| Description | 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. |
| In vivo | 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. |
| molecular weight | 376.388 |
| Molecular formula | C18H21FN4O4 |
| CAS | 119354-43-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. He XJ, et al. Efficacy and Safety of Antofloxacin-Based Triple Therapy for Helicobacter pylori Eradication Failure in China [published online ahead of print, 2021 Feb 8]. Dig Dis Sci. 2021;10.1007/s10620-021-06856-z. 2. Liu L, et al. Modulation of pharmacokinetics of theophylline by antofloxacin, a novel 8-amino-fluoroquinolone, in humans. Acta Pharmacol Sin. 2011;32(10):1285-1293. 3. Zhou YF, et al. In Vivo Pharmacokinetic and Pharmacodynamic Profiles of Antofloxacin against Klebsiella pneumoniae in a Neutropenic Murine Lung Infection Model. Antimicrob Agents Chemother. 2017;61(5):e02691-16. Published 2017 Apr 24. |