Delafloxacin injection (delafloxacin meglumine) was approved by the U.S. FDA on June 19, 2017, and was marketed by Melinta in the U.S. under the trade name Baxdela.
The resistance of almost all gram-negative and gram-positive pathogens to fluoroquinolone antibiotics has increased since the 1990s. Therefore, it is an important task of medical research to develop new antibacterial drugs with high antibacterial activity, antipathogen effect, higher safety, and showing enhanced pharmacokinetic properties. Drafloxacin is a new type of fluoroquinolone compound, which is characterized by resistance to Gram-positive bacteria (such as MRSA) and Gram-negative pathogens (including quinolone-resistant Escherichia coli and Klebsiella pneumoniae) Broad-spectrum antibacterial activity. With its low MIC value against Gram-positive bacteria (especially MRSA) and anaerobic bacteria and its activity against Gram-negative bacteria, drafloxacin has a good application prospect in the treatment of bacterial infections. There are two routes of administration of drafloxacin: intravenous injection and oral administration, with a wide range of applications and good clinical application value. The solubility of drafloxacin meglumine in different pH media is low. The sulfobutyl beta cyclodextrin (SBECD) SBE-β-CD is used for inclusion and solubilization of drafloxacin meglumine. It becomes a freeze-dried powder injection, which simplifies the prescription composition and improves the safety and bioavailability.
As the problem of antimicrobial resistance has become more and more serious, the advent of new antimicrobial drugs can cope with this problem to a certain extent. As a new broad-spectrum fluoroquinolone antibacterial drug, drafloxacin provides a new choice for dealing with acute bacterial skin and skin structure infections. In addition, since drafloxacin shows extensive antibacterial activity against a large number of highly resistant bacteria, it may also be used as an alternative treatment for a variety of serious infections, including complex skin infections, respiratory infections, and endocarditis. , Complex urinary tract infections and other severe infectious diseases are expected to become a powerful tool for clinically fighting drug-resistant bacterial infections and have potential market value.
The molecular formula of drafloxacin is: C18H12ClF3N4O4,
Relative molecular weight is 440.76
Drafloxacin injection (BAXDELA) contains 300 mg of freeze-dried powder injection and 2400 mg of sulfobutyl beta cyclodextrin (SBECD). The molar ratio of drug molecule to sulfobutyl beta cyclodextrin sodium is 1:1.4.