Delafloxacin Meglumine is the meglumine salt of Delafloxacin. It is a small molecule and broad-spectrum fourth-generation fluoroquinolone antibiotic. It was developed by Melinta Therapeutics. It is more active than other quinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Delafloxacin Meglumine is soluble in DMSO.
| Mechanism of Action | Delafloxacin Meglumine inhibits DNA replication and repair by targeting two enzymes: DNA gyrase (topoisomerase II) and topoisomerase IV. This prevents the relaxation of positive supercoils introduced during DNA elongation. It has a balanced activity against both of these enzymes and this equipotent enzyme inhibition should limit resistance selection since double mutations are rare genetic events. In addition, it has a distinct chemical structure that increases its potency in acidic environments. It exhibits concentration-dependent bacteriocidal activity. |
| Spectrum | Delafloxacin Meglumine has broad-spectrum activity against Gram-positive bacteria (ie Staphylococcus and Streptococcus), Gram-negative bacteria (ie. E. coli, Klebsiella pneumonia, Pseudomonas aeruginosa), atypical bacteria, and anaerobic bacteria. It has antibacterial activity against fluoroquinolone-resistant isolates. In vitro activity is similar to levofloxacin. It has in vitro and in vivo efficacy against MSSA and MRSA. |
| Microbiology Applications |
Delafloxacin Meglumine has activity against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible Staphylococcus aureus (MSSA), Streptococci, Enterobacteriaceae and Pseudomonas. In contrast to most fluoroquinolones that are switterionic, it has dual-targeting anionic character, which results in an increase in its accumulation in bacteria and cells at acidic pH. This property means it has an advantage in acidic environments such as intracellular environments and biofilms. Formulations containing Delafloxacin have been used against the bacteria causing acute bacterial skin and skin structure infections (ABSSSIs) and it was in this capacity that FDA approval was granted in June 2017. |
| Molecular Formula | C19H21ClFN3O3 · HCl |
| References |
Gunderson SM, Hayes RA, Quinn JP and Danziger LH (2004) In vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Antimicrob Agents Chemother. 48(1):203-208 PMID 14693540 Hoover et al (2017) Clinical pharmacology of delafloxacin in patients with hepatic impairment. J. Clin. Pharmacol 57(3):328-335 PMID 27570245 Jorgensen SCJ, Mercuro NJ, Davis SL, Rybak MJ (2018) Delafloxacin: Place in therapy and review of microbiologic, clinical and pharmacologic properties. Infect. Dis. Ther. 7(2):197-217 PMID 29605887 Lepak AJ and Andes DR (2016) In vivo pharmacodynamic target assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a murine lung infection model. Antimicrob. Agents Chemother. 60(8):4764-4769 PMID 27216072 Markham A (2017) Delafloxacin: First Global Approval. Drugs 77:1481–1486 |