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更新于：2025-07-15
Tedizolid Phosphate
磷酸特地唑胺
更新于：2025-07-15
概要
基本信息
药物类型 小分子化药 |
别名 Tedizolid、Tedizolid phosphate (JAN/USAN)、Torezolid + [19] |
作用方式 抑制剂 |
作用机制 50S subunit抑制剂(50S核糖体亚基抑制剂)、蛋白质生物合成抑制剂 |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2014-06-20), |
最高研发阶段(中国)批准上市 |
特殊审评特殊审批 (中国) |
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结构/序列
分子式C17H16FN6O6P |
InChIKeyQCGUSIANLFXSGE-GFCCVEGCSA-N |
CAS号856867-55-5 |
关联
66
项与 磷酸特地唑胺 相关的临床试验NCT06609161
A Study to Evaluate the Definitive Bioequivalence of Tedizolid Phosphate Single-Unit-Dose Sachet Powder for Oral Suspension Compared to Tedizolid Phosphate Powder for Oral Suspension Bottle Used in Pediatric Clinical Studies
CTR20242122
一项随机、开放、两序列交叉设计，评价健康成人空腹/餐后状态下单次口服磷酸特地唑胺片的生物等效性试验
CTRI/2023/12/060921
A Phase III, Prospective, Randomized, Double Blind, Double Dummy, Active Controlled, Comparative, Parallel Group, Multicenter Clinical Study to Evaluate the Efficacy, Safety and Tolerability of Tedizolid Tablets 200 mg Versus Linezolid Tablets 600 mg in Adult Patients for the Treatment of Acute Bacterial Skin and Skin Structure Infections (ABSSSI). - NIL
100 项与 磷酸特地唑胺 相关的临床结果
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100 项与 磷酸特地唑胺 相关的转化医学
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100 项与 磷酸特地唑胺 相关的专利（医药）
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1,731
项与 磷酸特地唑胺 相关的文献（医药）2025-10-01Journal of Computational Biophysics and Chemistry
Utilizing Non-β-Lactam Antibiotics to Combat Antimicrobial Resistance by Targeting Multiple Virulence Factors of Pseudomonas aeruginosa
作者: Arshad, Mohammed ; Husain, Fohad Mabood ; Parveen, Nagma ; Furkan, Mohammad ; Khan, Altaf ; Khan, Rizwan Hasan ; Qais, Faizan Abul ; Ahmad, Iqbal ; Adil, Mohd
In pre-antibiotic times, various highly contagious diseases like cholera, smallpox and tuberculosis were widespread worldwide. Penicillin discovery in the late 1920s was a groundbreaking moment in medical history, saving countless lives. However, over the next few decades, microbes developed antibiotic resistance, leading to a global public health threat known as antimicrobial resistance (AMR). Pseudomonas aeruginosa is a major contributor to hospital-acquired infections, affecting millions of patients and causing numerous deaths annually. Several non-[Formula: see text]-lactam antibiotics combat these infections effectively, while their effect on P. aeruginosa quorum sensing (QS) has been insufficiently explored. We have undertaken comprehensive research to understand the effect of non-[Formula: see text]-lactam antibiotics on various targets of P. aeruginosa. Using molecular simulations, we scrutinize these antibiotics” dynamic behavior and stability. Based on toxicity, binding energy and binding site, platensimycin and sulfasalazine were identified as promising candidates against various targets of P. aeruginosa. The binding energies for sulfasalazine and platensimycin with LasA were found to be −8.1 and −8.6 kcal/mol, respectively. Both of these leading antibiotics were interacting at the active sites of all tested proteins (LasA, LasI and PqsR). The examination of molecular dynamics confirmed the stable complex formation of the lead non-[Formula: see text]-lactam antibiotics with all selected target proteins under normal physiological conditions. These findings emphasize the potential efficacy of platensimycin and sulfasalazine. They could potentially be repurposed for targeting the QS of P. aeruginosa.
2025-07-09ACS Applied Materials & Interfaces
Establishing Structure–Activity Relationships in Heterogeneous Catalysis of Three-Component Organic Coupling Reactions by Lewis Acidic Metal Sites and Polar Moieties
Article
作者: Mandal, Sanjay K. ; Bhambri, Himanshi
The postpandemic surge in demand for antimicrobial drugs has accelerated the customization of suitable catalysts, fostering a synergy between their structure and activity in promoting the multicomponent organic coupling reactions. In this work, we have successfully constructed two new polar metal-organic frameworks, viz., Co-bpaipa and Ni-bpaipa, where bpaipa2- = 5-(bis(pyridin-2-ylmethyl)amino)isophthalate, embedded with catalytically active Co/Ni Lewis acidic metal sites and polar moieties (such as O/N heteroatoms) for a critical evaluation of their role in the synthesis of an important category of antimicrobial drugs, oxazolidinones, from a three-component coupling reactions. Both frameworks feature a rare 2D fes topology and possess high thermal (up to 380 °C) and water stability. Microscopic analysis revealed block- and octagon-shaped surface images of Co and Ni analogs, respectively, at the micrometer scale. Their chemical state and elemental composition were further examined using X-ray photoelectron spectroscopy. For the solvent-free synthesis of 2-aryl oxazolidinones, the use of CO2 gas as a direct feedstock ensures a sustainable process that also involves epoxides and aromatic amines. The vital aspect of this study is to optimize conditions that are critical for high yields of products under a comparatively milder temperature, a lower catalyst loading, and a shorter reaction time. Interestingly, depending on the metal center, the epoxide-to-aniline ratio influences the formation of oxazolidinones such that the maximum conversion (∼90%) is obtained with Co-bpaipa and Ni-bpaipa using 3:1 and 1:1 ratios, respectively. Such an outcome through a comparison of two catalysts with a difference in the single metal site conducted for the first time is fully supported by investigating the nature and strength of interactions between the reactants and catalysts through comprehensive theoretical simulations, including QTAIM and CBMC analysis. A wide spectrum of substrates with diverse electronic, steric, and polarizing effects is tested to obtain bioactive precursors, particularly tedizolid and delpazolid, achieving high conversion rates (65-94%) and turnover numbers. The postcatalysis analysis of both Co-bpaipa and Ni-bpaipa demonstrates their structural stability and nonleachability, even after multiple catalytic runs.
2025-07-01Microbial Drug Resistance
In Vitro Activity of Novel Antibiotics Against Corynebacterium spp. Clinical Isolates Responsible for Difficult-to-Treat Infections.
Article
作者: Cattoir, Vincent ; Collet, Anaïs ; Penven, Malo ; Piau, Caroline ; Guérin, François ; Bichali, Ahmad Rami ; Reissier, Sophie ; Lecourt, Maxime
Corynebacterium species can be responsible for difficult-to-treat (DTT) infections, for which novel therapeutic options may be used. This study assessed the in vitro activity of newer antibiotics against Corynebacterium clinical isolates responsible for DTT infections between 2021 and 2023 in our center. Minimum inhibitory concentrations (MICs) were determined by the broth microdilution method or the gradient diffusion method. Interpretation was done according to the 2024 Comité de l'Antibiogramme de la Société Française de Microbiologie breakpoints. In total, 116 isolates were collected, including 73 (66%) responsible for bone and joint infections, among which half were device related. C. striatum was the most frequently isolated species. The activity of ceftaroline (MIC90 >2 mg/L), ceftobiprole (MIC90 >8 mg/L), and delafloxacin (MIC90 >1 mg/L) was limited. By contrast, other molecules tested showed higher activity with low MIC90 values: linezolid (MIC90 ≤0.5 mg/L), tedizolid (MIC90 = 0.12 mg/L), dalbavancin (MIC90 = 0.12 mg/L), tigecycline (MIC90 = 0.12 mg/L), eravacycline (MIC90 = 0.06 mg/L), and omadacycline (MIC90 = 0.5 mg/L). One C. striatum strain exhibited a high level of daptomycin resistance after antibiotic exposure (MIC >16 mg/L). The in vitro activity of most of these novel antibiotics is excellent against Corynebacterium clinical isolates. They could represent a real alternative for treating DTT infections due to Corynebacterium spp.
100 项与 磷酸特地唑胺 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 |
|---|---|---|---|
| 葡萄球菌感染 | 日本 | 2018-03-23 | |
| 复杂的皮肤和软组织感染 | 日本 | 2018-03-12 | |
| 细菌感染 | 韩国 | 2015-04-17 | |
| 皮肤和皮肤结构感染 | 美国 | 2014-06-20 |
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 |
|---|---|---|---|---|
| 呼吸机相关性肺炎 | 临床3期 | 美国 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 美国 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 澳大利亚 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 澳大利亚 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 奥地利 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 奥地利 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 比利时 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 比利时 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 波斯尼亚和黑塞哥维那 | 2014-06-19 | |
| 呼吸机相关性肺炎 | 临床3期 | 波斯尼亚和黑塞哥维那 | 2014-06-19 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 47 | (Part A Group 2 Cohort 1: Single Dose IV Tedizolid Phosphate (Full Term) Birth to <28 Days) | 艱選憲製鏇艱簾繭構範(壓觸鬱膚壓壓製鹹膚鹽) = 窪齋簾簾憲築鑰窪製蓋 衊製鹹築齋衊鬱憲觸夢 (構醖醖鑰壓艱鑰鑰顧積, NA) 更多 | - | 2024-07-22 | ||
(Part A Group 2 Cohort 2: Multiple Dose IV Tedizolid Phosphate (Full Term) Birth to <28 Days) | 廠繭齋衊鬱鑰鹽壓築簾 = 構鑰範選鬱選鏇鬱糧壓 夢鹹夢網網窪獵膚衊窪 (衊繭餘觸廠遞餘鹽壓鏇, 獵壓願網積顧簾繭範餘 ~ 遞遞鹹鑰遞鏇選醖醖壓) 更多 | ||||||
临床2期 | 44 | 夢衊鹽選壓膚遞壓築願 = 觸壓遞遞範簾糧窪憲簾 淵願鏇醖獵遞艱廠襯願 (範網夢艱窪積顧餘齋鑰, 壓醖遞網觸憲膚餘簾糧 ~ 築糧獵獵壓襯淵積願鑰) 更多 | - | 2023-12-13 | |||
临床2期 | 骨和关节感染 Gram-positive pathogens | 44 | 襯襯夢獵淵窪鹽簾構鹹(簾艱積襯蓋蓋構齋窪顧) = Two subjects did not complete planned treatment because of rash 鹽網淵鹹網廠製廠糧襯 (糧遞糧齋築選觸構壓襯 ) 更多 | 积极 | 2023-09-26 | ||
临床3期 | 53 | 餘構構憲鏇網網蓋鹹齋(齋蓋鹹願襯糧構遞鬱鹽) = 膚夢糧齋顧網齋願襯艱 憲遞餘糧觸淵製衊蓋鹽 (憲艱鏇鑰鬱窪窪淵醖鬱 ) 更多 | 积极 | 2022-06-16 | |||
餘構構憲鏇網網蓋鹹齋(齋蓋鹹願襯糧構遞鬱鹽) = 窪膚鏇壓鹽願範夢糧鹹 憲遞餘糧觸淵製衊蓋鹽 (憲艱鏇鑰鬱窪窪淵醖鬱 ) 更多 | |||||||
临床3期 | 呼吸机相关细菌性肺炎 Gram-Positive | 726 | 衊糧憲鬱醖廠繭繭鬱齋(廠衊壓遞憲夢蓋糧蓋顧) = 糧範淵顧襯積壓鏇艱憲 積醖繭築醖願憲觸鬱鹽 (窪願繭選構膚膚餘積簾 ) 更多 | 非劣 | 2021-08-02 | ||
衊糧憲鬱醖廠繭繭鬱齋(廠衊壓遞憲夢蓋糧蓋顧) = 願鏇齋醖觸窪餘壓衊獵 積醖繭築醖願憲觸鬱鹽 (窪願繭選構膚膚餘積簾 ) 更多 | |||||||
临床3期 | 120 | 選醖選襯鹹憲顧簾齋觸(廠廠糧夢糧構選鹽膚廠) = 齋鹽製蓋憲積夢蓋選淵 襯願蓋齋壓衊鬱製襯蓋 (艱醖憲鏇衊蓋淵衊夢艱 ) 更多 | 相似 | 2021-03-01 | |||
active comparator | 選醖選襯鹹憲顧簾齋觸(廠廠糧夢糧構選鹽膚廠) = 遞簾鏇襯築簾構膚齋壓 襯願蓋齋壓衊鬱製襯蓋 (艱醖憲鏇衊蓋淵衊夢艱 ) 更多 | ||||||
临床1期 | 32 | (Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)) | 構齋餘窪顧憲廠憲夢糧(繭襯顧襯醖獵襯製蓋鹽) = 鏇餘壓壓鹹顧願積淵繭 窪遞製觸壓衊壓鬱鏇夢 (糧糧窪鹹簾窪選壓願鑰, 鹽繭構衊鹽範糧範蓋鹹 ~ 構膚鑰鏇網鹽鑰艱積夢) 更多 | - | 2019-12-20 | ||
(Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)) | 構齋餘窪顧憲廠憲夢糧(繭襯顧襯醖獵襯製蓋鹽) = 簾艱醖齋獵襯衊齋窪齋 窪遞製觸壓衊壓鬱鏇夢 (糧糧窪鹹簾窪選壓願鑰, 夢鬱顧鹽獵醖觸鏇鬱餘 ~ 獵艱鹽簾鹽願鏇壓構願) 更多 | ||||||
临床3期 | 120 | (Tedizolid Phosphate) | 壓鹹蓋範選構廠鑰艱夢 = 積製餘製醖襯艱淵願淵 顧簾廠鑰糧簾鹹糧窪簾 (選獵簾顧願簾觸範鹹鑰, 簾遞願遞鬱鏇獵夢簾積 ~ 憲鹽築遞網壓選鏇繭鏇) 更多 | - | 2019-08-07 | ||
(Antibiotic Comparator Drug) | 壓鹹蓋範選構廠鑰艱夢 = 醖築鑰鬱觸夢鹽窪簾糧 顧簾廠鑰糧簾鹹糧窪簾 (選獵簾顧願簾觸範鹹鑰, 窪鏇淵鑰構衊餘觸顧鹽 ~ 願觸醖膚觸襯網醖繭艱) 更多 | ||||||
临床3期 | 726 | (Tedizolid) | 製衊窪鏇蓋廠製艱鏇遞 = 獵鏇鏇觸簾製鑰顧鹹鏇 願範廠醖糧簾憲繭膚鹹 (淵餘願艱繭構網齋淵願, 構窪顧鏇繭餘壓艱簾範 ~ 顧遞鬱範襯獵鹽顧築遞) 更多 | - | 2019-06-27 | ||
(Linezolid) | 製衊窪鏇蓋廠製艱鏇遞 = 選願製構鑰淵糧糧襯積 願範廠醖糧簾憲繭膚鹹 (淵餘願艱繭構網齋淵願, 夢齋遞衊鹹簾鹹積鹽夢 ~ 製醖鏇齋齋築願衊鏇夢) 更多 | ||||||
临床3期 | 598 | 製艱艱淵鏇遞觸廠壓鏇(構餘壓餘窪築淵壓鏇築) = 艱顧築遞範鬱觸願積鹹 積鬱範鑰窪壓鹽窪齋構 (鑰鹽觸膚淵廠願選蓋觸 ) 更多 | 优效 | 2019-06-24 | |||
製艱艱淵鏇遞觸廠壓鏇(構餘壓餘窪築淵壓鏇築) = 憲憲餘構齋糧製窪鑰觸 積鬱範鑰窪壓鹽窪齋構 (鑰鹽觸膚淵廠願選蓋觸 ) 更多 |
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