Meeting the Unmet Need in the Management of MDR Gram-Positive Infections with Oral Bactericidal Agent Levonadifloxacin

Abstract

Levonadifloxacin (intravenous) and its oral prodrug alalevonadifloxacin are broad-spectrum antibacterial agents developed for the treatment of difficult-to-treat infections caused by multidrug-resistant Gram-positive bacteria, especially methicillin-resistant Staphylococcus aureus, atypical bacteria, anaerobic bacteria, and biodefence pathogens as well as Gram-negative bacteria. Levonadifloxacin has a well-defined mechanism of action involving a strong affinity for DNA gyrase as well as topoisomerase IV. Alalevonadifloxacin with widely differing solubility and oral bioavailability has pharmacokinetic profile identical to levonadifloxacin. Unlike existing MRSA drugs such as vancomycin and linezolid, which cause unfavorable side effects like nephrotoxicity, bone-marrow toxicity, and muscle toxicity, levonadifloxacin/alalevonadifloxacin has demonstrated superior safety and tolerability features with no serious adverse events. Levonadifloxacin/alalevonadifloxacin could be a useful weapon in the battle against infections caused by resistant microorganisms and could be a preferred antibiotic of choice for empirical therapy in the future.

Integrated Virtual Screening and MD Simulation Study to Discover Potential Inhibitors of Mycobacterial Electron Transfer Flavoprotein-Oxidoreductase

“…Levonadi oxacin, a novel broad-spectrum uoroquinolone, effectively targets challenging infections caused by multidrug-resistant Gram-positive, intracellular, atypical, anaerobic, and Gram-negative bacteria, particularly respiratory pathogens, with superior safety, tolerability, and minimal drug-drug interactions attributed to its lack of CYP interaction [59]. Levonadi oxacin demonstrates superior penetration into alveolar macrophages (AMs) and epithelial lining uid (ELF), with mean values surpassing those reported for levo oxacin and moxi oxacin.…”

Formulation and Evaluation of Film-Coated Alalevonadifloxacin Mesylate Tablet using Opadry®

“…AFM a highly water-soluble L-alanine ester mesylate salt, has an oral bioavailability of 89% and is being explored as the drug's oral prodrug formulation. [3][4][5] Opadry® yellow, a shaded film-coating method that has been discovered to hide AFM from light action for a long time without changing AFM's release profile. 6 It is a prepared formulation, easy to prepare, takes little time to prepare and apply, and utilizes common coating equipment that is simple to clean.…”