| Description | Gatifloxacin hydrochloride (AM-1155 hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, which can inhibit the bacterial enzyme DNA rotase and topoisomerase IV. |
| In vivo | All eyes showed evidence of infection by 48 hours postinoculation with 36 of 41 eyes (87.8%) exhibiting moderate-to-severe keratitis. All eyes exhibited corneal healing by day 15, with no significant differences among groups. Three of 4 groups receiving gatifloxacin tended to have smaller fluorescein retention area scores than did the ciprofloxacin group. No eyes tested positive for Pseudomonas at the end of the study. No corneal precipitates were found following as many as 48 doses/day of gatifloxacin[1]. |
| Animal experiments | Heptanol-induced corneal ulcers in New Zealand White rabbits (n = 41; 8 females/group) were inoculated with 10(6) CFU of Pseudomonas aeruginosa. Gatifloxacin 0.3% dosing varied among 4 groups with frequencies of 16-48 doses/day (days 1-2), 3-16 doses/day (days 3-7), and maintenance dosing of 3-4 doses/day (days 8-22). Ciprofloxacin 0.3% was administered as labeled for corneal ulcers, with 44 doses on day 1, 16 doses on day 2, and 4 doses/day on days 3-21[1] |
| Target activity | Topo II:36.7 μM |
| Synonyms | AM-1155 (hydrochloride), BMS-206584 (hydrochloride), PD135432 (hydrochloride), 加替沙星盐酸盐 |
| molecular weight | 411.86 |
| Molecular formula | C19H23ClFN3O4 |
| CAS | 121577-32-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 10 mg/mL (24.28 mM), Sonication is recommended. DMSO: 4.12 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Jensen, H., et al., Comparison of ophthalmic gatifloxacin 0.3% and ciprofloxacin 0.3% in healing of corneal ulcers associated with Pseudomonas aeruginosa-induced ulcerative keratitis in rabbits. J Ocul Pharmacol Ther, 2005. 21(1): p. 36-43. 2. Fukuda, H., S. Hori, and K. Hiramatsu, Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother, 1998. 42(8): p. 1917-22. |