHODS:
Seven aminoglycosides were comparatively analyzed in silico using docking and molecular dynamics simulations against megalin CR10. Gentamicin, which showed one of the most favorable predicted interaction profiles, was selected for biological evaluation. Cell viability was assessed in HEK293, HeLa, and U87MG cells, while calcium signaling and NF-κB activation were measured in HEK293 cells as indicators of cellular stress.
RESULTS:
Gentamicin reduced viability in a cell-type-dependent manner and induced calcium and NF-κB responses in HEK293 cells. Computational analyses suggested predominantly electrostatic interactions with megalin CR10, with gentamicin, tobramycin, and neomycin showing the most favorable predicted binding energies.
CONCLUSIONS:
The experimental and computational findings support a sequential in silico-to-in vitro workflow in which cellular assays define a gentamicin-associated stress phenotype, while molecular modeling identifies megalin CR10 as a structurally plausible aminoglycoside-recognition region that may contribute to tissue uptake or retention in organs expressing LRP2/megalin.
100 项与 妥布霉素 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 |
|---|---|---|---|
| 支气管扩张 | 中国 | 2022-10-11 | |
| 囊性纤维化 | 日本 | 2012-09-28 | |
| 囊性纤维化 | 日本 | 2012-09-28 | |
| 肺部感染 | 欧盟 | 2011-07-20 | |
| 肺部感染 | 冰岛 | 2011-07-20 | |
| 肺部感染 | 列支敦士登 | 2011-07-20 | |
| 肺部感染 | 挪威 | 2011-07-20 | |
| 肺部感染 | 英国 | 2011-07-20 | |
| 假单胞菌感染 | 美国 | 1997-12-22 | |
| 急性支气管炎 | 日本 | 1986-03-01 | |
| 膀胱炎 | 日本 | 1986-03-01 | |
| 出血性败血症 | 日本 | 1986-03-01 | |
| 腹膜炎 | 日本 | 1986-03-01 | |
| 肺炎 | 日本 | 1986-03-01 | |
| 肾盂肾炎 | 日本 | 1986-03-01 | |
| 脓皮症 | 日本 | 1986-03-01 | |
| 继发感染 | 日本 | 1986-03-01 | |
| 睑缘炎 | 日本 | 1981-12-07 | |
| 结膜炎 | 日本 | 1981-12-07 | |
| 角膜溃疡 | 日本 | 1981-12-07 |
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 |
|---|---|---|---|---|
| 白内障 | 临床3期 | 美国 | 2009-02-01 | |
| 铜绿假单胞菌感染 | 临床3期 | 立陶宛 | 2005-09-19 | |
| 眼部感染 | 临床3期 | 美国 | 2005-07-01 | |
| 术后并发症 | 临床3期 | 美国 | 2005-07-01 | |
| 非囊性支气管扩张 | 临床2期 | 比利时 | 2017-02-08 | |
| 非囊性支气管扩张 | 临床2期 | 法国 | 2017-02-08 | |
| 非囊性支气管扩张 | 临床2期 | 德国 | 2017-02-08 | |
| 非囊性支气管扩张 | 临床2期 | 意大利 | 2017-02-08 | |
| 非囊性支气管扩张 | 临床2期 | 西班牙 | 2017-02-08 | |
| 非囊性支气管扩张 | 临床2期 | 英国 | 2017-02-08 |
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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3期 | 854 | SDD prophylaxis | 窪獵網艱窪壓齋選選願(壓鹹構範襯獵鏇艱獵鑰) = 願鑰醖齋膚蓋築醖艱築 壓獵衊繭餘選遞築鑰鹽 (製淵鹽願糧範顧積願繭 ) | 积极 | 2025-12-04 | ||
N/A | 338 | Tobramycin eyedrops (Conservative management) | 膚壓鬱襯糧膚鹹鹽齋廠(醖糧願蓋壓鬱選繭築壓) = 齋鹽衊顧醖構網艱鏇製 獵觸積鹹糧遞顧齋鑰獵 (範襯夢艱夢鹹襯鏇鬱築 ) 更多 | 积极 | 2025-04-03 | ||
N/A | 13 | Tobramycin inhalation solution (TIS) 170 mg | 壓顧膚襯憲壓鹹艱鏇壓(積獵餘鏇淵糧遞選築憲) = one patient 糧餘齋獵醖鬱構餘築鏇 (夢簾觸選繭願鬱鑰醖襯 ) 更多 | 积极 | 2023-09-09 | ||
临床3期 | 11 | (Antibiotic) | 鏇築淵醖衊願製憲衊鑰 = 艱鏇齋糧鹹齋鏇齋襯糧 憲遞壓顧夢遞艱蓋築夢 (夢蓋範觸夢範餘獵鹹繭, 遞鏇觸餘艱遞願構鬱醖 ~ 築窪積鬱鏇壓獵餘觸夢) 更多 | - | 2023-06-15 | ||
Placebo: normal saline (Normal Saline) | 鏇築淵醖衊願製憲衊鑰 = 鬱鏇餘鹽艱艱簾願醖膚 憲遞壓顧夢遞艱蓋築夢 (夢蓋範觸夢範餘獵鹹繭, 願窪鬱糧製繭醖蓋襯廠 ~ 憲築憲範鑰網醖齋壓觸) 更多 | ||||||
临床4期 | 16 | Aerosolized Placebo (Aerosolized Placebo) | 壓夢醖憲簾醖夢鏇膚膚(構製繭鬱蓋構衊蓋廠觸) = 顧鏇淵齋鏇遞憲構顧鹽 醖壓膚衊醖鬱糧選觸鬱 (範繭積顧築構鬱構蓋範, 網遞襯窪顧憲鏇膚膚鹹 ~ 襯製醖製構憲糧簾鏇遞) 更多 | - | 2023-05-22 | ||
(Aerosolized Tobramycin or Vancomycin) | 壓夢醖憲簾醖夢鏇膚膚(構製繭鬱蓋構衊蓋廠觸) = 願窪壓窪鏇鏇鏇蓋齋鑰 醖壓膚衊醖鬱糧選觸鬱 (範繭積顧築構鬱構蓋範, 繭構構淵繭餘遞遞蓋顧 ~ 衊衊窪鬱鹹繭憲繭製憲) 更多 | ||||||
临床2/3期 | 非囊性支气管扩张 维持 | 58 | 艱醖鑰選繭觸壓築顧廠(顧醖蓋簾選觸鑰築餘遞): RR = 0.74 (95% CI, 0.49 ~ 1.14), P-Value = 0.15 | - | 2022-12-03 | ||
Placebo | |||||||
临床4期 | 51 | (Standard Colistin Arm) | 範範鹽遞鬱糧鹽壓糧壓(壓構廠壓壓窪繭網願夢) = 網願憲顧鏇範選製餘築 夢構鑰獵壓顧築齋簾膚 (鹽鬱齋鏇繭繭簾膚廠製, 9.5) 更多 | - | 2022-10-06 | ||
(Modified Colistin Arm) | 範範鹽遞鬱糧鹽壓糧壓(壓構廠壓壓窪繭網願夢) = 糧齋遞網艱餘遞糧鬱選 夢構鑰獵壓顧築齋簾膚 (鹽鬱齋鏇繭繭簾膚廠製, 3.0) 更多 | ||||||
临床1/2期 | 19 | (Tobramycin Topical Antibiotic Nasal Saline Rinse) | 鏇簾憲齋艱餘遞鏇鏇餘 = 憲齋膚選範壓選範鹽醖 衊鹽網鹹選艱襯鏇襯蓋 (鏇襯遞淵構製憲觸遞廠, 憲遞艱製顧願繭鬱積衊 ~ 遞夢獵簾積鹹壓選觸願) 更多 | - | 2022-04-20 | ||
(Levofloxacin Topical Antibiotic Nasal Saline Rinse) | 鏇簾憲齋艱餘遞鏇鏇餘 = 糧鬱鑰淵齋襯齋鏇獵範 衊鹽網鹹選艱襯鏇襯蓋 (鏇襯遞淵構製憲觸遞廠, 窪獵築夢選鹹網艱鹹憲 ~ 夢衊鑰築餘壓淵構願壓) 更多 | ||||||
临床4期 | - | 20 | Tobramycin+Vancomycin (Intraarticular Concentrations of Tobramycin and Vancomycin) | 憲廠願窪鬱膚選淵窪鑰(鬱餘夢窪夢選艱繭壓糧) = 醖選蓋鏇艱蓋淵憲壓遞 鹽膚窪蓋製獵簾鹽鏇觸 (壓蓋襯製選糧築窪醖獵, 夢構築窪醖選鹹蓋顧廠 ~ 淵製鹽醖範構鑰簾衊鏇) 更多 | - | 2021-10-05 | |
Tobramycin+Vancomycin (Vancomycin and Tobramycin Serum Concentration) | 鹹鬱糧餘蓋蓋餘選廠構(憲觸簾顧醖簾窪積築廠) = 獵壓餘醖窪範遞構鬱淵 襯繭願獵齋獵獵繭壓鹹 (製窪襯築鬱築膚網製艱, 鏇繭鬱遞醖蓋築膚築願 ~ 齋鏇獵選齋醖簾糧繭鏇) 更多 | ||||||
临床3期 | 49 | 壓餘觸構夢構艱鬱觸鹽 = 築願繭獵壓壓蓋遞壓廠 齋鑰艱築範齋醖廠鑰遞 (積襯網夢製鑰鏇憲醖獵, 襯顧網齋鹹蓋鹹積願鏇 ~ 範鏇繭顧鏇鏇製積選糧) 更多 | - | 2021-06-02 |
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