Delving into the Latest Updates on Chinfloxacin Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Chinfloxacin

Target

Bacterial DNA gyrase x Topoisomerase IV

Mechanism

Bacterial DNA gyrase inhibitors, Topoisomerase IV inhibitors

Therapeutic Areas

Infectious DiseasesRespiratory Diseases

Active Indication-

Inactive Indication

Bacterial InfectionsPneumoniaSoft Tissue Infections

Originator Organization

Beijing Xiehe Bioengineering United Company

Active Organization-

Inactive Organization

Zhejiang Medicine Co., Ltd.Beijing Xiehe Bioengineering United Company

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC21H23ClF3N3O4

InChIKeyCHIJJPUAAHFCSG-OEQYQXMYSA-N

CAS Registry1359213-95-8

View All Structures (2)

OBJECTIVESTo evaluate the in vivo antibacterial efficacy of chinfloxacin, a novel fluoroquinolone, in murine systemic and local infection models.METHODSThe efficacy of chinfloxacin in systemic infection was evaluated in a mouse peritonitis model using isolates of methicillin-susceptible Staphylococcus aureus (MSSA, n = 3), methicillin-resistant Staphylococcus aureus (MRSA; n = 1), penicillin-intermediate Streptococcus pneumoniae (PISP; n = 1), penicillin-resistant S. pneumoniae (PRSP; n = 2), vancomycin-susceptible Enterococcus faecalis (VSE; n = 1), vancomycin-resistant E. faecalis (VRE; n = 2), Escherichia coli (n = 3) and Klebsiella pneumoniae (n = 2). The local infections included mouse pulmonary infections caused by penicillin-susceptible S. pneumoniae (PSSP; n = 1), PRSP (n = 1) and K. pneumoniae (n = 2).RESULTSIn the mouse systemic infection model, chinfloxacin demonstrated potent activity against MSSA [50% effective dose (ED(50)) 2.28-4.15 mg/kg], MRSA (ED(50) 14.75 mg/kg), PISP (ED(50) 6.20 mg/kg), PRSP (ED(50) 3.51-5.03 mg/kg), VSE (ED(50) 25.02 mg/kg), VRE (ED(50) 5.18-15.39 mg/kg), E. coli (ED(50) 1.25-1.90 mg/kg) and K. pneumoniae (ED(50) 2.92-8.28 mg/kg). The therapeutic efficacy of chinfloxacin was generally similar to (P > 0.05) that of moxifloxacin, significantly higher (P < 0.01 or P < 0.05) than that of levofloxacin in Gram-positive isolate infections (MSSA, MRSA, PISP, PRSP, VSE and VRE), and less than that of levofloxacin against E. coli and K. pneumoniae infections (P < 0.01). In the mouse pulmonary infection model, chinfloxacin showed potent activity towards S. pneumoniae (higher than levofloxacin and ciprofloxacin) and K. pneumoniae (lower than levofloxacin and similar to or higher than ciprofloxacin) infections.CONCLUSIONSThe results validated the potent efficacy of chinfloxacin in vivo. The high efficacy of chinfloxacin in murine systemic and local infections warrants investigation of its clinical use.

01 Jan 2012·ChemotherapyQ4 · MEDICINE

In vitro Antibacterial Activity of Chinfloxacin, a New Fluoroquinolone Antibiotic

Q4 · MEDICINE

Article

Author: Yang, Xin-Yi ; You, Xuan-Wang ; Cen, Shan ; Yuan, Min ; You, Xue-Fu ; Guo, Hui-Yuan ; Li, Guo-Qing ; Zhang, Wei-Xin ; Lou, Ren-Hui ; Hu, Xin-Xin ; Li, Cong-Ran ; Jiang, Jian-Dong

Background: Chinfloxacin is a novel synthetic fluoroquinolone with a structure similar to moxifloxacin. The in vitro activity of chinfloxacin was evaluated in the current study. Method: Chinfloxacin was tested against a total of 1,739 clinical isolates representing 23 species using the agar dilution method. Studies of bactericidal activity, including minimum bactericidal concentrations (MBC) and time-kill curve determinations, were conducted according to the recommendations of the Clinical and Laboratory Standards Institute. Results: Minimum inhibitory concentrations (MIC)50s and MIC90s of chinfloxacin were found to be the same or 2-fold lower than those of moxifloxacin against gram-positive isolates except for Streptococcus pyogenes (against which chinfloxacin showed similar MIC50 as moxifloxacin but 2-fold higher MIC90), and the same as or 2-fold higher than those of moxifloxacin against gram-negative isolates. Chinfloxacin showed potent bactericidal activity with MBC/MIC ratios in the range of 1–2 for almost all the isolates tested. Time-kill curves further demonstrated chinfloxacin as a concentration-dependent bactericidal agent usually effective at concentrations of 2 MIC or higher. Conclusion: Chinfloxacin showed similar in vitro activity as moxifloxacin.

100 Deals associated with Chinfloxacin Hydrochloride

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 1	CN	Beijing Xiehe Bioengineering United Company	-
Bacterial Infections	Phase 1	CN	Zhejiang Medicine Co., Ltd.	-
Pneumonia	Phase 1	CN	Beijing Xiehe Bioengineering United Company	-
Pneumonia	Phase 1	CN	Zhejiang Medicine Co., Ltd.	-
Soft Tissue Infections	Phase 1	CN	Beijing Xiehe Bioengineering United Company	-
Soft Tissue Infections	Phase 1	CN	Zhejiang Medicine Co., Ltd.	-