ChemicalBook CAS DataBase List 873888-67-6

873888-67-6

Name	Antofloxacin hydrochloride
CAS	873888-67-6
Molecular Formula	C18H22ClFN4O4
MDL Number	MFCD28124371
Molecular Weight	412.85
MOL File	873888-67-6.mol

Hazard Information

Uses

Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species[1][2][3].

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 (Pharmacokinetic Analysis)^[3]
Dosage:	2.5~160 mg/kg
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.

IC 50

Quinolone

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. DOI: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. DOI:10.1038/aps.2011.78
[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. DOI:10.1128/AAC.02691-16

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