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Delafloxacin meglumine

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Delafloxacin meglumine Basic information

Product Name:
Delafloxacin meglumine
Synonyms:
  • 100850
  • ABT 492 meglumine (Delafloxacin meglumine)
  • Delafloxacin meglumine (ABT492 meglumine
  • (2R,3R,4R,5S)-2,3,4,5-tetrahydroxy-6-(MethylaMino)hexyl 1-(6-aMino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate
  • ABT 492 MegluMine
  • ABT492 MegluMine
  • ABT-492 MegluMine
  • Delafloxacin (MegluMine)
CAS:
352458-37-8
MF:
C25H29ClF3N5O9
MW:
635.98
Product Categories:
  • API
Mol File:
352458-37-8.mol
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Delafloxacin meglumine Chemical Properties

storage temp. 
under inert gas (nitrogen or Argon) at 2–8 °C
solubility 
Soluble in DMSO
form 
Powder
color 
Off-white to yellow
InChIKey
AHJGUEMIZPMAMR-KUAVVOKVNA-N
SMILES
[C@@H](O)([C@@H](O)CNC)[C@H](O)[C@H](O)CO.ClC1C(N2CC(O)C2)=C(F)C=C2C(=O)C(C(=O)O)=CN(C3N=C(N)C(F)=CC=3F)C=12 |&1:0,2,7,9,r|
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Delafloxacin meglumine Usage And Synthesis

Physical Form

Solid

Description

Delafloxacin meglumine (Baxdela, WQ-3034, ABT-492, RX-3341; Melinta Therapeutics) was approved by the U.S. Food and Drug Administration (FDA) in June 2017 for the treatment of acute bacterial skin and skin structure infections on the basis of data from two phase III trials.

Uses

Delafloxacin is a broad-spectrum anionic fluoroquinolone and its distinct chemical structure increases its potency in acidic environments. It is known to inhibit DNA replication and repair by targeting DNA gyrase and topoisomerase IV. Delafloxacin is administered via both oral and parenteral routes. It has potent activity against methicillin-resistant Staphylococcus aureus and Streptococci, and is also effective against Enterobacteriaceae and Pseudomonas aeruginosa.

Indications

Delafloxacin meglumine (Baxdelae Melinta) is a fluoroquinolone antibacterial agent with properties that are most similar to other members of this class, such as levofloxacin, moxifloxacin, and ciprofloxacin. It is supplied in formulations for oral and intravenous administration. It is indicated for the treatment of adults with ABSSSIs caused by susceptible isolates of the gram-positive bacteria Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillin-susceptible isolates), Staphylococcus haemolyticus, Staphylococcus lugdunensis, Streptococcus agalactiae, Streptococcus anginosus group (including S. anginosus, S. intermedius, and S. constellatus), Streptococcus pyogenes, and Enterococcus faecalis, and the gram-negative bacteria Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, and Pseudomonas aeruginosa. It is the first fluoroquinolone to be demonstrated to be effective in the treatment of infections caused by MRSA, and its spectrum of antibacterial action, which also includes problem pathogens such as Pseudomonas aeruginosa, is broader than that of other antimicrobial agents that are indicated for the treatment of ABSSSIs[1].

Biological Activity

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine is a broad spectrum fluoroquinolone antibiotic. Delafloxacin has a wide range of activity against drug-resistant Staphylococcus aureus, Streptococcus pneumoniae and Klebsiella pneumoniae.

in vivo

Delafloxacin (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against S. aureus. Against all four strains are observed a decrease of 1.5 to 2.2 log10 CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log10 kill from initial burden for all S. aureus strains[1].
Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t1/2=0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively)[1].

Animal Model:Mice with a neutropenic murine lung infection model (four S. aureus, four S. pneumoniae, and four K. pneumoniae strains)[1]
Dosage:The total daily doses vary from 0.156 to 640 mg/kg/24 h
Administration:0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injection
Result:Inhibited S. aureus strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively.
Inhibited S. pneumoniae strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively.
Inhibited K. pneumonia strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively.
Animal Model:Neutropenic mice[1]
Dosage:2.5, 10, 40, and 160 mg/kg; 0.2 mL
Administration:Subcutaneous injection; 24 h
Result:The maximum drug concentrations (Cmax) concentrations ranged from 2 to 71 mg/L. AUC0-∞ values ranged from 2.8 to 152 mg?h/L and were linear across the 2.5- to 160-mg dosing range. The elimination half-life (t1/2) ranged from 0.7 to 1 h.

IC 50

Quinolone

References

[1] Daniel A. Hussar, Molly A. Walter. “Delafloxacin meglumine, Meropenem trihydrate/vaborbactam, Secnidazole, and Benznidazole.” ACS Applied Bio Materials 58 2 (2018): Pages 223-227.

Delafloxacin meglumineSupplier

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