更新于：2024-11-04
Biapenem
比阿培南
更新于：2024-11-04
概要
基本信息
原研机构- |
最高研发阶段批准上市 |
首次获批日期 (2001-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C15H18N4O4S |
InChIKeyMRMBZHPJVKCOMA-YJFSRANCSA-N |
CAS号120410-24-4 |
关联
14
项与 比阿培南 相关的临床试验Population pharmacokinetics and personalized dosing strategy of biapenem: a retrospective study of 2018-2022
Population Pharmacokinetics and Dosage Individualization of Biapenem,Meropenem,Piperacillin and Tazobactam,Tigecycline,Levofloxacin .Etc in Elderly Patients Who Was Hospitalized in Intensive Care Unit
Clinical Efficacy of Combination Therapy Based on High-dose Biapenem in CRKP Infections
100 项与 比阿培南 相关的临床结果
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100 项与 比阿培南 相关的转化医学
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100 项与 比阿培南 相关的专利（医药）
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326
项与 比阿培南 相关的文献（医药）2024-09-01Indian Journal of Medical Microbiology
Current trend of biapenem susceptibility and disc diffusion breakpoints in Enterobacterales and Pseudomonas aeruginosa
Article
作者: Veeraraghavan, Balaji ; Solaimalai, Dhanalakshmi ; Adhiya, Ranjan ; Walia, Kamini ; Abdullah, Fiza ; Bakthavatchalam, Yamuna Devi ; Jennifer, Lydia ; Srinivasan, Devishree ; Ashok, Anand
INTRODUCTION:
Biapenem has been recently approved by the Drug Controller General of India for the treatment of complicated urinary tract infections (cUTI). However, there are no assessment studies that evaluate the in-vitro activity of biapenem against contemporary ESBL-producing Indian Enterobacterales isolates. To determine the activity of biapenem against contemporary ESBLs and/or OXA-1/ampC producing Enterobacterales and Pseudomonas aeruginosa isolates.
METHODOLOGY:
Isolates were tested for susceptibility to biapenem and its comparators using the broth microdilution method. Presence of ESBLs (SHV, TEM, CTX-M) genes, OXA-1, and ampC genes (ACC, ACT, DHA, CIT/CMY, FOX) using multiplex PCR.
RESULTS:
Against ESBL with OXA-1 and/or ampC-producing E. coli, ESBL-K. pneumoniae, and cephalosporin-resistant P. aeruginosa, biapenem showed in-vitro activity similar to that of meropenem. Overall, a biapenem disc concentration of 10 μg provided no error rates for testing E. coli, K. pneumoniae, and P. aeruginosa isolates.
CONCLUSION:
It is more accurate to test biapenem at a 10 μg disc concentration and apply more stringent disc diffusion breakpoints for interpretation.
2024-06-01Journal of global antimicrobial resistance
In vitro activity, pharmacodynamic profile and dose optimization of biapenem against NDM and OXA-48-like carbapenemase-producing Klebsiella pneumoniae: A multicentre study in Thailand
Article
作者: Boonmee, Patcharapa ; Pungcharoenkijkul, Supanun ; Santimaleeworagun, Wichai ; Nulsopapon, Parnrada ; Nasomsong, Worapong ; Siangtrong, Chirakhana
BACKGROUND:
Biapenem (BIPM) exhibited a less efficient substrate for various metallo-β-lactamase (MBL) than other carbapenems.
OBJECTIVE:
We aimed to evaluate in vitro susceptibility data of BIPM and optimal dose based on Monte Carlo simulation to extend treatment options.
METHODS:
We collected 192 carbapenem-resistant Klebsiella pneumoniae (CRKP) clinical isolates from unique patients among multicentres in Thailand, from June 2019 to March 2023. BIPM disk diffusion and broth-microdilution testing were performed to obtain minimum inhibitory concentration (MIC). Each BIPM regimen was simulated using the Monte Carlo technique to calculate the probability of target attainment (PTA) and the cumulative fraction of response (CFR).
RESULTS:
The most common genotypes among 192 CRKP isolates were blaOXA-48 (62.3%), blaOXA-48+blaNDM (22.6%) and blaNDM (15.1%). BIPM showed 22.4 and 28.6% susceptible rate when interpreted at clinical breakpoints of 1 and 2 mg/L. The MIC50 and MIC90 of BIPM against CRKP were 8 and 32 mg/L. The BIPM dosing regimens of 300 mg q 6 h infused 6 h and 600 mg q 8 h infused 8 h met the PTA target of %fTime >MIC at 50%, 75% and 100% against isolates MICs of ≤2 mg/L. Based on CFR ≥90%, no BIPM regimens were effective against all the studied CRKP isolates.
CONCLUSION:
BIPM exhibited a partially susceptible rate among the CRKP isolates in Thailand. The current suggested dose of BIPM with prolonged infusion appears appropriate regimen against CRKP MICs of ≤2 mg/L. However, the empirical use of BIPM for severe CRE infection is not recommended unless the susceptibility has been confirmed.
2024-04-01Drug metabolism and pharmacokinetics
Preferential meropenem absorption activated by 1α,25-dihydroxyvitamin D3 and shared with foscarnet, a phosphate transporter substrate, in the rat ileum
Article
作者: Saito, Toshihide ; Oda, Masako ; Saitoh, Hiroshi ; Ichimura, Yuichi
Meropenem (MEPM) is used for the treatment of serious infectious diseases solely as. INJECTABLE: Therefore, the development of an oral formulation would expand its clinical utility. To this end, an exact understanding of the absorption characteristics of MEPM is essential. In this study, MEPM absorption in the rat small intestine was investigated using an in situ loop technique and an in vitro diffusion chamber method. The disappearance ratios of MEPM (0.1 mM) were in the order of ileum > duodenum > jejunum. The extensive MEPM disappearance in the ileum was significantly reduced in the presence of foscarnet, a Na+-dependent phosphate transporter (NaPi-T) substrate, whereas glycylsarcosine, thiamine, taurocholic acid, and biapenem had no effects. The mucosal-to-serosal (M-to-S) permeation of MEPM across the rat ileal segments was very small under normal experimental conditions. However, on addition of 1α,25-dihydroxyvitamin D3 (1,25(OH)2D3) to the experimental medium, the M-to-S permeation of MEPM markedly increased, showing a more than 7-fold greater apparent permeation coefficient. The present results suggest that MEPM is preferentially absorbed in the rat ileum, sharing with foscarnet, and that 1,25(OH)2D3 potentially activates the absorption of MEPM there. A likely candidate for involvement in MEPM absorption was NaPi-T or a related transporter.
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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 |
|---|---|---|---|
| 膀胱炎 | 日本 | 2001-10-02 | |
| 出血性败血症 | 日本 | 2001-10-02 | |
| 肺脓肿 | 日本 | 2001-10-02 | |
| 腹膜炎 | 日本 | 2001-10-02 | |
| 肺炎 | 日本 | 2001-10-02 | |
| 肾盂肾炎 | 日本 | 2001-10-02 | |
| 继发感染 | 日本 | 2001-10-02 | |
| 细菌感染 | - | - | 2001-01-01 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 泌尿道感染 | 临床2期 | 中国 | 2009-06-19 | |
| 呼吸道感染 | 临床2期 | 中国 | - |
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