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更新于：2025-08-13
Cilastatin Sodium/Imipenem/Relebactam
西司他丁/亚胺培南/瑞来巴坦
更新于：2025-08-13
概要
基本信息
药物类型 小分子化药 |
别名 Cilastatin/imipenem/relebactam、Cilastatin/relebactam/imipenem、IMI/REL + [15] |
作用方式 抑制剂 |
作用机制 酶抑制剂、PBPs抑制剂(细菌青霉素结合蛋白家族抑制剂)、β-lactamase抑制剂(β-内酰胺酶抑制剂) |
在研适应症 |
非在研适应症 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、优先审评 (美国) |
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结构/序列
分子式C12H19N3O5S |
InChIKeyGSOSVVULSKVSLQ-JJVRHELESA-N |
CAS号74431-23-5 |
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关联
16
项与 西司他丁/亚胺培南/瑞来巴坦 相关的临床试验ChiCTR2300070223
An assessment of the Ceftolozane/Tazobactam and Imipenem/Relebactam activity in the hypervirulent Klebsiella pneumoniae
NCT05561764
A Multicenter, Open-label Study to Determine the Pharmacokinetics, Safety, and Outcomes of Imipenem/Cilastatin/Relebactam During Treatment of Acute Pulmonary Exacerbations in Adolescent and Adult Patients With Cystic Fibrosis
NCT05146154
Impact of Obesity on the Pharmacokinetics of Imipenem-Relebactam in ICU Patients
100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的临床结果
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100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的转化医学
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100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的专利（医药）
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32
项与 西司他丁/亚胺培南/瑞来巴坦 相关的文献（医药）2025-08-01INFECTION
Comparison of the in vitro activities and resistance mechanisms against imipenem–relebactam and ceftazidime–avibactam in clinical KPC-producing Klebsiella pneumoniae isolated in China
Article
作者: Zhuo, Chao ; Guo, Yingyi ; Li, Jiahui ; Zhuo, Chuyue ; Chen, Jiakang ; Lin, Zhiwei ; Yao, Likang ; Yang, Xu ; Xiao, Shunian ; He, Nanhao ; Wang, Yijing ; Wang, Jiong ; Lin, Yexin ; Zhang, Yan
BACKGROUND:
Ceftazidime-avibactam (CAZ-AVI) and imipenem-relebactam (IMI-REL) are both antibiotics with promising prospects for treating Klebsiella pneumoniae carbapenemase (KPC)-producing Klebsiella pneumoniae (KPC-Kp) infections. However, differences in the in vitro activities and resistance mechanisms to CAZ-AVI and IMI-REL in clinical KPC-Kps have not been described.
METHODS:
In this study, KPC-Kp isolates from hospitalized patients in China were collected and subjected to antimicrobial susceptibility testing of IMI-REL and CAZ-AVI using the broth microdilution method. Whole-genome sequencing (WGS) and functional validation of mutations were performed on resistant strains, and RT-qPCR was used to determine the expression levels of blaKPC.
RESULTS:
The results showed that 21 (2.7%) of 782 clinical KPC-Kp strains were CAZ-AVI-resistant, 6 (0.8%) of 782 strains were IMI-REL-resistant, and 5 strains among them were resistant to both CAZ-AVI and IMI-REL. Strains resistant to both CAZ-AVI and IMI-REL can be effectively inhibited by tigecycline and polymyxin B. WGS and complementation experiments showed that KPC mutations are linked to high-level resistance to CAZ-AVI; while OmpK36 mutations may be the vital mechanism of IMI-REL resistance, confers resistance to CAZ-AVI simultaneously. Furthermore, RT-qPCR indicated that elevated blaKPC expression may play an important role in both CAZ-AVI and IMI-REL resistance.
CONCLUSIONS:
In summary, this study suggested that IMI-REL may have superior inhibitory effects in vitro on KPC-Kps than CAZ-AVI, and described the differences in resistance mechanisms between the two antibiotics.
2025-06-01Infectious Diseases Now
Antimicrobial activity of new anti-Pseudomonas beta-lactam-beta-lactamase inhibitors against Pseudomonas aeruginosa respiratory isolates recovered during the study for Monitoring Antimicrobial Resistance Trends (SMART) program in France (2016–2022)
Article
作者: Pailhoriès, Hélène ; Eckert, Catherine ; Pierrat, Gautier ; Woerther, Paul-Louis ; Corvec, Stéphane ; Kempf, Marie ; Zins, Charlie ; Bourge, Xavier ; Boyer, Sophie ; Dahyot, Sandrine ; Chenouard, Rachel
OBJECTIVES:
To assess the susceptibility of ceftolozane/tazobactam (C/T) and comparators to Pseudomonas aeruginosa isolates recovered from respiratory-tract-infections (RTI) between 2016-2022 in the French SMART study.
METHODS:
Antibiotic susceptibility testing and minimum inhibitory concentrations (MICs) of 717 P.aeruginosa isolates collected in five French hospitals were determined and interpreted according to the EUCAST-2022 guidelines. P. aeruginosa isolates resistant (R) to imipenem and/or C/T were screened by PCR for extended-spectrum-β-lactamases (ESBLs), AmpC and carbapenemase genes. The identified genes were sequenced and the variants determined.
RESULTS:
All in all, 96.5 % of P. aeruginosa isolates were susceptible to C/T, comparable to the susceptibilities of meropenem-vaborbactam (MVB = 96.5 %), imipenem/relebactam (IMI/REL = 96.9 %) and ceftazidime-avibactam (C/A = 97.0 %). MIC50 and MIC90 for C/T were 0.5 and 2 mg/L respectively against the 717 isolates. Among the 242 isolates (33.7 %) resistant to at least one anti-Pseudomonas β-lactam, close to 90 % were susceptible to C/T, C/A, MVB and IMI/REL. Among the 80 isolates resistant to piperacillin-tazobactam, cefepime and ceftazidime, 76.3 % were susceptible to C/T and only IMI/REL and amikacin reached susceptibility exceeding 80 %. Among the 32 isolates resistant to imipenem and meropenem, susceptibility exceeding 60 % was observed only for IMI/REL, C/T, and C/A. For these strains, the MIC50 of C/T was 2 mg/L, while that of C/A was at the resistance threshold (8 mg/L). IMI/REL had the strongest activity (72 %) against the 25 isolates resistant to C/T. Lastly, 53 imipenem and/or C/T-R isolates harbored a class C β-lactam (blaPDC) variant, and one of them also carried the blaPER-1 gene and another, the blaVIM-2 gene.
CONCLUSION:
C/T is a reliable treatment option in RTI caused by P. aeruginosa.
2025-05-01Journal of Global Antimicrobial Resistance
Whole-genome sequencing characterisation of a new KPC-245 variant-carrying Klebsiella pneumoniae strain isolated from a transplanted patient and resistant to ceftazidime/avibactam, meropenem/vaborbactam and imipenem/relebactam
Article
作者: Minucci, Rita ; Mularoni, Alessandra ; Conaldi, Pier Giulio ; Gallo, Alessia ; Monaco, Francesco ; Castelbuono, Salvatore ; Cona, Andrea ; Di Carlo, Daniele ; Vazzana, Roberta ; Vaiana, Claudia ; Cuscino, Nicola
OBJECTIVE:
In recent decades, the increasing prevalence of multidrug-resistant Klebsiella pneumoniae carbapenemase (KPC)-carrying K. pneumoniae (KPC-Kp) has become a worldwide public concern. Herein, we characterised a ceftazidime/avibactam (CAZ/AVI), meropenem/vaborbactam (MER/VAB) and imipenem/relebactam (IMI/REL)-resistant KPC-Kp strain isolated from a critically ill transplant patient.
METHODS:
Antimicrobial susceptibility testing and whole-genome sequencing (WGS) were conducted to characterise the strain at phenotypic and genotypic levels. Genomic DNA was sequenced using the Illumina platform. Bioinformatic analyses were used to investigate the genome sequences both for resistance and virulence features, and for the characterisation of plasmids.
RESULTS:
Phenotypic characterisation revealed that the KPC-Kp isolate was highly resistant to a wide range of antibiotics, including all β-lactam/β-lactamase inhibitor combinations such as CAZ/AVI, MER/VAB, IMI/REL and cefiderocol. WGS analysis showed that the isolate, belonging to the rare lineage ST661, contained several resistance and virulence genes. Among the resistance genes, we identified a new KPC variant within the mobile genetic element Tn4401-KPC-245-characterised by the insertion of nine amino acids (RAPNKDDYT) at position 263 as well as an amino acid change within the protein sequence, E274D, compared with KPC-3. Interestingly, the presence of mutations only in the blaKPC gene and not in other β-lactamase coding genes strongly points to the role of KPC-245 in β-lactam/β-lactamase inhibitor combinations and cefiderocol resistance.
CONCLUSIONS:
In our study, by using WGS analysis on a clinical isolate, we identified a new blaKPC variant within the Tn4401 transposon. Our results confirm the importance of continuous surveillance of multidrug-resistant K. pneumoniae in the clinical context.
100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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| - | 西司他丁/亚胺培南/瑞来巴坦 | - |
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 |
|---|---|---|---|
| 感染 | 日本 | 2021-06-23 | |
| 医院获得性细菌性肺炎 | 美国 | 2020-06-04 | |
| 呼吸机相关细菌性肺炎 | 美国 | 2020-06-04 | |
| 菌血症 | 欧盟 | 2020-02-13 | |
| 菌血症 | 冰岛 | 2020-02-13 | |
| 菌血症 | 列支敦士登 | 2020-02-13 | |
| 菌血症 | 挪威 | 2020-02-13 | |
| 医院获得性肺炎 | 欧盟 | 2020-02-13 | |
| 医院获得性肺炎 | 冰岛 | 2020-02-13 | |
| 医院获得性肺炎 | 列支敦士登 | 2020-02-13 | |
| 医院获得性肺炎 | 挪威 | 2020-02-13 | |
| 呼吸机相关性肺炎 | 欧盟 | 2020-02-13 | |
| 呼吸机相关性肺炎 | 冰岛 | 2020-02-13 | |
| 呼吸机相关性肺炎 | 列支敦士登 | 2020-02-13 | |
| 呼吸机相关性肺炎 | 挪威 | 2020-02-13 | |
| 复杂腹腔感染 | 美国 | 2019-07-16 | |
| 复杂的尿路感染 | 美国 | 2019-07-16 | |
| 革兰氏阴性菌感染 | 美国 | 2019-07-16 | |
| 肾盂肾炎 | 美国 | 2019-07-16 |
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 |
|---|---|---|---|---|
| 耐碳青霉烯类细菌感染 | 临床3期 | - | 2015-08-21 | |
| 粒细胞减少性发热 | 临床2期 | 美国 | 2021-09-14 | |
| 血液肿瘤 | 临床2期 | 美国 | 2021-09-14 | |
| 恶性实体肿瘤 | 临床2期 | 美国 | 2021-09-14 | |
| 脓毒症 | 临床1期 | 美国 | 2021-01-01 |
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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
临床3期 | 270 | Imipenem/cilastatin/relebactam (IMI/REL) | 選鏇糧鏇衊醖憲製鹽窪(繭願鏇範選糧糧糧願襯) = Secondary outcomes were comparable between treatment groups, including favorable CR 齋顧願鹽鹹窪鹽衊鑰鏇 (構簾鹽餘鹽簾願夢顧糧 ) 更多 | 积极 | 2025-04-01 | ||
Piperacillin/tazobactam (PIP/TAZ) | |||||||
临床1期 | 8 | 選鏇鹽壓襯網窪憲選鏇(餘鏇糧構膚鏇鬱蓋選淵) = 夢遞繭選壓選觸簾願壓 窪壓憲網壓餘顧餘糧願 (艱醖鏇廠選膚選廠鏇壓, 6.52) 更多 | - | 2024-08-07 | |||
临床2期 | 100 | 夢構鏇壓選繭襯遞淵醖(廠簾衊鹹膚齋壓鏇憲蓋) = 選鬱糧觸膚鹹簾襯積餘 襯齋遞糧鏇積鬱憲遞製 (網遞獵壓鬱遞鏇壓艱鏇, 鏇獵膚遞醖構顧網選淵 ~ 醖觸顧簾遞製獵獵淵襯) 更多 | - | 2024-03-12 | |||
临床1期 | 46 | 齋鏇鏇鬱膚蓋壓選簾衊(選襯蓋鬱齋構築簾積網) = 網窪糧夢積餘衊鏇壓醖 繭齋餘鹹觸製窪鏇觸窪 (醖構顧餘鹽鹹鹽獵壓簾 ) 更多 | - | 2023-08-10 | |||
临床3期 | 274 | (IMI/REL FDC) | 壓鬱蓋簾選獵願網廠範 = 繭築選壓醖觸膚衊顧憲 獵繭範築範糧齋繭齋選 (積顧選願鏇鹹膚淵願築, 壓餘夢選憲築糧鹽遞顧 ~ 願艱觸廠窪獵構鹽糧鹽) 更多 | - | 2023-06-28 | ||
(PIP/TAZ FDC) | 壓鬱蓋簾選獵願網廠範 = 醖獵齋鹹夢餘壓憲鏇簾 獵繭範築範糧齋繭齋選 (積顧選願鏇鹹膚淵願築, 鬱衊積鏇願獵壓製淵遞 ~ 襯製艱簾鑰製窪廠積衊) 更多 | ||||||
临床3期 | 47 | 膚襯膚齋願網觸範膚願(構糧蓋積蓋夢齋積艱獵) = 顧齋鑰簾鬱範獵衊壓醖 網鹹齋積鬱繭蓋獵觸壓 (範壓壓餘艱簾齋窪獵選 ) 更多 | 积极 | 2020-04-15 | |||
imipenem+colistin | 膚襯膚齋願網觸範膚願(構糧蓋積蓋夢齋積艱獵) = 壓構鏇製憲蓋構糧淵鹽 網鹹齋積鬱繭蓋獵觸壓 (範壓壓餘艱簾齋窪獵選 ) 更多 | ||||||
临床3期 | 83 | imipenem+relebactam+cilastatin (cIAI/cUTI) | 鬱廠蓋網膚襯鏇窪構顧 = 憲鹽糧鹹顧窪夢簾網襯 鬱艱願繭鑰夢鹽鑰鑰願 (壓獵鹽鏇衊簾製網艱淵, 繭齋餘築鹹遞襯艱醖餘 ~ 遞顧夢廠構築鹹淵鏇衊) 更多 | - | 2019-09-17 | ||
imipenem+relebactam+cilastatin (cIAI) | 艱顧製觸蓋鑰艱衊獵衊 = 淵範築繭遞廠遞構築繭 選構鏇繭鏇簾遞廠夢憲 (鑰餘顧廠壓衊選窪艱鏇, 窪製壓廠積餘鹹衊衊構 ~ 夢衊簾鹽鹽糧範壓衊簾) 更多 | ||||||
临床3期 | 50 | Placebo to CMS+Imipenem+Cilastatin/Relebactam (Group 1: Imipenem+Cilastatin/Relebactam) | 繭憲蓋願鏇鏇製願齋積 = 製夢願醖簾醖製醖艱壓 蓋衊顧淵襯觸觸醖構繭 (鹽構壓鬱願構膚淵蓋鏇, 襯襯構襯膚鬱範繭選膚 ~ 窪範簾艱廠淵鑰衊繭觸) 更多 | - | 2018-10-19 | ||
(Group 2: Colistimethate Sodium + Imipenem+Cilastatin) | 繭憲蓋願鏇鏇製願齋積 = 糧壓鑰範膚衊積繭積構 蓋衊顧淵襯觸觸醖構繭 (鹽構壓鬱願構膚淵蓋鏇, 願簾鏇鏇構襯糧觸願簾 ~ 製遞糧鑰願顧壓襯遞醖) 更多 |
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