Delafloxacin meglumine

Cell lines

S. aureus, S. pneumoniae, and K. pneumoniae

Preparation method

The solubility of this compound in DMSO is soluble. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.008-1 mg/l

Applications

The median free drug AUC / MIC associated with S. aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae groups was 1.45, 0.56, and 40.3, respectively. The AUC/MIC targets of the 1-log kill endpoint were 2 to 5 times higher. Delafloxacin has shown in vitro and in vivo efficacy against a variety of pathogens, including those that are phenotypic resistant to other classes. These results have potential relevance to clinical dose selection and assessment of the sensitivity breakpoints for delafloxacin treatment of lower respiratory tract infections involving these pathogens.

Animal models

A neutropenic murine lung infection model

Dosage form

2.5mg/kg,10mg/kg,40mg/kg and 160mg/kg (s.c.)

Application

At the beginning of treatment, the lung capacity of the mice was 6.3 ± 0.09 log10 CFU. In control mice, the bioburden increased by 2.1 ± 0.44 log10 CFU / lung during the study period. As the delafloxacin dose increased, a relatively steep dose-response relationship was observed. The maximum biomass reduction ranges from 2 log10 to more than 4 log10.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Lepak AJ, Andes DR. In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4764-9. doi: 10.1128/AAC.00647-16. PMID: 27216072; PMCID: PMC4958193..