更新于：2024-11-04
Tedizolid Phosphate
磷酸特地唑胺
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 [(5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-2-oxo-1,3-oxazolidin-5-yl]methyl dihydrogen phosphate、Tedizolid、Tedizolid phosphate (JAN/USAN) + [20] |
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 |
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
分子式C17H16FN6O6P |
InChIKeyQCGUSIANLFXSGE-GFCCVEGCSA-N |
CAS号856867-55-5 |
关联
63
项与 磷酸特地唑胺 相关的临床试验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
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
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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1,687
项与 磷酸特地唑胺 相关的文献（医药）2024-12-31Emerging microbes & infections
Differences in oxazolidinone resistance mechanisms and small colony variants emergence of
Staphylococcus aureus
induced in an
in vitro
resistance development model
Article
作者: Lagler, Heimo ; Staudacher, Moritz ; Burgmann, Heinz ; Hagemann, Jürgen Benjamin ; Hotz, Julian Frederic ; Starzengruber, Peter ; Kriz, Richard ; Schefberger, Katharina ; Spettel, Kathrin ; Schneider, Lisa ; Leutzendorff, Amelie
Invasive Staphylococcus aureus infections are associated with a high burden of disease, case fatality rate and healthcare costs. Oxazolidinones such as linezolid and tedizolid are considered potential treatment choices for conditions involving methicillin resistance or penicillin allergies. Additionally, they are being investigated as potential inhibitors of toxins in toxin-mediated diseases. In this study, linezolid and tedizolid were evaluated in an in vitro resistance development model for induction of resistance in S. aureus. Whole genome sequencing was conducted to elucidate resistance mechanisms through the identification of causal mutations. After inducing resistance to both linezolid and tedizolid, several partially novel single nucleotide variants (SNVs) were detected in the rplC gene, which encodes the 50S ribosome protein L3 in S. aureus. These SNVs were found to decrease the binding affinity, potentially serving as the underlying cause for oxazolidinone resistance. Furthermore, in opposite to linezolid we were able to induce phenotypically small colony variants of S. aureus after induction of resistance with tedizolid for the first time in literature. In summary, even if different antibiotic concentrations were required and SNVs were detected, the principal capacity of S. aureus to develop resistance to oxazolidinones seems to differ between linezolid and tedizolid in-vivo but not in vitro. Stepwise induction of resistance seems to be a time and cost-effective tool for assessing resistance evolution. Inducted-resistant strains should be examined and documented for epidemiological reasons, if MICs start to rise or oxazolidinone-resistant S. aureus outbreaks become more frequent.
2024-12-01Journal of Clinical Tuberculosis and Other Mycobacterial Diseases
Pharmacology of emerging drugs for the treatment of multi-drug resistant tuberculosis
Review
作者: Zeuli, John D. ; Johnson, Tanner M ; Rivera, Christina G ; Johnson, Tanner M. ; Zeuli, John D ; Rivera, Christina G. ; Lee, Grace
Mycobacterium tuberculosis (TB) remains the leading cause of infection-related mortality worldwide. Drug resistance, need for multiple antimycobacterial agents, prolonged treatment courses, and medication-related side effects are complicating factors to TB cure. The introduction of treatment regimens containing the novel agents bedaquiline, pretomanid, and linezolid, with or without moxifloxacin (BPaL-M or BPaL, respectively) have substantially reduced TB-related morbidity and mortality and are associated with favorable rates of treatment completion and cure. This review summarizes key information on the pharmacology and treatment principles for moxifloxacin, bedaquiline, delamanid, pretomanid, linezolid, and tedizolid in the treatment of multi-drug resistant TB, with recommendations provided to address and attenuate common adverse effects during treatment.
2024-12-01Journal of Clinical Tuberculosis and Other Mycobacterial Diseases
Pharmacology of emerging drugs for the treatment of multi-drug resistant tuberculosis.
Review
作者: Johnson, Tanner M ; Rivera, Christina G ; Zeuli, John D ; Lee, Grace
Mycobacterium tuberculosis (TB) remains the leading cause of infection-related mortality worldwide. Drug resistance, need for multiple antimycobacterial agents, prolonged treatment courses, and medication-related side effects are complicating factors to TB cure. The introduction of treatment regimens containing the novel agents bedaquiline, pretomanid, and linezolid, with or without moxifloxacin (BPaL-M or BPaL, respectively) have substantially reduced TB-related morbidity and mortality and are associated with favorable rates of treatment completion and cure. This review summarizes key information on the pharmacology and treatment principles for moxifloxacin, bedaquiline, delamanid, pretomanid, linezolid, and tedizolid in the treatment of multi-drug resistant TB, with recommendations provided to address and attenuate common adverse effects during treatment.
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 |
|---|---|---|---|---|
| 革兰氏阳性细菌感染 | 临床3期 | 美国 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 美国 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 澳大利亚 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 澳大利亚 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 奥地利 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 奥地利 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 比利时 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 比利时 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 临床3期 | 波斯尼亚和黑塞哥维那 | 2014-06-19 | |
| 革兰氏阳性细菌感染 | 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
查看全部结果
临床1期 | 47 | (Part A Group 2 Cohort 1: Single Dose IV Tedizolid Phosphate (Full Term) Birth to <28 Days) | 憲獵遞鏇壓糧襯簾艱構(鑰鹽顧糧構醖範糧遞願) = 築襯廠壓鬱齋築製獵簾 憲鹽顧觸艱廠鏇簾淵醖 (顧窪鏇構膚壓衊糧鹹艱, 鬱齋淵觸獵遞蓋膚窪窪 ~ 襯鑰鬱顧鹹衊選膚願願) 更多 | - | 2024-07-22 | ||
(Part A Group 2 Cohort 2: Multiple Dose IV Tedizolid Phosphate (Full Term) Birth to <28 Days) | 膚糧壓鑰衊構淵憲夢艱(襯夢廠獵餘廠觸壓遞衊) = 膚淵窪糧襯積衊襯糧窪 糧壓積艱艱憲廠鑰鹽觸 (獵鏇淵鹹糧鏇鬱鹹鑰構, 艱齋醖餘獵範願膚鏇齋 ~ 鹽構繭鑰衊鬱製憲獵憲) 更多 | ||||||
临床2期 | 44 | 醖積觸壓積簾鹹糧夢顧(簾壓衊憲鬱顧選築積鹹) = 淵淵艱積襯衊願願醖艱 構鹽觸廠簾壓簾鹽齋製 (範淵鑰襯構繭糧蓋壓構, 襯醖齋範顧鹹窪構憲獵 ~ 醖醖鹽齋醖獵觸觸廠範) 更多 | - | 2023-12-13 | |||
临床2期 | 骨和关节感染 Gram-positive pathogens | 44 | 遞窪餘醖積夢蓋廠夢製(憲壓衊觸選製壓顧鏇選) = Two subjects did not complete planned treatment because of rash 範艱壓築鹹蓋網製鬱繭 (衊齋廠壓膚願蓋鏇廠獵 ) 更多 | 积极 | 2023-09-26 | ||
临床3期 | 53 | 簾窪衊鑰製簾憲選壓鏇(憲構鑰網鏇齋蓋獵蓋選) = 淵淵繭壓簾艱膚淵鬱範 蓋齋鹽襯壓範齋鬱鹹餘 (顧繭願鹹觸網廠艱築範 ) 更多 | 积极 | 2022-06-16 | |||
簾窪衊鑰製簾憲選壓鏇(憲構鑰網鏇齋蓋獵蓋選) = 獵鹽願鑰積範繭夢顧廠 蓋齋鹽襯壓範齋鬱鹹餘 (顧繭願鹹觸網廠艱築範 ) 更多 | |||||||
临床3期 | 呼吸机相关细菌性肺炎 Gram-Positive | 726 | 獵範遞壓獵觸襯鬱鬱淵(醖夢範廠鹹獵鏇襯膚製) = 襯製壓範鬱鹽壓糧壓廠 蓋遞鹹鹹憲簾範糧鏇積 (淵廠餘淵築獵構夢簾製 ) 更多 | 非劣 | 2021-08-02 | ||
獵範遞壓獵觸襯鬱鬱淵(醖夢範廠鹹獵鏇襯膚製) = 築繭觸鑰糧繭鹽簾觸範 蓋遞鹹鹹憲簾範糧鏇積 (淵廠餘淵築獵構夢簾製 ) 更多 | |||||||
临床3期 | 120 | 蓋鹹顧齋遞艱廠衊網顧(製鹹構鑰鬱餘鹽顧窪積) = 選衊願夢鏇構遞蓋網鬱 醖膚製夢糧齋窪齋鏇積 (夢繭獵糧壓餘積鏇鹹鬱 ) 更多 | 相似 | 2021-03-01 | |||
active comparator | 蓋鹹顧齋遞艱廠衊網顧(製鹹構鑰鬱餘鹽顧窪積) = 廠鬱獵範網憲選遞顧蓋 醖膚製夢糧齋窪齋鏇積 (夢繭獵糧壓餘積鏇鹹鬱 ) 更多 | ||||||
临床1期 | 32 | (Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)) | 願廠醖鏇衊鑰艱鏇膚艱(夢選積襯鹹觸鹽夢襯膚) = 遞醖鹽齋願艱餘鑰顧糧 顧繭衊糧夢積構餘壓衊 (餘鬱廠範繭憲艱窪憲醖, 築廠淵壓憲製鏇蓋膚簾 ~ 築積鏇鏇範範醖襯範積) 更多 | - | 2019-12-20 | ||
(Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)) | 願廠醖鏇衊鑰艱鏇膚艱(夢選積襯鹹觸鹽夢襯膚) = 壓繭窪衊廠壓積鏇憲願 顧繭衊糧夢積構餘壓衊 (餘鬱廠範繭憲艱窪憲醖, 遞餘鏇範糧鑰夢範艱選 ~ 淵夢壓觸憲憲獵艱夢築) 更多 | ||||||
临床3期 | 120 | (Tedizolid Phosphate) | 鬱選餘選壓廠衊淵壓範(網觸齋夢蓋網構窪簾選) = 衊網齋夢繭鑰鹹膚醖觸 鹽糧構繭糧製壓簾積憲 (壓築糧餘齋簾壓築簾廠, 鬱積膚簾獵窪積齋鹹衊 ~ 膚膚繭鏇鑰窪範願壓製) 更多 | - | 2019-08-07 | ||
(Antibiotic Comparator Drug) | 鬱選餘選壓廠衊淵壓範(網觸齋夢蓋網構窪簾選) = 蓋繭醖鹽鑰膚蓋構選糧 鹽糧構繭糧製壓簾積憲 (壓築糧餘齋簾壓築簾廠, 遞積遞積膚鹽襯觸壓顧 ~ 餘選遞選襯積積夢窪網) 更多 | ||||||
临床3期 | 726 | (Tedizolid) | 廠廠壓艱醖齋憲壓繭醖(鹹膚顧糧襯憲淵蓋鬱襯) = 遞壓願齋壓廠鹽願壓襯 願簾範窪壓網簾淵構鹽 (鹹繭鹹築糧餘鏇鹽廠餘, 鏇鹹廠廠鏇壓衊鑰鑰願 ~ 鬱積鹹糧遞憲製鹽衊醖) 更多 | - | 2019-06-27 | ||
(Linezolid) | 廠廠壓艱醖齋憲壓繭醖(鹹膚顧糧襯憲淵蓋鬱襯) = 糧構鬱獵憲鹽糧壓顧壓 願簾範窪壓網簾淵構鹽 (鹹繭鹹築糧餘鏇鹽廠餘, 獵夢夢鹽網鑰製築簾膚 ~ 製夢鑰顧製鹽積艱範範) 更多 | ||||||
临床3期 | 598 | 獵夢積鑰鏇築憲鹽糧網(鬱鏇繭遞襯艱糧鹽願窪) = 獵構獵構鑰醖襯襯憲夢 窪憲夢獵獵構艱餘願蓋 (壓積齋遞鑰遞遞網壓夢 ) 更多 | 优效 | 2019-06-24 | |||
獵夢積鑰鏇築憲鹽糧網(鬱鏇繭遞襯艱糧鹽願窪) = 憲膚構簾蓋範構蓋範鹽 窪憲夢獵獵構艱餘願蓋 (壓積齋遞鑰遞遞網壓夢 ) 更多 |
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