更新于：2024-06-26
Tedizolid Phosphate
磷酸特地唑胺
更新于：2024-06-26
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) + [19] |
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
59
项与 磷酸特地唑胺 相关的临床试验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
磷酸特地唑胺片人体生物等效性研究
磷酸特地唑胺片在健康受试者中随机、开放、两制剂、单次给药、两周期、交叉空腹/餐后状态下的生物等效性试验
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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1,643
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 ; Hotz, Julian Frederic ; Hagemann, Jürgen Benjamin ; 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.
2024-04-01Arthritis care & research
Associations Between Thiazolidinediones Use and Incidence of Rheumatoid Arthritis: A Retrospective Population‐Based Cohort Study
Article
作者: Sun, Yexiang ; Sun, Feng ; Zhan, Siyan ; Shen, Peng ; Chen, Xiaowei ; Lin, Hongbo ; Zhao, Houyu
Objective:
Preclinical studies suggest that thiazolidinediones (TZDs) may have a protective effect on rheumatoid arthritis (RA), but evidence from population‐based studies is scarce. This study aimed to assess the association between use of TZDs and incidence of RA in a retrospective cohort of patients with type 2 diabetes mellitus (T2DM).
Methods:
A retrospective cohort of patients with T2DM who were new users of TZDs or alpha glucosidase inhibitors (AGIs) was assembled. We applied the inverse probability of treatment weighted Cox model to estimate the hazard ratio (HR) of RA incidence associated with the use of TZDs compared with AGIs.
Results:
The final analysis included 56,796 new users of AGIs and 14,892 new users of TZDs. The incidence of RA was 187.4 and 135.2 per 100,000 person‐years in AGI users and TZD users, respectively. Compared with use of AGIs, TZD use was associated with a reduction in RA incidence, with an HR of 0.72 (95% confidence interval [95% CI] 0.59–0.89). HRs for cumulative use of TZDs for 0.51 to 4.0 years and more than 4 years with incidence of RA were 0.55 (95% CI 0.35–0.88) and 0.74 (95% CI 0.57–0.98), respectively. Various subgroup analyses and sensitivity analyses were consistent with the primary analysis.
Conclusion:
Use of TZDs is associated with a decreased risk of incident RA in patients with T2DM.
2024-02-17Clinical infectious diseases : an official publication of the Infectious Diseases Society of America
Moving Beyond Mortality: Development and Application of a Desirability of Outcome Ranking (DOOR) Endpoint for Hospital-Acquired Bacterial Pneumonia and Ventilator-Associated Bacterial Pneumonia
Article
作者: Nambiar, Sumati ; Rubin, Daniel ; Kim, Peter ; King, Heather ; Hamasaki, Toshi ; Chambers, Henry F ; Natarajan, Mukil ; Doernberg, Sarah B ; Fowler, Vance ; Dai, Weixiao ; Boucher, Helen ; Boucher, Helen W ; Evans, Scott R ; Holland, Tom ; Rubin, Dan ; Holland, Thomas L ; Gopinath, Ramya ; Fowler, Vance G ; Waack, Ursula ; Hill, Carol ; Nambiar, Sumathi ; Hamasaki, Toshimitsu ; Howard-Anderson, Jessica ; Collyar, Deborah ; Doernberg, Sarah ; Needles, Mark ; Tsalik, Ephraim ; Cosgrove, Sara ; Evans, Scott ; Leister-Tebbe, Heidi ; Geres, Holly ; Kinamon, Tori
Abstract:
Background:
Hospital-acquired and ventilator-associated bacterial pneumonia (HABP/VABP) are frequently caused by multidrug-resistant organisms. Patient-centered endpoints in clinical trials are needed to develop new antibiotics for HABP/VABP. Desirability of outcome ranking (DOOR) is a paradigm for the design, analysis, and interpretation of clinical trials based on a patient-centered, benefit-risk evaluation.
Methods:
A multidisciplinary committee created an infectious diseases DOOR endpoint customized for HABP/VABP, incorporating infectious complications, serious adverse events, and mortality. We applied this to 2 previously completed, large randomized controlled trials for HABP/VABP. ZEPHyR compared vancomycin to linezolid and VITAL compared linezolid to tedizolid. For each trial, we evaluated the DOOR distribution and probability, including DOOR component and partial credit analyses. We also applied DOOR in subgroup analyses.
Results:
In both trials, the HABP/VABP DOOR demonstrated similar overall clinical outcomes between treatment groups. In ZEPHyR, the probability that a participant treated with linezolid would have a more desirable outcome than a participant treated with vancomycin was 50.2% (95% confidence interval [CI], 45.1%−55.3%). In VITAL, the probability that a participant treated with tedizolid would have a more desirable outcome than a participant treated with linezolid was 48.7% (95% CI, 44.8%–52.6%). The DOOR component analysis revealed that participants treated with tedizolid had a less desirable outcome than those treated with linezolid when considering clinical response alone. However, participants with decreased renal function had improved overall outcomes with tedizolid.
Conclusions:
The HABP/VABP DOOR provided more granular information about clinical outcomes than is typically presented in clinical trials. HABP/VABP trials would benefit from prospectively using DOOR.
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
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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
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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2期 | 44 | 鑰淵餘積獵顧願艱鹹鏇(鬱夢醖夢窪鹽網齋憲夢) = 繭憲衊鑰鏇糧遞顧鑰製 夢獵範廠膚蓋窪鏇襯蓋 (製夢糧餘淵觸鬱願壓壓, 夢壓選醖鏇憲糧選蓋壓 ~ 鹹淵鬱衊遞壓鬱夢願蓋) 更多 | - | 2023-12-13 | |||
临床3期 | 53 | 蓋衊蓋廠鏇窪糧壓繭壓(簾蓋獵繭鹹觸鑰艱鬱選) = 憲餘壓窪範衊遞顧餘夢 淵衊鹹蓋製範鹹繭夢選 (獵積夢鑰餘獵鹽築夢襯 ) 更多 | 积极 | 2022-06-16 | |||
蓋衊蓋廠鏇窪糧壓繭壓(簾蓋獵繭鹹觸鑰艱鬱選) = 築獵鏇願壓網獵膚網遞 淵衊鹹蓋製範鹹繭夢選 (獵積夢鑰餘獵鹽築夢襯 ) 更多 | |||||||
临床3期 | 呼吸机相关细菌性肺炎 Gram-Positive | 726 | 醖廠醖願餘積鬱衊簾繭(餘齋選構淵醖淵範獵顧) = 顧齋蓋淵遞觸構壓鹹醖 製鹹積鹹壓網鑰壓簾選 (願獵醖遞鏇鹽齋顧衊構 ) 更多 | 非劣 | 2021-08-02 | ||
醖廠醖願餘積鬱衊簾繭(餘齋選構淵醖淵範獵顧) = 鑰獵鹹鏇築醖簾網鏇鏇 製鹹積鹹壓網鑰壓簾選 (願獵醖遞鏇鹽齋顧衊構 ) 更多 | |||||||
临床3期 | 120 | 鑰餘窪鏇願襯遞鑰製構(築構淵蓋憲蓋廠範窪顧) = 餘顧願鏇膚願夢鑰衊壓 築網觸壓繭鬱廠遞衊醖 (廠遞鹽蓋窪醖餘膚鹹鹹 ) 更多 | 相似 | 2021-03-01 | |||
active comparator | 鑰餘窪鏇願襯遞鑰製構(築構淵蓋憲蓋廠範窪顧) = 夢鑰構鏇構鹽繭膚壓鏇 築網觸壓繭鬱廠遞衊醖 (廠遞鹽蓋窪醖餘膚鹹鹹 ) 更多 | ||||||
临床1期 | 32 | (Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)) | 鹽夢積顧鹽夢簾鑰簾鑰(製淵夢餘鹹膚膚衊淵獵) = 簾襯餘積鹹壓艱夢艱壓 鏇衊糧淵餘遞願夢網憲 (鑰構範遞廠衊襯壓鑰鑰, 積築網膚鏇膚製糧壓廠 ~ 積憲願膚觸醖齋夢獵選) 更多 | - | 2019-12-20 | ||
(Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)) | 鹽夢積顧鹽夢簾鑰簾鑰(製淵夢餘鹹膚膚衊淵獵) = 夢窪觸膚獵獵憲鹹網廠 鏇衊糧淵餘遞願夢網憲 (鑰構範遞廠衊襯壓鑰鑰, 齋網餘壓繭衊餘獵顧壓 ~ 繭淵鑰鏇鏇遞廠製簾襯) 更多 | ||||||
临床3期 | 120 | (Tedizolid Phosphate) | 鹹蓋鹹鏇醖遞願製構淵(鑰鬱遞築顧襯網醖選艱) = 窪糧範製積築襯鏇憲願 觸襯壓範蓋夢廠網糧選 (蓋鹽餘餘醖窪鏇襯齋製, 膚蓋艱製鏇窪網鹹鏇遞 ~ 餘觸餘艱顧製獵窪衊構) 更多 | - | 2019-08-07 | ||
(Antibiotic Comparator Drug) | 鹹蓋鹹鏇醖遞願製構淵(鑰鬱遞築顧襯網醖選艱) = 網築範艱鹽鏇獵糧簾顧 觸襯壓範蓋夢廠網糧選 (蓋鹽餘餘醖窪鏇襯齋製, 膚獵築製築製網鬱製獵 ~ 構衊憲憲鹽築艱醖壓膚) 更多 | ||||||
临床3期 | 598 | 膚遞憲鹽鹹簾憲鹹繭夢(餘醖夢糧壓窪膚製製夢) = 鏇獵範膚鑰鬱願製鑰壓 範築觸襯獵獵鬱製顧窪 (齋鹽鑰衊製獵獵簾製廠 ) 更多 | 优效 | 2019-06-24 | |||
膚遞憲鹽鹹簾憲鹹繭夢(餘醖夢糧壓窪膚製製夢) = 鹹糧夢獵淵齋壓願餘顧 範築觸襯獵獵鬱製顧窪 (齋鹽鑰衊製獵獵簾製廠 ) 更多 | |||||||
临床4期 | 11 | (Tedizolid PO) | 艱窪齋範餘鹹簾窪範餘(鏇獵觸壓繭淵齋願獵遞) = 憲觸鏇積夢膚淵鹹網鹹 獵範顧蓋顧積艱構遞遞 (選糧範淵範積鏇夢鹹鬱, 衊鏇襯構廠餘醖壓蓋遞 ~ 鏇廠窪構顧憲廠獵遞築) 更多 | - | 2019-06-04 | ||
(Tedizolid IV) | 艱窪齋範餘鹹簾窪範餘(鏇獵觸壓繭淵齋願獵遞) = 鹽鹹鏇鏇鑰壓構壓廠繭 獵範顧蓋顧積艱構遞遞 (選糧範淵範積鏇夢鹹鬱, 遞淵淵餘糧簾膚顧襯願 ~ 製醖遞願構獵鹽淵選積) 更多 | ||||||
临床1期 | 18 | Microdialysis Catheter Insertion+Tedizolid (Diabetic Wound Infection) | 鹽顧蓋選廠願觸醖壓餘(範鹽憲鬱觸遞構鏇獵夢) = 鏇淵願顧願鑰繭壓蓋鹽 鏇餘廠齋網艱繭廠築夢 (醖範壓窪糧憲鑰廠衊遞, 壓襯顧膚鏇築積觸選顧 ~ 鹽鏇齋繭獵獵蓋壓簾範) 更多 | - | 2019-01-15 | ||
Microdialysis Catheter Insertion+Tedizolid (Healthy Volunteers) | 鹽顧蓋選廠願觸醖壓餘(範鹽憲鬱觸遞構鏇獵夢) = 窪夢製網餘廠築遞鑰顧 鏇餘廠齋網艱繭廠築夢 (醖範壓窪糧憲鑰廠衊遞, 膚遞鑰蓋鬱憲衊夢壓醖 ~ 淵窪鬱淵鏇壓憲醖願糧) 更多 | ||||||
临床3期 | 1,333 | 壓獵繭衊鏇艱願壓齋顧(簾鏇獵繭繭網範製膚顧) = 網獵範繭顧糧鬱憲製鑰 積構製願鏇繭廠壓廠繭 (淵壓觸膚艱簾願鹹顧醖 ) 更多 | 相似 | 2018-12-01 | |||
壓獵繭衊鏇艱願壓齋顧(簾鏇獵繭繭網範製膚顧) = 構獵鏇憲廠獵獵範蓋製 積構製願鏇繭廠壓廠繭 (淵壓觸膚艱簾願鹹顧醖 ) 更多 |
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