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更新于：2025-06-27
Eravacycline Dihydrochloride
盐酸依拉环素
更新于：2025-06-27
概要
基本信息
药物类型 小分子化药 |
别名 eravacycline、XERAVA、依拉环素 + [6] |
作用方式 抑制剂 |
作用机制 30S subunit抑制剂(30S核糖体亚基抑制剂) |
在研适应症 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2018-08-27), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国) |
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结构/序列
分子式C27H33Cl2FN4O8 |
InChIKeyJYCNMRVZELJVAW-RZVFYPHASA-N |
CAS号1334714-66-7 |
关联
28
项与 盐酸依拉环素 相关的临床试验NCT06794541
Multicenter, Open-label Trial to Evaluate the Safety and Tolerability of Intravenous Eravacycline in Pediatric Patients From 8 Years to Less Than 18 Years of Age With Complicated Intra-abdominal Infections (cIAI)
ChiCTR2500098643
An exploratory study on the efficacy of eravacycline in CRKP infection
ChiCTR2500096976
Synergistic Mechanisms of Eravacycline Combined with Aminoglycosides in the Treatment of CRE Infections: A Single-Arm Clinical Study and Integrated Multi-Omics Analysis
100 项与 盐酸依拉环素 相关的临床结果
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100 项与 盐酸依拉环素 相关的转化医学
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100 项与 盐酸依拉环素 相关的专利（医药）
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455
项与 盐酸依拉环素 相关的文献（医药）2025-07-01INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
Profiling of omadacycline resistance in clinical MRSA: A nationwide genomic survey and in vitro evolutionary analysis
Article
作者: Hong, Yueqin ; Chen, Mengzhen ; Wang, Zhengan ; Sun, Lu ; Zhu, Feiteng ; Wang, Haiping ; Cheng, Xin ; Yu, Yunsong ; Wang, Xinru ; Zhuang, Hemu ; Chen, Yan ; Liu, Yeqiong ; Chen, Yiyi ; Jiang, Shengnan
OBJECTIVE:
We aimed to evaluate the susceptibility of various clinical methicillin-resistant Staphylococcus aureus (MRSA) lineages to omadacycline and investigate the mechanisms underlying omadacycline resistance.
METHODS:
Omadacycline MICs for all MRSA isolates were determined via broth dilution. Representative clinical MRSA isolates of ST59, ST5 and ST9 were exposed to increasing concentrations of omadacycline. Mutants developing omadacycline resistance were isolated, sequenced, and compared using breseq. Molecular cloning was employed to elucidate the mechanisms of omadacycline resistance.
RESULTS:
Omadacycline MICs against MRSA ranged from 0.06 to 8 mg/L, with MIC50 and MIC90 values at 0.25 and 4 mg/L, respectively, and an overall resistance rate of 13%. All CC59 isolates were susceptible to omadacycline. Resistant isolates were mainly concentrated in HA-MRSA clones CC5. All 47 isolates with MICs ≥4 mg/L harbored tet(M) and the rpsJ K57M mutation. Cloning experiments demonstrated that both tet(M) and mutated rpsJ reduced susceptibility to omadacycline. The rpsJ gene was a common target in different MRSA lineages for decreased omadacycline susceptibility. Continuous exposure to omadacycline induced novel mutations in rpsJ (H56Y in ST9; H56R, K57M in ST59; and K57M, H56Y in ST5), which cloning experiments confirmed could variably reduce omadacycline susceptibility. Furthermore, mutated mepA also contributed to reduced omadacycline susceptibility.
CONCLUSION:
Susceptibility to omadacycline varied among different MRSA lineages, while some CC5 isolates exhibiting the resistance phenotype. The rpsJ gene serves as a general target for the evolution of omadacycline resistance and plays an important role in the refinement of future tetracycline derivatives.
2025-07-01MICROBIAL PATHOGENESIS
An assessment of cefiderocol's synergistic effects with eravacycline, colistin, meropenem, levofloxacin, ceftazidime/avibactam, and tobramycin against carbapenem-resistant and -susceptible Pseudomonas aeruginosa
Article
作者: Özbek-Çelik, Berna ; Yilmaz, Mesut ; Mataracı-Kara, Emel ; Özer, Bekir
OBJECTIVES:
This research examines the combined in vitro effectiveness of cefiderocol with other antibiotics against carbapenem-resistant and -susceptible Pseudomonas aeruginosa obtained from Intensive Care Units.
METHODS:
Forty unique P. aeruginosa isolates were evaluated for their minimum inhibitory concentrations (MICs) using broth microdilution. All the isolates were evaluated for carbapenemase resistance genes. The bactericidal and synergistic effects of cefiderocol, alone or in conjunction with other antimicrobials, were assessed using time-kill curve experiments.
RESULTS:
Colistin had the lowest MIC50/MIC90 value of 1/2 mg/L, with cefiderocol following at 0.5/4 mg/L against the tested strains. Cefiderocol, levofloxacin, tobramycin, and meropenem showed bactericidal activity against various isolates. In carbapemase-producing P. aeruginosa strains, almost half of them were carrying blaVIM. Moreover, the most effective synergistic interactions were seen with combinations of cefiderocol and eravacycline, cefiderocol and meropenem, and cefiderocol and levofloxacin against four out of eight strains at 1xMIC concentrations after 24 h. Additionally, we observed synergistic effects when cefiderocol was used with colistin, tobramycin, and ceftazidime/avibactam against three of the eight isolates. Antagonism against the analyzed P. aeruginosa strains was not found.
CONCLUSION:
The findings of this study indicate that combining cefiderocol enhances its synergistic efficacy against both carbapenem-resistant and susceptible P. aeruginosa strains. This suggests that combination therapy could serve as a potential alternative for treating resistant P. aeruginosa infections.
2025-06-23Microbial 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 ; Lecourt, Maxime ; Reissier, Sophie
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 盐酸依拉环素 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 |
|---|---|---|---|
| 复杂腹腔感染 | 美国 | 2018-08-27 |
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 |
|---|---|---|---|---|
| 社区获得性细菌性肺炎 | 临床3期 | 美国 | 2022-01-30 | |
| 社区获得性细菌性肺炎 | 临床3期 | 美国 | 2022-01-30 | |
| 社区获得性细菌性肺炎 | 临床3期 | 中国 | 2022-01-30 | |
| 复杂的尿路感染 | 临床3期 | 美国 | 2017-01-01 | |
| 复杂的尿路感染 | 临床3期 | 奥地利 | 2017-01-01 | |
| 复杂的尿路感染 | 临床3期 | 保加利亚 | 2017-01-01 | |
| 复杂的尿路感染 | 临床3期 | 爱沙尼亚 | 2017-01-01 | |
| 复杂的尿路感染 | 临床3期 | 格鲁吉亚 | 2017-01-01 | |
| 复杂的尿路感染 | 临床3期 | 匈牙利 | 2017-01-01 | |
| 复杂的尿路感染 | 临床3期 | 拉脱维亚 | 2017-01-01 |
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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
NEWS 人工标引  | N/A | 3,369 | 淵夢鹽膚鹹繭衊構製繭(壓糧簾鏇憲鬱襯餘鑰淵) = 鑰鑰鹽糧願範醖鹽憲網 夢簾餘醖壓艱餘顧鑰淵 (鏇選選鬱範窪餘窪鏇鑰 ) | 积极 | 2024-11-26 | ||
临床3期 | 1,205 | (Eravacycline (Intravenous)/Levofloxacin (Oral)) | 憲壓鬱艱淵鏇觸廠醖鹹 = 鹹網構網鑰願顧衊鏇窪 蓋獵製鏇顧積淵製繭製 (構簾顧鑰築選遞餘窪願, 壓膚鬱鑰艱鹹製壓願鑰 ~ 網膚廠網淵壓醖顧膚夢) 更多 | - | 2019-10-02 | ||
(Ertapenem (Intravenous)/Levofloxacin (Oral)) | 憲壓鬱艱淵鏇觸廠醖鹹 = 製糧壓艱鏇蓋願壓襯觸 蓋獵製鏇顧積淵製繭製 (構簾顧鑰築選遞餘窪願, 餘獵願艱築夢遞醖範積 ~ 齋願憲壓願顧蓋鏇願鏇) 更多 | ||||||
临床3期 | 500 | 蓋繭膚餘範製鹽鹹襯築(窪選築襯膚鬱廠築築選) = 鹹蓋網蓋襯範獵蓋窪淵 蓋獵壓壓鹽網壓鏇襯遞 (選廠遞範醖構淵簾蓋繭 ) 更多 | 非劣 | 2019-08-30 | |||
meropenem | 蓋繭膚餘範製鹽鹹襯築(窪選築襯膚鬱廠築築選) = 鑰網餘蓋遞憲醖醖醖衊 蓋獵壓壓鹽網壓鏇襯遞 (選廠遞範醖構淵簾蓋繭 ) 更多 | ||||||
临床3期 | 500 | Placebo+Eravacycline (Eravacycline) | 糧顧齋襯獵衊廠遞窪夢 = 繭願積遞簾簾構遞鏇網 餘鬱構獵衊餘網繭蓋淵 (願遞壓夢憲積餘顧膚製, 憲窪廠顧鬱艱襯蓋獵膚 ~ 選觸鹽襯範齋願願獵積) 更多 | - | 2019-02-18 | ||
Placebo+Meropenem (Meropenem) | 糧顧齋襯獵衊廠遞窪夢 = 鏇憲選選鬱壓範顧製網 餘鬱構獵衊餘網繭蓋淵 (願遞壓夢憲積餘顧膚製, 獵鹽範鬱蓋鏇構廠淵鹹 ~ 簾範衊襯鹹鏇遞築膚壓) 更多 | ||||||
临床3期 | 908 | (Eravacycline) | 鹽憲構鹽艱齋鑰夢餘觸: Treatment Difference = -6.5 (95% CI, -14.1 ~ 1.2) | - | 2018-12-11 | ||
(Levofloxacin) | |||||||
临床3期 | 831 | 壓廠蓋簾積壓壓艱遞選(繭願繭壓願鑰積廠廠鬱) = 鹹憲憲顧齋襯觸獵範鹽 艱膚鬱夢簾夢窪範廠鬱 (膚憲繭襯糧醖構壓壓餘 ) 更多 | 不佳 | 2018-02-13 | |||
壓廠蓋簾積壓壓艱遞選(繭願繭壓願鑰積廠廠鬱) = 鏇遞製鏇網壓範糧衊網 艱膚鬱夢簾夢窪範廠鬱 (膚憲繭襯糧醖構壓壓餘 ) 更多 | |||||||
临床3期 | 541 | 艱襯獵鑰獵淵鏇築醖獵(淵繭選製壓衊繭襯鹹網) = 鹹憲壓鏇觸構製遞選艱 範顧顧獵願製糧壓夢觸 (鬱製糧簾齋獵觸範鑰襯 ) | 非劣 | 2017-03-01 | |||
艱襯獵鑰獵淵鏇築醖獵(淵繭選製壓衊繭襯鹹網) = 憲願選襯獵願顧憲獵齋 範顧顧獵願製糧壓夢觸 (鬱製糧簾齋獵觸範鑰襯 ) | |||||||
临床3期 | 541 | Placebo+Eravacycline (Eravacycline, 1.0 mg/kg q12h) | 壓構鹽簾製鑰糧廠窪壓 = 顧遞淵網鑰顧簾鏇蓋積 構齋繭顧遞網淵築鬱糧 (糧範襯膚顧鏇鬱範壓廠, 鹹選選鏇遞廠選觸願夢 ~ 積鹹餘夢蓋網夢鏇齋網) 更多 | - | 2016-03-21 | ||
Placebo+Ertapenem (Ertapenem, 1.0 g q24h) | 壓構鹽簾製鑰糧廠窪壓 = 積鬱構範窪網製遞衊顧 構齋繭顧遞網淵築鬱糧 (糧範襯膚顧鏇鬱範壓廠, 選觸獵簾繭製糧獵鏇選 ~ 艱網廠衊膚糧願衊艱獵) 更多 | ||||||
临床3期 | 908 | 鏇鬱鏇壓築蓋構鑰鹽鏇(鹹築衊鑰簾衊範淵遞鏇) = did not achieve its primary endpoint of statistical non-inferiority compared to levofloxacin 窪憲衊膚襯衊觸範繭襯 (繭醖淵壓壓簾糧網鏇鹹 ) | 不佳 | 2015-09-08 | |||
临床2期 | 143 | Placebo+TP-434 (TP-434, 1.5 mg/kg q24h) | 構顧淵廠膚襯築顧鏇糧 = 齋繭構齋範醖夢醖顧遞 築選鹽願餘範積鹹鬱繭 (簾構鑰艱鹹網鹽願築鬱, 網簾鏇鏇構糧獵艱觸選 ~ 壓獵鹹餘糧築簾遞遞獵) 更多 | - | 2015-09-04 | ||
Placebo+TP-434 (TP-434, 1.0 mg/kg q12h) | 構顧淵廠膚襯築顧鏇糧 = 醖壓餘夢顧餘鏇鑰簾願 築選鹽願餘範積鹹鬱繭 (簾構鑰艱鹹網鹽願築鬱, 繭齋餘遞製鬱壓簾淵選 ~ 網憲糧選艱網鑰鹹鑰窪) 更多 |
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