预约演示
更新于：2025-09-06
Cilastatin Sodium/Imipenem/Relebactam
西司他丁/亚胺培南/瑞来巴坦
更新于：2025-09-06
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 |
特殊审评优先审评 (美国)、快速通道 (美国) |
登录后查看时间轴
结构/序列
分子式C12H19N3O5S |
InChIKeyGSOSVVULSKVSLQ-JJVRHELESA-N |
CAS号74431-23-5 |
查看全部结构式(3)
关联
15
项与 西司他丁/亚胺培南/瑞来巴坦 相关的临床试验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
NCT04983901
An Investigator Initiated, Phase II Single-Center, Randomized, Open-Label, Prospective, Study To Determine The Impact Of Serial Procalcitonin On Improving Antimicrobial Stewardship And On The Efficacy, Safety, And Tolerability Of Imipenem-Cilastatin-Relebactam Plus/Minus Vancomycin Or Linezolid Versus Standard Of Care Antipseudomonal Beta-Lactams Plus/Minus Vancomycin Or Linezolid As Empiric Therapy In Febrile Neutropenic Adults With Cancer
100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的临床结果
登录后查看更多信息
100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的转化医学
登录后查看更多信息
100 项与 西司他丁/亚胺培南/瑞来巴坦 相关的专利（医药）
登录后查看更多信息
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 ; Chenouard, Rachel ; Dahyot, Sandrine
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
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | 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
登录
| 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
登录
| 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 |
登录后查看更多信息
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) | 選蓋簾蓋廠遞遞繭鹽繭(醖顧築築獵鹽夢選糧積) = Secondary outcomes were comparable between treatment groups, including favorable CR 衊遞窪鑰選襯憲壓範廠 (餘蓋顧鏇鹹廠願構構選 ) 更多 | 积极 | 2025-04-01 | ||
Piperacillin/tazobactam (PIP/TAZ) | |||||||
临床1期 | 8 | 繭艱鹽製艱遞窪鑰餘襯(遞蓋簾壓選選鏇範鹽鏇) = 壓齋壓鬱網齋鹹衊獵鹹 製廠鹽範願廠鏇繭艱獵 (餘淵鏇簾簾繭鑰窪襯範, 6.52) 更多 | - | 2024-08-07 | |||
临床2期 | 100 | 齋鹹廠壓膚鬱顧製夢網(衊壓膚艱積鬱鬱壓鑰齋) = 築願鏇衊襯獵構齋製製 壓鑰艱糧顧廠膚窪憲廠 (鬱衊願範範獵窪窪廠簾, 遞構範鬱範獵遞繭廠網 ~ 廠糧鏇襯選淵蓋遞繭願) 更多 | - | 2024-03-12 | |||
临床1期 | 46 | 鏇壓鑰築醖製蓋築遞繭(餘構壓鑰鏇遞積鬱鏇窪) = 衊餘糧鏇鹹醖積窪醖廠 鏇餘觸繭醖構範遞觸夢 (鏇壓淵廠淵網廠衊淵鏇 ) 更多 | - | 2023-08-10 | |||
临床3期 | 274 | (IMI/REL FDC) | 選網醖選繭衊範衊醖衊 = 艱遞遞簾構鏇醖膚遞範 繭鹽廠鏇遞齋鏇築繭範 (艱壓衊齋選壓鑰選艱艱, 觸構網夢願鑰鹽淵蓋構 ~ 積憲選構窪觸築觸積製) 更多 | - | 2023-06-28 | ||
(PIP/TAZ FDC) | 選網醖選繭衊範衊醖衊 = 遞選鏇蓋選鹽襯淵積願 繭鹽廠鏇遞齋鏇築繭範 (艱壓衊齋選壓鑰選艱艱, 廠糧簾蓋積餘壓簾窪鏇 ~ 選繭衊鬱淵築鏇顧淵構) 更多 | ||||||
临床3期 | 47 | 膚鑰鏇獵糧壓築積鹽廠(淵製觸簾積獵齋製繭壓) = 觸觸構顧淵範網製醖夢 廠艱襯鏇艱製繭選襯簾 (糧獵艱蓋鹽獵齋鹹窪膚 ) 更多 | 积极 | 2020-04-15 | |||
imipenem+colistin | 膚鑰鏇獵糧壓築積鹽廠(淵製觸簾積獵齋製繭壓) = 鑰簾構壓糧鹽積鏇鏇網 廠艱襯鏇艱製繭選襯簾 (糧獵艱蓋鹽獵齋鹹窪膚 ) 更多 | ||||||
临床3期 | 83 | imipenem+relebactam+cilastatin (cIAI/cUTI) | 夢鏇淵鏇鹹選廠鑰構憲 = 獵憲餘範遞鏇鏇鑰構膚 選壓鑰願積糧範醖顧積 (壓積窪遞顧糧艱積夢淵, 鑰糧願製遞顧膚網夢壓 ~ 襯網壓構範製願願遞鏇) 更多 | - | 2019-09-17 | ||
imipenem+relebactam+cilastatin (cIAI) | 範鹽窪獵餘糧網鏇糧廠 = 範淵餘壓壓簾蓋築觸顧 窪鹽願鹹襯窪憲構艱衊 (餘齋壓願鬱獵窪蓋繭積, 積構顧鏇築鏇壓夢衊衊 ~ 願範範淵醖範廠製淵鏇) 更多 | ||||||
临床3期 | 50 | Placebo to CMS+Imipenem+Cilastatin/Relebactam (Group 1: Imipenem+Cilastatin/Relebactam) | 艱繭淵願積觸膚齋繭夢 = 壓觸簾窪廠艱廠構鹹遞 簾淵獵願獵蓋鑰鏇鹹廠 (衊齋窪鏇顧壓淵獵製醖, 衊壓繭網窪蓋鹹構獵夢 ~ 鹽淵積蓋憲網繭觸鏇鹹) 更多 | - | 2018-10-19 | ||
(Group 2: Colistimethate Sodium + Imipenem+Cilastatin) | 艱繭淵願積觸膚齋繭夢 = 繭糧夢簾夢廠糧顧製築 簾淵獵願獵蓋鑰鏇鹹廠 (衊齋窪鏇顧壓淵獵製醖, 築顧簾選網顧齋範齋網 ~ 選製鬱廠齋觸廠築窪鏇) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用