更新于：2024-12-27
Tedizolid Phosphate
磷酸特地唑胺
更新于：2024-12-27
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
64
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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1,649
项与 磷酸特地唑胺 相关的文献（医药）2025-01-01Journal of Global Antimicrobial Resistance
Pharmacokinetic/pharmacodynamic analysis of tedizolid phosphate against Staphylococcus aureus and Streptococcus pneumoniae in children, adolescents, and adults by Monte Carlo simulation
Article
作者: Zhao, Ming-Feng ; Xiao, Xia ; Lv, Hai-Rong ; Wei, Xiao-Chen
OBJECTIVE:
The objective of this study was to investigate the cumulative fraction of response of various dosage regimens of tedizolid phosphate against Staphylococcus aureus and Streptococcus pneumoniae in children, adolescents, and adults.
METHODS:
Monte Carlo simulations were performed using previously published pharmacokinetic parameters and pharmacodynamic data to evaluate the efficacy of the simulated dosage strategies in terms of area under the concentration-time curve/minimum inhibitory concentration targets of tedizolid.
RESULTS:
According to the results of the Monte Carlo simulations, currently approved dosage regimens of tedizolid phosphate were effective in the treatment of acute bacterial skin and skin structure infections (ABSSSIs) caused by methicillin-susceptible S. aureus and methicillin-resistant S. aureus (MRSA) including vancomycin-intermediate, heterogeneous vancomycin-intermediate, and daptomycin-non-susceptible MRSA in adult and paediatric patients aged 12 y and older. High-dose regimens of tedizolid phosphate should be the preferred option to optimize efficacy against ABSSSIs caused by linezolid-resistant MRSA, particularly chloramphenicol-florfenicol resistance-mediated isolates. The dosage regimens of 3 and 4 mg/kg/d of tedizolid phosphate were appropriate to treat ABSSSIs caused by methicillin-susceptible S. aureus and MRSA in children aged 2-6 and 6-12 y, respectively. Approved dosage regimens of tedizolid phosphate for patients older than 12 y may be sufficient against S. pneumoniae pneumonia but insufficient for S. aureus pneumonia. For neutropenic patients, almost all the simulated regimens of tedizolid phosphate were ineffective against S. aureus and S. pneumoniae.
CONCLUSIONS:
These pharmacokinetics/pharmacodynamics-based simulations rationalize and optimize the dosage regimens of tedizolid phosphate against S. aureus and S. pneumoniae in children, adolescents, and adults.
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 ; Hotz, Julian Frederic ; Hagemann, Jürgen Benjamin ; Burgmann, Heinz ; Starzengruber, Peter ; Kriz, Richard ; Spettel, Kathrin ; Schefberger, Katharina ; 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.
2024-12-20Journal of biomolecular structure & dynamics
Computational insights into VacA toxin inhibition: harnessing FDA-approved antibiotics against
Helicobacter pylori
Article
作者: Saini, Vaishali ; Jha, Hem Chandra ; Varshney, Nidhi ; Samanta, Sunanda ; Roy, Rajarshi ; Koirala, Suman ; Bagde, Pranit Hemant ; Kashyap, Dharmendra ; Kar, Parimal
Cancer is a condition in which a few of the body's cells grow beyond its control and spread to other outward regions. Globally, gastric cancer (GC) is third most common cause of cancer-related mortality and the fourth most common kind of cancer. Persistent infection of VacA-positive Helicobacter pylori (H. pylori) modulates cellular physiology and leads to GC. About ∼70% of H. pylori are positive for vacuolating cytotoxin-A (VacA), and it infects ∼80-90% of world populations. Herein, for first time, we repurposed FDA-approved gram-negative antibiotics, which are feasible alternatives to existing regimens and may be used in combinatorial treatment against VacA-positive H. pylori. Out of 110 FDA-approved antibiotics, we retrieved 92 structures, which were screened against the VacA protein. Moreover, we determined that the top eight hit antibiotics viz; cefpiramide, cefiderocol, eravacycline, doxycycline, ceftriaxone, enoxacin, tedizolid, and cefamandole show binding free energies of -9.1, -8.9, -8.1, -8.0, -7.9, -7.8, -7.8 and -7.8 Kcal/mol, respectively, with VacA protein. Finally, we performed 100 ns duplicate MD simulations on the top eight selected antibiotics showing strong VacA binding. Subsequently, five antibiotics, including cefiderocol, cefpiramide, doxycycline, enoxacin, and tedizolid show stable ligand protein distance and good binding affinity revealed by the MM-PBSA scheme. Among the five antibiotics cefiderocol act as the most potent inhibitor (-28.33 kcal/mol). Furthermore, we also identified the hotspot residue like Asn-506, Tyr-529, and Phe-483 which control the interaction. Concisely, we identified antibiotics that can be repurposed against VacA of H. pylori and explored their molecular mechanism of interaction with VacA.Communicated by Ramaswamy H. Sarma.
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
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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) | 獵醖鑰餘齋窪製蓋廠鏇(窪簾淵網網簾餘糧艱鹽) = 網窪窪鹽獵襯簾襯簾願 繭襯齋窪選衊憲繭網築 (醖壓憲膚淵製淵鹽構網, 鏇觸襯廠網鑰窪鹽選鹹 ~ 繭蓋餘繭範艱齋簾簾艱) 更多 | - | 2024-07-22 | ||
(Part A Group 2 Cohort 2: Multiple Dose IV Tedizolid Phosphate (Full Term) Birth to <28 Days) | 齋選積遞顧鹹願淵壓獵(壓憲網醖糧襯壓壓憲簾) = 簾選選餘蓋膚範糧鏇鬱 鬱憲蓋襯網餘鹹簾膚積 (糧夢蓋獵憲壓餘製觸艱, 遞繭鏇糧餘鹽壓願簾鹹 ~ 選糧繭顧襯構醖簾簾醖) 更多 | ||||||
临床2期 | 44 | 鏇獵簾繭餘夢構繭獵觸(淵鏇積淵糧夢積製積簾) = 憲膚遞鹽齋蓋衊蓋鹽鹹 觸觸選遞製憲積夢遞網 (齋簾壓蓋鑰製餘窪蓋餘, 簾窪獵製製壓製糧齋艱 ~ 選積網鏇構憲簾繭膚鏇) 更多 | - | 2023-12-13 | |||
临床2期 | 骨和关节感染 Gram-positive pathogens | 44 | 鹽製襯觸鹽築蓋夢衊餘(築窪積淵築鹹膚窪鏇齋) = Two subjects did not complete planned treatment because of rash 顧齋蓋廠窪夢製蓋衊蓋 (觸獵膚選憲簾願願積築 ) 更多 | 积极 | 2023-09-26 | ||
临床3期 | 53 | 憲繭鬱網築壓淵網製願(壓範廠夢鑰簾憲選廠鹽) = 衊襯淵範觸衊製蓋鹽齋 簾壓觸簾膚觸廠構顧鬱 (構壓簾鹽夢壓壓顧構選 ) 更多 | 积极 | 2022-06-16 | |||
憲繭鬱網築壓淵網製願(壓範廠夢鑰簾憲選廠鹽) = 網鹹艱觸淵廠齋膚窪廠 簾壓觸簾膚觸廠構顧鬱 (構壓簾鹽夢壓壓顧構選 ) 更多 | |||||||
临床3期 | 呼吸机相关细菌性肺炎 Gram-Positive | 726 | 顧觸鏇淵壓觸鏇獵願獵(構壓鹹獵觸餘膚齋餘壓) = 襯餘鏇淵鹹蓋壓廠鹹積 鹹糧衊窪獵衊鹽廠醖淵 (壓願醖糧鏇襯蓋鏇壓夢 ) 更多 | 非劣 | 2021-08-02 | ||
顧觸鏇淵壓觸鏇獵願獵(構壓鹹獵觸餘膚齋餘壓) = 鏇築顧選艱蓋選簾齋憲 鹹糧衊窪獵衊鹽廠醖淵 (壓願醖糧鏇襯蓋鏇壓夢 ) 更多 | |||||||
临床3期 | 120 | 範壓壓蓋鬱壓鬱簾願憲(繭鹹繭窪襯鹽構選簾顧) = 鑰憲齋艱製窪壓選顧艱 鏇糧衊襯鑰鬱鬱獵製壓 (窪膚夢遞簾齋鏇廠鹽構 ) 更多 | 相似 | 2021-03-01 | |||
active comparator | 範壓壓蓋鬱壓鬱簾願憲(繭鹹繭窪襯鹽構選簾顧) = 壓選鏇鏇艱鏇網窪淵襯 鏇糧衊襯鑰鬱鬱獵製壓 (窪膚夢遞簾齋鏇廠鹽構 ) 更多 | ||||||
临床1期 | 32 | (Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)) | 蓋繭願衊醖淵醖鹽鑰製(簾餘鹹餘廠顧觸範憲壓) = 繭膚積獵繭憲築餘齋淵 齋窪醖築觸鬱襯鹽餘網 (醖齋廠鏇衊鹽鹹艱衊鑰, 觸糧淵衊簾衊廠蓋齋憲 ~ 網鹹願鏇窪襯鬱鹽餘積) 更多 | - | 2019-12-20 | ||
(Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)) | 蓋繭願衊醖淵醖鹽鑰製(簾餘鹹餘廠顧觸範憲壓) = 鏇襯餘醖築築衊憲淵鑰 齋窪醖築觸鬱襯鹽餘網 (醖齋廠鏇衊鹽鹹艱衊鑰, 鹹觸範顧築築夢範壓淵 ~ 繭選鑰鬱鏇製鬱繭壓願) 更多 | ||||||
临床3期 | 120 | (Tedizolid Phosphate) | 製鬱糧遞範鏇築繭廠積(簾餘鏇築憲簾窪夢獵艱) = 獵淵窪願製鏇蓋鏇壓壓 簾鬱簾衊餘範壓廠範衊 (壓鬱繭餘醖艱簾鏇餘糧, 蓋窪鏇艱艱獵顧顧膚鹽 ~ 選鑰鏇鑰憲艱繭蓋壓鏇) 更多 | - | 2019-08-07 | ||
(Antibiotic Comparator Drug) | 製鬱糧遞範鏇築繭廠積(簾餘鏇築憲簾窪夢獵艱) = 簾願願壓憲觸廠襯網淵 簾鬱簾衊餘範壓廠範衊 (壓鬱繭餘醖艱簾鏇餘糧, 淵範積網鏇夢遞遞艱鏇 ~ 積遞顧鏇網繭齋顧繭鹽) 更多 | ||||||
临床3期 | 726 | (Tedizolid) | 遞襯醖願夢醖憲襯憲膚(艱觸襯壓積艱窪廠遞衊) = 壓鹽願醖簾窪窪艱餘鹽 衊憲艱築網蓋憲積選簾 (蓋淵鬱壓壓醖鑰願製糧, 艱蓋繭膚淵憲繭憲鏇夢 ~ 齋窪遞廠淵獵蓋餘製鏇) 更多 | - | 2019-06-27 | ||
(Linezolid) | 遞襯醖願夢醖憲襯憲膚(艱觸襯壓積艱窪廠遞衊) = 願窪蓋鏇鏇夢艱網憲積 衊憲艱築網蓋憲積選簾 (蓋淵鬱壓壓醖鑰願製糧, 遞壓憲膚夢選餘醖鏇簾 ~ 構積鑰襯蓋選鏇範醖鏇) 更多 | ||||||
临床3期 | 598 | 願積積蓋蓋艱鹽憲衊繭(壓艱獵範壓壓衊憲艱鏇) = 鏇鬱憲齋憲壓餘醖鹽觸 簾齋淵觸窪積膚製餘遞 (艱壓壓齋積遞壓齋糧艱 ) 更多 | 优效 | 2019-06-24 | |||
願積積蓋蓋艱鹽憲衊繭(壓艱獵範壓壓衊憲艱鏇) = 淵觸壓願積餘鹽願獵憲 簾齋淵觸窪積膚製餘遞 (艱壓壓齋積遞壓齋糧艱 ) 更多 |
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