Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C19H15F3N4O3.H2O |
| Molecular Weight | 422.3579 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.NC1CCN(C1)C2=NC3=C(C=C2F)C(=O)C(=CN3C4=CC=C(F)C=C4F)C(O)=O
InChI
InChIKey=FCHGAGZTPICOSW-UHFFFAOYSA-N
InChI=1S/C19H15F3N4O3.H2O/c20-9-1-2-15(13(21)5-9)26-8-12(19(28)29)16(27)11-6-14(22)18(24-17(11)26)25-4-3-10(23)7-25;/h1-2,5-6,8,10H,3-4,7,23H2,(H,28,29);1H2
| Molecular Formula | C19H15F3N4O3 |
| Molecular Weight | 404.3426 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including:
http://medical.taishotoyama.co.jp/data/if/pdf/ozx.pdf
Curator's Comment: description was created based on several sources, including:
http://medical.taishotoyama.co.jp/data/if/pdf/ozx.pdf
Tosufloxacin is a fluoroquinolone antibacterial agent. Tosufloxacin is an inhibitor of bacterial DNA gyrase and topoisomerase IV. Tosufloxacin is indicated for the treatment of various infections such as skin, respiratory, urinary, gynecologic, ophthalmologic, otolaryngologic, dental infections. Fluoroquinolones including tosufloxacin have a potential risk of inducing cartilage and joint toxicity in children. It is also associated with severe thrombocytopenia and nephritis, and hepatotoxicity.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2311224 |
|||
Target ID: CHEMBL2363076 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Curative | Ozex Approved UseIt is usually used to treat various infections such as skin/respiratory/urinary/gynecologic/ophthalmologic/otolaryngologic/dental infections. Launch Date6.3296641E11 |
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| Curative | Ozex Approved UseIt is usually used to treat various infections such as skin/respiratory/urinary/gynecologic/ophthalmologic/otolaryngologic/dental infections. Launch Date6.3296641E11 |
|||
| Curative | Ozex Approved UseIt is usually used to treat various infections such as skin/respiratory/urinary/gynecologic/ophthalmologic/otolaryngologic/dental infections. Launch Date6.645024E11 |
|||
| Curative | Ozex Approved UseIt is usually used to treat various infections such as skin/respiratory/urinary/gynecologic/ophthalmologic/otolaryngologic/dental infections. Launch Date6.3296641E11 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Fluoronaphthyridines as antibacterial agents. 4. Synthesis and structure-activity relationships of 5-substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8- naphthyridine-3-carboxylic acids. | 1992 Feb 7 |
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| Comparative in-vitro activities of the new quinolone, Bay y 3118, and ciprofloxacin, sparfloxacin, tosufloxacin, CI-960 and CI-990. | 1993 Apr |
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| In-vitro activity of quinolones and macrolides against mycobacteria. | 1994 Sep |
|
| Trovafloxacin is active against Toxoplasma gondii. | 1996 Aug |
|
| Therapeutic effect of the quinolone prodrug prulifloxacin against experimental urinary tract infections in mice. | 1996 Dec |
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| N-1-tert-butyl-substituted quinolones: in vitro anti-Mycobacterium avium activities and structure-activity relationship studies. | 1996 Nov |
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| Structure-activity relationships of quinolone agents against mycobacteria: effect of structural modifications at the 8 position. | 1996 Oct |
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| [In vitro anti-MAC activities of new quinolones in focus (2)]. | 1996 Sep |
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| [Molecular epidemiology of fluoroquinolone-resistant Streptococcus pneumoniae in Japan]. | 2004 May |
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| An unusual form of crystal-forming chronic interstitial nephritis following long-term exposure to tosufloxacin tosilate. | 2004 Nov |
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| Terbium sensitized determination of tosufloxacin using electrochemiluminescence method. | 2005 Apr |
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| In vitro activity of pazufloxacin, tosufloxacin and other quinolones against Legionella species. | 2005 Dec |
|
| VapB-positive Rhodococcus equi infection in an HIV-infected patient in Japan. | 2005 Feb |
|
| [Clinical study of male urethritis in Oogaki Municipal Hospital]. | 2005 Jan |
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| [Study on the accumulation of fluoroquinolones in clinical isolates of susceptible and multi-drug-resistant Escherichia coli strains]. | 2005 Jan |
|
| Antimicrobial safety: focus on fluoroquinolones. | 2005 Jul 15 |
|
| [Clinical experience of streptococcal balanoposthitis in 47 healthy adult males]. | 2005 Nov |
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| Antimicrobial activities of tosufloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella branhamella catarrhalis isolated from otolaryngological infectious diseases. | 2005 Oct |
|
| [Successful treatment with voriconazole for disseminated cutaneous and visceral infection by Fusarium solani in a patient with acute myeloid leukemia]. | 2006 Aug |
|
| [Evaluation of efficacy of oral quinolone against Streptococcus pneumoniae AND Haemophilus influenzae with the use of Monte Carlo simulation]. | 2006 Dec |
|
| In vitro activity of sitafloxacin compared with several fluoroquinolones against Streptococcus anginosus and Streptococcus constellatus. | 2006 Feb |
|
| [Sensitivity surveillance of Streptococcus pneumoniae isolates for several antibiotics in Gifu prefecture (2004)]. | 2006 Jun |
|
| Antibacterial activity of tosufloxacin against major organisms detected from patients with respiratory or otorhinological infections: comparison with the results obtained from organisms isolated about 10 years ago. | 2006 Jun |
|
| [Antibacterial activity of tosufloxacin against major organisms detected from patients with respiratory infections]. | 2007 Apr |
|
| [Effectiveness of switch therapy for peritonitis]. | 2007 Aug |
|
| A novel in vivo rabbit model that mimics human dosing to determine the distribution of antibiotics in ocular tissues. | 2007 Aug |
|
| Multidrug-resistant typhoid fever outbreak in travelers returning from Bangladesh. | 2007 Dec |
|
| [Susceptibility of clinical isolates from primary care clinics to oral antibacterial agents]. | 2007 Feb |
|
| Tosufloxacin tosilate-induced thrombocytopenic purpura. | 2007 Jul |
|
| [A case of acute bronchitis caused by Neisseria meningitidis associated with HIV infection]. | 2007 Nov |
|
| Effect of GrlA mutation on the development of quinolone resistance in Staphylococcus aureus in an in vitro pharmacokinetic model. | 2007 Nov |
|
| [Sensitivity surveillance of Haemophilus influenzae isolates for several antibiotics in Gifu Prefecture (2006)]. | 2008 Aug |
|
| Antibiotic prophylaxis for transrectal prostate biopsy: a prospective randomized study of tosufloxacin versus levofloxacin. | 2008 Jul |
|
| Mutations in the quinolone resistance determining region in Staphylococcus epidermidis recovered from conjunctiva and their association with susceptibility to various fluoroquinolones. | 2008 Jun |
|
| In vitro susceptibilities of bacterial isolates from conjunctival flora to gatifloxacin, levofloxacin, tosufloxacin, and moxifloxacin. | 2008 Mar |
|
| Quantitative comparison of the convulsive activity of combinations of twelve fluoroquinolones with five nonsteroidal antiinflammatory agents. | 2009 |
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| Fluoroquinolones reduce carrageenan-induced edema in rats and the involvement of the glucocorticoid receptor system. | 2009 Apr |
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| Measurement of AQCmax of five different ophthalmic solutions and discussion of its new application. | 2009 Aug |
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| Prediction of pharmacological and xenobiotic responses to drugs based on time course gene expression profiles. | 2009 Dec 2 |
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| Functional characterization of multidrug and toxin extrusion protein 1 as a facilitative transporter for fluoroquinolones. | 2009 Feb |
|
| Corneal deposits after topical tosufloxacin in a patient with poor tear secretion. | 2009 Jan |
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| [Antibacterial activity of quinolones against various clinically isolated strains and evaluation of efficacy based on the pharmacokinetics/pharmacodynamics theory]. | 2009 Jun |
|
| Levofloxacin 0.5% ophthalmic solution: a review of its use in the treatment of external ocular infections and in intraocular surgery. | 2009 Jun 18 |
|
| [Efficacy of tosufloxacin in genital chlamydial infections]. | 2009 Oct |
|
| Antituberculosis activity of the molecular libraries screening center network library. | 2009 Sep |
|
| [Intractable pediatric infectious disease: examining the ability of a new drug, tosufloxacin tosilate hydrate for pediatric]. | 2010 Dec |
|
| [Antibiotic susceptibility of blood-borne Streptococcus pneumoniae and efficacy assessment of respiratory quinolones using Monte Carlo simulation]. | 2010 Feb |
|
| [Epidemiological analysis of Streptococcus pneumoniae in Gifu prefecture]. | 2010 Jun |
|
| Risk factors for acute prostatitis after transrectal biopsy of the prostate. | 2010 Jun |
|
| Legionella pneumophila induces cathepsin B-dependent necrotic cell death with releasing high mobility group box1 in macrophages. | 2010 Nov 22 |
Patents
Sample Use Guides
In general, for adults, take 2 to 3 tablets (300 to 450 mg of the active ingredient) a day, in 2 to 3 divided doses. The dosage may be adjusted according to disease, symptoms, etc. of the patient. If symptoms are severe or the effect is insufficient, take 4 tablets (600 mg) a day.
Osteomyelitis, arthritis: In general, for adults, take 1 tablet (150 mg of the active ingredient) at a time, 3 times a day. The dosage may be adjusted according to disease, symptoms, etc. of the patient. If symptoms are severe or the effect is insufficient, take 4 tablets (600 mg) a day.
Typhoid/paratyphoid fever: In general, for adults, take 1 tablet (150 mg of the active ingredient) at a time, 4 times a day for 14 days.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:02:43 UTC 2023
by
admin
on
Fri Dec 15 16:02:43 UTC 2023
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| Record UNII |
6239812J7L
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| Record Status |
Validated (UNII)
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| Record Version |
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-
Download
| Name | Type | Language | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C795
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6239812J7L
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DTXSID80910234
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44154493
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C76233
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107097-79-0
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ANHYDROUS->SOLVATE | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |