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Chemical Structure| 112811-59-3 Chemical Structure| 112811-59-3

Structure of Gatifloxacin
CAS No.: 112811-59-3

Chemical Structure| 112811-59-3

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CAS No.: 112811-59-3

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Gatifloxacin inhibits DNA gyrase and topoisomerase IV in bacterial. It is an antibiotic of the fourth-generation fluoroquinolone family.

Synonyms: BMS-206584; AM-1155; BMS 206584-01

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Product Details of Gatifloxacin

CAS No. :112811-59-3
Formula : C19H22FN3O4
M.W : 375.39
SMILES Code : O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CC(C)NCC4)=C3OC)C1=O)O
Synonyms :
BMS-206584; AM-1155; BMS 206584-01
MDL No. :MFCD00895399

Safety of Gatifloxacin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Gatifloxacin

DNA

Isoform Comparison

Biological Activity

Target

  • Topoisomerase

In Vitro:

Cell Line
Concentration Treated Time Description References
THP-1 cells 4 μM 30 minutes Measure drug uptake in THP-1 cells PMC5560534
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. PMC6820539
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. PMC11648225
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. PMC11648225
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. PMC126977
Streptococcus pneumoniae 257 0.6 μg/mL 30 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. PMC126977
MDCKII-MDR1 cells 2.5 mM 30 minutes To study the effect of gatifloxacin on P-gp mediated [14C] erythromycin uptake, results showed gatifloxacin significantly increased [14C] erythromycin uptake. PMC2902587
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. PMC90238
Bacillus anthracis (Ames strain) 0.125 mg/L To determine the in vitro minimum inhibitory concentration (MIC) of gatifloxacin against Bacillus anthracis. PMC2167989

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Swiss Webster mice Acute toxoplasmosis model Oral 100, 200, 400 mg/kg Once daily for 10 days 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. PMC90238
C57BL/6J mice Tuberculosis model Gavage 100 or 300 mg/kg 5 days per week for 12 weeks 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. PMC166105
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. PMC9027311
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. PMC127012
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. PMC2167989
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. PMC2292517
BALB/c mice Mice cornea model Topical instillation 0.3% Single instillation, incubated for 10 minutes 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. PMC6820539
BALB/c mice Mice cornea model Topical administration 10μL Single dose, observed for 2 hours 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. PMC4853790
New Zealand White rabbits Tuberculosis granuloma model Oral 100 mg/kg Single dose Study pharmacokinetics of Gatifloxacin in granulomas PMC5560534

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03625739 - Recruiting December 31, 2026 China ... More >> Beijing Children's Hospital of Capital Medical University Recruiting Beijing, China Contact: Adong Shen, Master ?? 13370115087 ?? shenad16@hotmail.com Less <<
NCT00831961 - Completed - United States, Tennessee ... More >> Vanderbilt Eye Institute Nashville, Tennessee, United States, 37232 Less <<
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... More >> 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 Less <<
NCT00407017 Cataract Surgery Phase 4 Completed - United States, Florida ... More >> The Center for Excellence in Eye Care Miami, Florida, United States, 33176 Less <<
NCT00621933 - Completed - United States, Utah ... More >> Salt Lake City, Utah, United States Less <<
NCT00621933 - Completed - -
NCT00620997 Corneal Abrasions Phase 1 Completed - Canada, Ontario ... More >> London Health Sciences Center London, Ontario, Canada, N6A 5W9 Less <<
NCT03479736 - Completed - United States, New Jersey ... More >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 Less <<
NCT02943967 Surgical Procedure, Unspecifie... More >>d Less << Not Applicable Completed - Brazil ... More >> Federal University of S?o Paulo Sao Paulo, Brazil, 04023-062 Less <<
NCT02196740 Periapical Diseases Not Applicable Unknown June 2015 China, Guangdong ... More >> Jicheng Lin Guangzhou, Guangdong, China, 510055 Less <<
NCT02717871 Keratitis; Infectious Disease ... More >>(Manifestation) Less << Phase 3 Recruiting August 2018 Switzerland ... More >> University of Geneva Recruiting Geneva, GE, Switzerland, 1211 Contact: Farhad Hafezi, MD, PhD ?? ?? fhafezi@elza-institute.com ?? Principal Investigator: Farhad Hafezi, MDPhD Less <<
NCT03237182 Tuberculosis, Multidrug-Resist... More >>ant Less << Phase 4 Recruiting December 2021 South Africa ... More >> King Dinuzulu Hospital Recruiting Durban, Kwa-Zulu Natal, South Africa Contact: Nesri Padayatchi, MBcHB ?? 0312604550 ?? nesri.padayatchi@caprisa.org ?? Contact: Resha Boodhram, BTech ?? 0828383651 ?? resha.boodhram@caprisa.org Less <<
NCT00433225 Macula Thickening Phase 4 Completed - United States, New York ... More >> Ophthalmic Consultants of Long Island Rockville Centre, New York, United States, 11570 Less <<
NCT00478764 Cataract Not Applicable Completed - United States, Wisconsin ... More >> Davis Duehr Dean Baraboo Baraboo, Wisconsin, United States, 53913 Less <<
NCT01881438 - Completed - -
NCT03578276 Cataract Phase 4 Recruiting June 15, 2019 United States, South Carolina ... More >> 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 Less <<
NCT00410891 - Completed - -
NCT00382460 Actue Coronary Syndromes Phase 4 Completed - -
NCT00703313 Healthy Phase 4 Completed - United States, Florida ... More >> Vistakon Jacksonville, Florida, United States, 32256 Less <<
NCT00874887 Anti-biotic Resistance Phase 4 Completed - United States, Minnesota ... More >> Minneapolis, Minnesota, United States Canada, Saskatchewan Saskatoon, Saskatchewan, Canada Less <<
NCT01928693 - Terminated(study terminated du... More >>e to slow accrual) Less << - -
NCT00874887 - Completed - -
NCT00216385 Tuberculosis Phase 3 Unknown - Benin ... More >> 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 Less <<
NCT00347828 Eye Infection ... More >> Infection Less << Phase 4 Unknown - United States, Massachusetts ... More >> Ophthalmic Consultants of Boston Boston, Massachusetts, United States, 02114 Less <<
NCT00464438 Bacterial Conjunctivitis Phase 4 Completed - United States, California ... More >> Sacramento, California, United States Canada, Ontario Whitby, Ontario, Canada Less <<
NCT01928693 Corneal Ulcers Phase 2 Terminated(study terminated du... More >>e to slow accrual) Less << - United States, Tennessee ... More >> Cornea Consultants of Nashville Nashville, Tennessee, United States, 37203 Less <<
NCT00464438 - Completed - -
NCT00651586 Acute Bacterial Corneal Ulcers... More >> Bacterial Keratitis Less << Phase 2 Completed - United States, Texas ... More >> Galveston, Texas, United States India Madurai, Tamilnadu, India Less <<
NCT00414011 Epithelium, Corneal Not Applicable Completed - United States, District of Col... More >>umbia Walter Reed Army Medical Center Washington, District of Columbia, United States, 20307 Less <<
NCT00410891 Intravitreous ... More >> Injections Less << Phase 4 Completed - United States, California ... More >> Stanford Stanford, California, United States, 94304 Less <<
NCT00396084 - Completed - -
NCT00414011 - Completed - -
NCT00396084 Tuberculosis Phase 1 Phase 2 Completed - United States, California ... More >> 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 Less <<
NCT00509873 Bacterial Conjunctivitis Phase 3 Completed - United States, Louisiana ... More >> Gretna, Louisiana, United States Less <<
NCT00518089 Bacterial Conjunctivitis Phase 3 Completed - United States, California ... More >> Downey, California, United States India Rajajinagar, Bangalore, India Less <<
NCT00518089 - Completed - -
NCT00466570 Conjunctical Flora Not Applicable Withdrawn - -
NCT00569881 - Completed - -
NCT00824070 Cataract Extraction Phase 1 Completed - United States, New York ... More >> Ophthalmic Consultants of Long Island Rockville Center, New York, United States, 11570 Less <<
NCT00892918 Primary Pterygium Not Applicable Unknown June 2010 Israel ... More >> Meir Medical Center Not yet recruiting Kfar Saba, Israel, 44281 Contact: Fani Segev, MD ?? 972-52-6995044 ?? fsegev@netvision.net.il Less <<
NCT00509873 - Completed - -
NCT00824070 - Completed - -
NCT02980523 Bacterial Conjunctivitis Phase 2 Completed - -
NCT00905762 Healthy Phase 1 Completed - United States, New York ... More >> Bausch & Lomb Incorporated Rochester, New York, United States, 14609 Less <<
NCT01421693 Enteric Fever ... More >> Typhoid Fever Less << Phase 4 Completed - Nepal ... More >> Civil Hospital Kathmandu, Nepal Patan Hospital Kathmandu, Nepal Less <<
NCT01330355 - Terminated(Lack of enrollment) - -
NCT00335231 Endophthalmitis Not Applicable Withdrawn(Protocol changes und... More >>erway. Trial never started) Less << - Canada, Ontario ... More >> Hotel Dieu Hospital Kingston, Ontario, Canada, K7L 5G2 Less <<
NCT01330355 Bacterial Conjunctivitis Phase 3 Terminated(Lack of enrollment) - United States, New Jersey ... More >> Bausch & Lomb Incorporated Bridgewater, New Jersey, United States, 08807 Less <<
NCT03696342 Conjunctivitis, Bacterial Phase 3 Active, not recruiting April 2020 Mexico ... More >> MD office. Juan Carlos Ochoa Tavares Guadalajara, Jalisco, Mexico, 44600 Less <<
NCT01218737 Ocular Infection and Inflammat... More >>ion Less << Phase 3 Completed - Brazil ... More >> Federal University of Sao Paulo - Dept of Ophthalmology Sao Paulo, SP, Brazil, 04023-062 Less <<
NCT00350363 Ophthalmic Surgery Phase 4 Completed - United States, California ... More >> Stanford Stanford, California, United States, 94304 Less <<
NCT00350363 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.64mL

5.33mL

2.66mL

References

 

Historical Records

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