Pneumonia is one of the most common infectious diseases encountered worldwide. The major pathogen of community-acquired pneumonia (CAP) continues to be S. pneumoniae. In the hospital setting, S. aureus and Gram-negative bacteria are more commonly encountered and are frequently drug resistant. Delafloxacin is a novel fluoroquinolone antibiotic in development for the treatment of respiratory tract infections. It has a broad spectrum of activity that includes drug-resistant S. aureus, S. pneumoniae, and Klebsiella pneumoniae. The lowest MICs were observed for S. aureus (range, 0.004 to 0.008 mg/liter). The in vitro potency against S. pneumoniae and K. pneumoniae strains was more varied (range, 0.016 to 0.125 mg/liter and 0.06 to 1 mg/liter, respectively). As for pharmacokinetics, exposure to delafloxacin increased in a dose-dependent manner across the dose range. Cmax concentrations ranged from 2 to 71 mg/liter. AUC0–∞ values ranged from 2.8 to 152 mg · h/liter and were linear across the 2.5- to 160-mg dosing range (R2 of 0.99). The elimination half-life ranged from 0.7 to 1 h[3].
Delafloxacin/德拉沙星 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Pseudomonas aeruginosa
1, 4, 10 µg/mL
24 h
To evaluate the antibacterial activity of Delafloxacin against multidrug-resistant Pseudomonas aeruginosa (MDR-Psa), it was found that Delafloxacin demonstrated significantly better antibacterial activity than comparator fluoroquinolones in a CF sputum time-kill model, particularly at lower simulated physiologic concentrations
Antibiotics (Basel). 2023 Jun 20;12(6):1078.
Ureaplasma urealyticum
0.125-4 mg/mL
Evaluate the in vitro activity of Delafloxacin against U. urealyticum, showing low MIC values (MIC90=4 mg/mL)
Microbiol Spectr. 2022 Jun 29;10(3):e0009922.
Ureaplasma parvum
0.031-4 mg/mL
Evaluate the in vitro activity of Delafloxacin against U. parvum, showing low MIC values (MIC90=2 mg/mL)
Microbiol Spectr. 2022 Jun 29;10(3):e0009922.
Mycoplasma hominis
0.031-1 mg/mL
Evaluate the in vitro activity of Delafloxacin against M. hominis, showing low MIC values (MIC90=1 mg/mL)
Microbiol Spectr. 2022 Jun 29;10(3):e0009922.
S. aureus biofilms
9 µg/ml
48 h
Investigate the effect of Delafloxacin on antibiotic tolerance in S. aureus biofilms, showing significantly reduced bactericidal effect under arginine-deprived conditions.
Nat Commun. 2024 Aug 7;15(1):6734.
Delafloxacin/德拉沙星 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
Aerosol infection model of melioidosis
Subcutaneous injection
30, 50, and 80 mg/kg body weight
Four times daily for 21 days
To evaluate the efficacy of Delafloxacin in an aerosol infection model of melioidosis, results showed survival rates of 90% to 100% in the 50 and 80 mg/kg dose groups and 70% in the 30 mg/kg dose group. No detectable B. pseudomallei was found in the spleens of all Delafloxacin-treated cohorts at the end of the study.
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