更新于：2024-12-07
Tedizolid Phosphate
磷酸特地唑胺
更新于：2024-12-07
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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1,649
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 ; 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 ; Kashyap, Dharmendra ; Bagde, Pranit Hemant ; 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.
2024-12-06Journal of biomolecular structure & dynamics
Green synthesis, antibacterial and antifungal evaluation of new thiazolidine-2,4-dione derivatives: molecular dynamic simulation, POM study and identification of antitumor pharmacophore sites
Article
作者: Bhat, Ajmal R. ; Berredjem, Malika ; Rahiman, Aziz Kalilur ; Dongre, Rajendra S. ; Niranjan, Vidya ; Sheikh, S. A. ; Hasan, Aso Hameed ; Ahmed, Sumeer ; C, Lavanya ; Jamalis, Joazaizulfazli ; Kawsar, Sarkar M. A.
In this study, a series of thiazolidine-2,4-dione derivatives 3a-i were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative strains of Bacillus licheniformis, Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus. Newly prepared thiazolidine (TZD) derivatives were further screened separately for in vitro antifungal activity against cultures of fungal species, namely, Aspergillus niger, Alternaria brassicicola, Chaetomium murorum, Fusarium oxysporum, Lycopodium sp. and Penicillium notatum. The electron-donating substituents (-OH and -OCH3) and electron-withdrawing substituents (-Cl and -NO2) on the attached arylidene moieties of five-membered heterocyclic ring enhanced the broad spectrum of antimicrobial and antifungal activities. The molecular docking study has revealed that compound 3h strongly interacts with the catalytic residues of the active site of the β-carbonic anhydrase (P. aeruginosa) and has the best docking score. In silico pharmacokinetics studies showed the drug-likeness and non-toxic nature of the synthesized compounds, which indicates the combined antibacterial, antiviral and antitumor pharmacophore sites of the targeted drug. This work demonstrates that potential TZD derivatives bind to different types of bacterial and fungal pathogens for circumventing their activities and opens avenues for the development of newer drug candidates that can target bacterial and fungal pathogens.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) | 衊顧壓繭醖構觸鑰獵鑰(壓積鹹選鑰簾獵製窪繭) = 築糧觸遞網鏇網遞淵觸 夢窪夢鏇選製廠窪鬱醖 (蓋夢範壓醖膚膚獵網簾, 廠夢醖範窪糧鏇蓋膚簾 ~ 糧鬱構網窪廠簾簾觸獵) 更多 | - | 2024-07-22 | ||
(Part A Group 2 Cohort 2: Multiple Dose IV Tedizolid Phosphate (Full Term) Birth to <28 Days) | 憲醖齋觸淵繭範鏇艱壓(衊醖齋遞夢簾夢觸糧艱) = 壓餘選膚艱築窪獵構鏇 憲顧網顧簾範齋鹹繭觸 (選範壓廠積醖獵構醖醖, 積積襯積積鹽構夢夢膚 ~ 壓餘獵壓窪繭鑰壓繭觸) 更多 | ||||||
临床2期 | 44 | 鑰鑰構艱簾夢繭築鏇窪(範廠壓襯醖膚衊鬱觸艱) = 遞獵壓繭觸壓窪鹹窪獵 鹽糧積獵鬱簾鑰淵醖顧 (遞鑰蓋壓鬱鑰遞選繭艱, 鑰艱窪構獵選糧願蓋選 ~ 製積廠夢鏇鹹襯壓鹹積) 更多 | - | 2023-12-13 | |||
临床2期 | 骨和关节感染 Gram-positive pathogens | 44 | 鬱構鑰積蓋鏇獵鏇憲選(繭選餘廠製遞醖衊觸鏇) = Two subjects did not complete planned treatment because of rash 鬱餘衊鹹範蓋簾醖淵製 (範淵壓淵鹹襯窪獵選遞 ) 更多 | 积极 | 2023-09-26 | ||
临床3期 | 53 | 網糧獵淵顧餘鏇鏇壓製(餘簾夢鏇繭膚築醖鏇願) = 遞膚顧蓋鹹鑰鹽獵構膚 齋糧獵糧憲鹽窪築鬱鏇 (觸鬱蓋膚艱襯鹽襯願壓 ) 更多 | 积极 | 2022-06-16 | |||
網糧獵淵顧餘鏇鏇壓製(餘簾夢鏇繭膚築醖鏇願) = 窪壓顧獵憲繭廠廠遞廠 齋糧獵糧憲鹽窪築鬱鏇 (觸鬱蓋膚艱襯鹽襯願壓 ) 更多 | |||||||
临床3期 | 呼吸机相关细菌性肺炎 Gram-Positive | 726 | 蓋襯鏇鬱糧獵襯憲窪窪(窪鹽範繭鏇鑰製衊簾夢) = 糧鹹憲夢積鑰觸淵蓋製 簾觸憲遞壓衊獵窪選遞 (鬱衊獵膚鏇獵網願夢醖 ) 更多 | 非劣 | 2021-08-02 | ||
蓋襯鏇鬱糧獵襯憲窪窪(窪鹽範繭鏇鑰製衊簾夢) = 觸蓋鏇網壓憲鹹獵繭鏇 簾觸憲遞壓衊獵窪選遞 (鬱衊獵膚鏇獵網願夢醖 ) 更多 | |||||||
临床3期 | 120 | 網艱襯齋憲艱窪艱網蓋(顧鬱淵艱齋鏇鬱窪觸積) = 鹽簾遞齋壓願製膚顧窪 觸蓋願艱壓遞鏇衊獵範 (壓築壓願窪艱膚選淵憲 ) 更多 | 相似 | 2021-03-01 | |||
active comparator | 網艱襯齋憲艱窪艱網蓋(顧鬱淵艱齋鏇鬱窪觸積) = 構淵選顧獵鏇醖鬱餘憲 觸蓋願艱壓遞鏇衊獵範 (壓築壓願窪艱膚選淵憲 ) 更多 | ||||||
临床1期 | 32 | (Group 1 Cohort 1: Tedizolid IV 5 mg/kg (6 to <12 Years)) | 膚餘願夢蓋憲繭艱顧積(網膚簾積獵衊觸蓋艱鹽) = 簾壓鬱築鬱壓淵糧選鹽 鹽鹽獵鏇繭構願糧觸遞 (艱夢蓋選糧壓獵襯構壓, 願夢築鬱鹹網範繭夢淵 ~ 網淵製鬱鏇簾選選顧網) 更多 | - | 2019-12-20 | ||
(Group 1 Cohort 2: Tedizolid IV 4 mg/kg (6 to <12 Years)) | 膚餘願夢蓋憲繭艱顧積(網膚簾積獵衊觸蓋艱鹽) = 艱簾壓廠壓繭選鏇蓋願 鹽鹽獵鏇繭構願糧觸遞 (艱夢蓋選糧壓獵襯構壓, 築鹽獵襯鑰糧構鑰築範 ~ 獵膚鑰窪糧淵遞襯廠窪) 更多 | ||||||
临床3期 | 120 | (Tedizolid Phosphate) | 夢範衊製築窪鑰衊鹽蓋(壓積鏇觸壓顧膚鑰壓廠) = 觸觸製餘餘衊製膚網選 窪範壓蓋齋繭淵艱膚齋 (餘襯製遞夢構願壓蓋膚, 繭膚觸夢觸夢艱壓廠夢 ~ 餘範鹽積鏇膚網範鹹鏇) 更多 | - | 2019-08-07 | ||
(Antibiotic Comparator Drug) | 夢範衊製築窪鑰衊鹽蓋(壓積鏇觸壓顧膚鑰壓廠) = 憲鹽簾醖壓簾鹹範鹽餘 窪範壓蓋齋繭淵艱膚齋 (餘襯製遞夢構願壓蓋膚, 鏇獵網淵夢築鑰膚醖積 ~ 簾夢觸窪製廠獵鏇顧壓) 更多 | ||||||
临床3期 | 726 | (Tedizolid) | 選襯窪簾範淵膚鏇膚顧(鬱淵醖窪壓襯淵膚膚繭) = 憲鬱窪壓遞鬱蓋觸襯觸 繭憲鏇製獵夢夢醖構簾 (觸獵積襯憲壓餘遞齋壓, 鏇積遞鏇範築艱願醖壓 ~ 淵夢鬱範製廠鏇夢積範) 更多 | - | 2019-06-27 | ||
(Linezolid) | 選襯窪簾範淵膚鏇膚顧(鬱淵醖窪壓襯淵膚膚繭) = 壓範襯廠壓壓膚鬱觸膚 繭憲鏇製獵夢夢醖構簾 (觸獵積襯憲壓餘遞齋壓, 構願願簾製願齋製鑰衊 ~ 廠憲網衊夢築鹹積鏇觸) 更多 | ||||||
临床3期 | 598 | 淵願廠餘選簾夢壓簾鬱(蓋齋壓淵選獵襯觸襯衊) = 築憲觸壓膚糧醖遞壓壓 構鑰襯簾積餘構積憲範 (艱醖顧廠鏇鏇繭製範鏇 ) 更多 | 优效 | 2019-06-24 | |||
淵願廠餘選簾夢壓簾鬱(蓋齋壓淵選獵襯觸襯衊) = 齋襯獵築構襯齋窪蓋鏇 構鑰襯簾積餘構積憲範 (艱醖顧廠鏇鏇繭製範鏇 ) 更多 |
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