Gatifloxacin is a fluoroquinolone antibiotic that inhibits bacterial type II topoisomerases (IC50=13.8μg/ml for S. aureus topoisomerase IV; IC50=0.109μg/ml for E. coli DNA gyrase) but shows low inhibition against HeLa cell topoisomerase II (IC50=265μg/ml)[3]. Gatifloxacin (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis[4].
Gatifloxacin/加替沙星 细胞实验
Cell Line
Concentration
Treated Time
Description
References
THP-1 cells
4 µM
30 minutes
Measure drug uptake in THP-1 cells
PLoS Comput Biol. 2017 Aug 17;13(8):e1005650.
Mouse corneal epithelial cells
0.3%
10 minutes
To evaluate the effect of ultrasound treatment on the permeability of gatifloxacin in mouse corneas. Results showed that ultrasound treatment significantly increased the initial fluorescence intensity of gatifloxacin on the corneal surface (by 67%) and prolonged its residence time in the corneal epithelium.
Sci Rep. 2019 Oct 29;9(1):15532.
Xanthomonas campestris pv. vesicatoria
0.5 mg/L
24 hours
To evaluate the antibacterial activity of gatifloxacin hydrochloride against Xanthomonas campestris pv. vesicatoria, showing substantial growth inhibition at 0.5 mg/L.
Front Microbiol. 2024 Dec 2;15:1504243.
Ralstonia solanacearum
0.0625 mg/L
24 hours
To evaluate the antibacterial activity of gatifloxacin hydrochloride against Ralstonia solanacearum, showing a 95% inhibition rate at 0.0625 mg/L.
Front Microbiol. 2024 Dec 2;15:1504243.
Streptococcus pneumoniae 314
0.4 μg/mL
30 hours
Evaluate the bactericidal effect of gatifloxacin at different AUC/MIC ratios. When AUC/MIC ratios were ≥27, complete eradication of bacteria was observed; when AUC/MIC ratios were ≤17, bacterial counts increased significantly between 8-24 hours.
Evaluate the bactericidal effect of gatifloxacin at different AUC/MIC ratios. When AUC/MIC ratios were ≥28, complete eradication of bacteria was observed; when AUC/MIC ratios were ≤21, bacterial counts increased significantly between 8-24 hours.
To study the effect of gatifloxacin on P-gp mediated [14C] erythromycin uptake, results showed gatifloxacin significantly increased [14C] erythromycin uptake.
Int J Pharm. 2010 Aug 16;395(1-2):114-21.
Human foreskin fibroblasts (HFFs)
0.21 mg/ml
48 hours
To evaluate the inhibitory effect of gatifloxacin on intracellular replication of T. gondii RH strain tachyzoites, showing an IC50 of 0.21 mg/ml at 48 hours.
To investigate the effect of ultrasound treatment on the permeability and residence time of gatifloxacin in Mice corneas. Results showed that ultrasound treatment significantly increased the initial fluorescence intensity of gatifloxacin on the corneal surface (by 67%) and prolonged its residence time in the corneal epithelium.
Sci Rep. 2019 Oct 29;9(1):15532.
New Zealand white rabbits
Healthy New Zealand white rabbits
Topical instillation into the conjunctival sac
0.3%
Every hour or every two hours for 12 hours
To compare the pharmacokinetics and distribution of 0.3% gatifloxacin ophthalmic gel and solution in rabbit ocular tissues. Results showed that GTX-Gel had better penetration than GTX-Sol in the cornea, aqueous humor, vitreous body, lens, and iris-ciliary body.
Antibiotics (Basel). 2022 Apr 10;11(4):502
BALB/c mice
Bacillus anthracis inhalation infection model
Intraperitoneal injection
1.875 to 100 mg·h/liter (AUC0-24)
Every 6 or 8 hours for 21 days
To evaluate the pharmacodynamic parameters of gatifloxacin in a Bacillus anthracis inhalation infection model and determine the relationship between AUC0-24/MIC ratio and survival. The maximum effect (97% survival) corresponded to an AUC0-24/MIC ratio of 30.
Study pharmacokinetics of Gatifloxacin in granulomas
PLoS Comput Biol. 2017 Aug 17;13(8):e1005650.
BALB/c mice
Nocardia brasiliensis infection model
Subcutaneous injection
100 mg/kg
Every 8 hours for 4 weeks
To evaluate the therapeutic effect of gatifloxacin on Nocardia brasiliensis infection, results showed that gatifloxacin was as efficient as linezolid in reducing lesion production.
To evaluate the therapeutic effect of gatifloxacin in combination with ethionamide for tuberculosis. Results showed that high-dose gatifloxacin (300 mg/kg) combined with ethionamide (25 mg/kg) sterilized the lungs, while low-dose (100 mg/kg) left about 10 CFU/lung. Adding pyrazinamide (450 mg/kg) resulted in no viable mycobacteria after the 8-week observation period.
To assess the therapeutic effect of gatifloxacin on acute toxoplasmosis in mice, showing that doses of 100 and 200 mg/kg/day significantly prolonged survival time, and the 400 mg/kg/day dose group had a 20% survival rate.
Measure the distribution and permeability of gatifloxacin in the Mice cornea. Results showed that gatifloxacin had relatively poor penetration and mainly stayed in the superficial epithelium.
Sci Rep. 2016 May 3;6:25339
Rabbits
Methicillin-sensitive Staphylococcus aureus (MSSA)-induced osteomyelitis model
Oral
40 mg/kg
Every 12 hours for 28 days
To compare the effectiveness of oral gatifloxacin with standard parenteral antibiotic (nafcillin) for the treatment of experimental methicillin-sensitive Staphylococcus aureus (MSSA)-induced osteomyelitis. Gatifloxacin was as effective as nafcillin in clearing the infection.
China
... 展开 >> Beijing Children's Hospital of Capital Medical University
Recruiting
Beijing, China
Contact: Adong Shen, Master 13370115087 shenad16@hotmail.com 收起 <<
United States, Kentucky
... 展开 >>
University of Louisville
Recruiting
Louisville, Kentucky, United States, 40202
Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu
Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu
Sub-Investigator: Forest Arnold, DO
Sub-Investigator: Timothy Wiemkwn, PhD
Sub-Investigator: Robert Kelley, PhD
Sub-Investigator: James Summersgill, PhD
Sub-Investigator: Ruth Carrico, PhD
Sub-Investigator: Julie Harting, PharmD
Sub-Investigator: Paula Peyrani, MD
Principal Investigator: David Seligson, MD
Sub-Investigator: Craig Roberts, MD
Principal Investigator: Julio Ramirez, MD 收起 <<
China
... 展开 >> Beijing Children's Hospital of Capital Medical University
Recruiting
Beijing, China
Contact: Adong Shen, Master 13370115087 shenad16@hotmail.com 收起 <<
United States, Kentucky
... 展开 >>
University of Louisville
Recruiting
Louisville, Kentucky, United States, 40202
Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu
Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu
Sub-Investigator: Forest Arnold, DO
Sub-Investigator: Timothy Wiemkwn, PhD
Sub-Investigator: Robert Kelley, PhD
Sub-Investigator: James Summersgill, PhD
Sub-Investigator: Ruth Carrico, PhD
Sub-Investigator: Julie Harting, PharmD
Sub-Investigator: Paula Peyrani, MD
Principal Investigator: David Seligson, MD
Sub-Investigator: Craig Roberts, MD
Principal Investigator: Julio Ramirez, MD 收起 <<
United States, South Carolina
... 展开 >>
Carolina Eyecare Physicians, LLC
Recruiting
Mount Pleasant, South Carolina, United States, 29464
Contact: Helga P Sandoval, MD, MSCR 843-881-3937 helga.sandoval@carolinaeyecare.com
Principal Investigator: Kerry D Solomon, MD
Sub-Investigator: Jefrrey F Hood, OD 收起 <<
Benin
... 展开 >> Programme National de Lutte contre la Tuberculose
Recruiting
Cotonou, Benin
Contact: Martin Gninafon, MD + 229 33 15 33 pnt@intnet.bj
Principal Investigator: Martin Gninafon, MD
Guinea
Service Pneumo-Phtisiologie, CHU Ignace Deen
Recruiting
Conakry, Guinea
Contact: Oumou Y Sow, MD +224 41 20 58 prsow@kassa.sotelgui.net.gn
Principal Investigator: Oumou Sow, MD
Kenya
Kenya Medical Research Institute
Recruiting
Nairobi, Kenya
Contact: Joseph Odhiambo, MD + 254 02 71 30 08 jodhiambo@nairobi.mimcom.net
Principal Investigator: Joseph Odhiambo, MD
Senegal
Programme National de Lutte contre la Tuberculose
Recruiting
Dakar, Senegal
Contact: Cheikh Seck, MD + 221 824.90.09 cheikbaf@yahoo.fr
Principal Investigator: Cheikh Seck, MD
South Africa
Medical Research Council
Recruiting
Durban, KwaZulu, South Africa
Contact: Roxana Rustomjee, MD +27 31 207 16 75 Roxana.rustomjee@mrc.ac.za
Principal Investigator: Roxana Rustomjee, MD 收起 <<
United States, California
... 展开 >>
San Francisco General Hospital - Pulmonary and Critical Care Medicine
San Francisco, California, United States, 94110-3518
Brazil
Universidade Federal do Espirito Santo - Duke Hubert-Yeargan Center
Vitória, Espírito Santo, Brazil, 29040-091 收起 <<
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