Antofloxacin is a well-tolerated, orally active, and broad-spectrum 8-amino-fluoroquinolone compound that exhibits potent antibacterial properties. It demonstrates superior activity against gyrA mutation-positive Helicobacter pylori strains, particularly in strains with mutations in the Asn87 position, when compared to levofloxacin. Additionally, Antofloxacin acts as a weak but reversible inhibitor of CYP1A2 and is clinically used to treat infections caused by various bacterial species.

Antofloxacin (2.5~160 mg/kg; s.c.; 24 hours) penetration ratio ranges from 1.22 to 1.54 for the total drug concentrations and is independent of the dose levels[3].

Antofloxacin increases the plasma theophylline concentration, partly by acting as a mechanism based inhibitor of CYP1A2. Antofloxacin inhibits the formation of the three metabolites of theophylline was time-, concentration- and NADPH-dependent, which is characteristic of mechanism-based inhibition[2]. Animal Model: Mice[3]Dosage: 2.5~160 mg/kg (Pharmacokinetic Analysis) Administration: S.c.; 24 hours Result: Penetration ratio ranged from 1.22 to 1.54 for the total drug concentrations and was independent of the dose levels.