Delving into the Latest Updates on Biapenem with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Biapenem (JAN/USAN/INN)

+ [11]

Target

PBPs

Action

inhibitors

Mechanism

PBPs inhibitors(Bacterial penicillin-binding protein inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System DisordersRespiratory Diseases+ [2]

Active Indication

CystitisHemorrhagic SepticemiaLung Abscess+ [5]

Inactive Indication

Complicated urinary tract infection

Originator Organization-

Active Organization

Meiji Seika Pharma Co., Ltd.

Nanjing Simcere Dongyuan Pharmaceutical Co. Ltd.

Inactive Organization

Wyeth Ltd. (India)

Beijing Furuikangzheng Medicine Technology Research Institute

Drug Highest PhaseApproved

First Approval Date

(01 Jan 2001),

Bacterial Infections

Regulation-

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Structure/Sequence

Molecular FormulaC15H18N4O4S

InChIKeyMRMBZHPJVKCOMA-YJFSRANCSA-N

CAS Registry120410-24-4

Clostridium difficile (C. difficile) stands as a primary cause of health-care-associated colitis in adults; however, extraintestinal manifestations of C. difficile, particularly bacteremia, are exceptionally rare. In this report, we document a case of an elderly male with multiple comorbidities who presented with an acute onset of fever. Diagnostic testing revealed the presence of concurrent bacteremia involving C. difficile and Klebsiella pneumonia. The multilocus sequence typing analysis identified this C. difficile strain as ST81. After receiving a combination treatment of vancomycin and biapenem, the patient successfully recovered and was subsequently discharged. This case report elucidates the clinical presentation and treatment strategies for C. difficile ST81 bacteremia, underscoring the critical need for heightened monitoring of extraintestinal infections in high-risk patients.

01 Nov 2024·Microbiological Research

Non-antibiotic pharmaceutical phenylbutazone binding to MexR reduces the antibiotic susceptibility of Pseudomonas aeruginosa

Article

Author: Meng, Qinghong ; Yu, Dan ; Yao, Kaihu ; Li, Yue ; Yuan, Lin ; Zhang, Youwen ; You, Xuefu ; Gao, Wei ; Yang, Yan ; Wang, Qing ; Shi, Wei ; Dong, Limin ; Sun, Lang

Antimicrobial resistance has been an increasingly serious threat to global public health. The contribution of non-antibiotic pharmaceuticals to the development of antibiotic resistance has been overlooked. Our study found that the anti-inflammatory drug phenylbutazone could protect P. aeruginosa against antibiotic mediated killing by binding to the efflux pump regulator MexR. In this study, antibiotic activity against P. aeruginosa alone or in combination with phenylbutazone was evaluated in vitro and in vivo. Resazurin accumulation assay, transcriptomic sequencing, and PISA assay were conducted to explore the underlying mechanism for the reduced antibiotic susceptibility caused by phenylbutazone. Then EMSA, ITC, molecular dynamic simulations, and amino acid substitutions were used to investigate the interactions between phenylbutazone and MexR. We found that phenylbutazone could reduce the susceptibility of P. aeruginosa to multiple antibiotics, including parts of β-lactams, fluoroquinolones, tetracyclines, and macrolides. Phenylbutazone could directly bind to MexR, then promote MexR dissociating from the mexA-mexR intergenic region and de-repress the expression of MexAB-OprM efflux pump. The overexpressed MexAB-OprM pump resulted in the reduced antibiotic susceptibility. And the His41 and Arg21 residues of MexR were involved in the phenylbutazone-MexR interaction. We hope this study would imply the potential risk of antibiotic resistance caused by non-antibiotic pharmaceuticals.

01 Oct 2024·Acta medica Okayama

Phenotypic and Genetic Characteristics of Carbapenemase-Producing Enterobacterales Isolates at Okayama University Hospital.

Article

Author: Iio, Koji ; Fukushima, Shinnosuke ; I Putu Bayu Mayura ; Matsushita, Osamu ; Tsuji, Shuma ; Gotoh, Kazuyoshi ; Miyoshi, Makoto ; Hagiya, Hideharu

Spread of carbapenemase-producing Enterobacterales (CPE) is an ongoing public health issue worldwide, including in Japan. In this study, we investigated the phenotypic and genetic characteristics of CPE isolates at Okayama University Hospital over the 5 years (2013-2018) prior to the outbreak of the 2019 coronavirus pandemic. Of 24 carbapenem-resistant Enterobacterales isolated during the study period, we identified 8 CPE isolates harboring blaIMP-1 (5 isolates) and blaIMP-6 genes (3 isolates). Bacterial species and carbapenem susceptibility patterns exhibited diversity. Minimum inhibitory concentrations (MICs) of meropenem were generally higher than those of imipenem and biapenem. Results of pulsed-field gel electrophoresis demonstrated that neither clonal nor plasmid-mediated outbreaks of blaIMP-harboring CPE isolates have developed at our hospital. One Klebsiella oxytoca isolate showed a high MIC (128 μg/mL) of meropenem, which could be explained by the high plasmid copy number. Subsequent analysis of this isolate may elucidate the intricacies of carbapenem resistance profiles among CPE isolates. Collectively, our findings underscore the necessity for ongoing genetic surveillance of CPE, complemented by tailored approaches for infection prevention and control.

100 Deals associated with Biapenem

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External Link

KEGG	Wiki	ATC	Drug Bank
D01057	Biapenem	J01DH05	DB13028

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cystitis	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Hemorrhagic Septicemia	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Lung Abscess	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Peritonitis	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Pneumonia	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Pyelonephritis	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Secondary infection	Japan	Meiji Seika Pharma Co., Ltd.	02 Oct 2001
Bacterial Infections	-	-	01 Jan 2001

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Complicated urinary tract infection	Preclinical	China	Beijing Furuikangzheng Medicine Technology Research Institute	19 Jun 2009
Bacterial Infections	Preclinical	United States	Wyeth Ltd. (India)	-
Bacterial Infections	Preclinical	United States	Wyeth Ltd. (India)	-
Respiratory Tract Infections	Preclinical	China	Beijing Furuikangzheng Medicine Technology Research Institute	-