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Chemical Compound Review

AC1NUZ81     7-[(4Z)-3-(aminomethyl)-4- methoxyimino...

Synonyms: KB-212128, FT-0631197, DB01155, I14-2707, 175463-14-6, ...
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Disease relevance of Gemifloxacin


High impact information on Gemifloxacin


Chemical compound and disease context of Gemifloxacin


Biological context of Gemifloxacin


Anatomical context of Gemifloxacin


Associations of Gemifloxacin with other chemical compounds


Gene context of Gemifloxacin

  • Staphylococcus aureus (MSSA) were highly susceptible (MIC(90) 0.06 mg/L) but MRSA less susceptible (MIC(90) 8 mg/L) to gemifloxacin [25].
  • Whereas LPS induced a rapid increase in NF-kappa B activation, gemifloxacin alone did not [26].
  • In addition, RNA from THP-1 cells was used in Northern blots to determine whether inhibition of secretion of IL-1 beta and TNF-alpha by gemifloxacin occurred at the transcription or translation level [26].
  • (i) The gemifloxacin MICs for isogenic 7785 mutants bearing either parC or gyrA quinolone resistance mutations were marginally higher than wild type at 0.12 to 0.25 microgram/ml, whereas the presence of both mutations increased the MIC to 0.5 to 1 microgram/ml [27].
  • The two- to fourfold increase in the MIC of gemifloxacin in genetically defined grlBA mutants and the twofold increase in a single gyrA mutant, supported by the low frequency of selection of resistant mutants at twice the MIC (7.4 x 10(-11) to 1.1 x 10(-10)), suggested similar targeting of the two enzymes by gemifloxacin [5].

Analytical, diagnostic and therapeutic context of Gemifloxacin

  • In a randomized crossover study, 16 volunteers (8 men, 8 women) received single oral doses of 320 mg of gemifloxacin and 400 mg of ofloxacin on two separate occasions in the fasting state to assess the urinary excretion and urinary bactericidal titers (UBTs) at intervals for up to 144 h [28].
  • Although clinical trials have shown that gemifloxacin is effective for the treatment of uncomplicated urinary tract infections, whether an oral dosage of 320 mg of gemifloxacin once daily is also adequate for the treatment of complicated urinary tract infections has yet to be confirmed [28].
  • Multiple serum or plasma and urine samples were collected on days 1 and 7 and were analyzed for gemifloxacin by high-performance liquid chromatography (HPLC)-fluorescence (study 1) or HPLC-mass spectrometry (study 2) [14].
  • The successful chiral separation of gemifloxacin in a urinary solution was demonstrated for both capillary and microchip electrophoresis [29].
  • Dose fractionation was used to simulate concentrations of gemifloxacin in human serum associated with 640 mg every 48 h (one dose), 320 mg every 24 h (two doses), and 160 mg every 12 h (four doses) [16].


  1. Novel symmetric and asymmetric DNA scission determinants for Streptococcus pneumoniae topoisomerase IV and gyrase are clustered at the DNA breakage site. Leo, E., Gould, K.A., Pan, X.S., Capranico, G., Sanderson, M.R., Palumbo, M., Fisher, L.M. J. Biol. Chem. (2005) [Pubmed]
  2. Appropriate outpatient treatment of acute bacterial exacerbations of chronic bronchitis. Martinez, F.J., Anzueto, A. Am. J. Med. (2005) [Pubmed]
  3. A critical review of the fluoroquinolones: focus on respiratory infections. Zhanel, G.G., Ennis, K., Vercaigne, L., Walkty, A., Gin, A.S., Embil, J., Smith, H., Hoban, D.J. Drugs (2002) [Pubmed]
  4. Activities and postantibiotic effects of gemifloxacin compared to those of 11 other agents against Haemophilus influenzae and Moraxella catarrhalis. Davies, T.A., Kelly, L.M., Hoellman, D.B., Ednie, L.M., Clark, C.L., Bajaksouzian, S., Jacobs, M.R., Appelbaum, P.C. Antimicrob. Agents Chemother. (2000) [Pubmed]
  5. Topoisomerase targeting with and resistance to gemifloxacin in Staphylococcus aureus. Ince, D., Zhang, X., Silver, L.C., Hooper, D.C. Antimicrob. Agents Chemother. (2003) [Pubmed]
  6. New approaches in the treatment of bacterial infections. Bush, K., Macielag, M. Current opinion in chemical biology. (2000) [Pubmed]
  7. Fluoroquinolone Resistance in Streptococcus pneumoniae: Area Under the Concentration-Time Curve/MIC Ratio and Resistance Development with Gatifloxacin, Gemifloxacin, Levofloxacin, and Moxifloxacin. Laplante, K.L., Rybak, M.J., Tsuji, B., Lodise, T.P., Kaatz, G.W. Antimicrob. Agents Chemother. (2007) [Pubmed]
  8. Activity of gemifloxacin against quinolone-resistant Streptococcus pneumoniae strains in vitro and in a mouse pneumonia model. Azoulay-Dupuis, E., Bédos, J.P., Mohler, J., Moine, P., Cherbuliez, C., Peytavin, G., Fantin, B., Köhler, T. Antimicrob. Agents Chemother. (2005) [Pubmed]
  9. In vitro and in vivo antibacterial activities of DW286, a new fluoronaphthyridone antibiotic. Yun, H.J., Min, Y.H., Lim, J.A., Kang, J.W., Kim, S.Y., Kim, M.J., Jeong, J.H., Choi, Y.J., Kwon, H.J., Jung, Y.H., Shim, M.J., Choi, E.C. Antimicrob. Agents Chemother. (2002) [Pubmed]
  10. Antibacterial properties of gemifloxacin and trovafloxacin in urine ex vivo: phase I study. García-Calvo, G., Parra, A., Aguilar, L., Ponte, C., Giménez, M.J., Carcas, A., Kinzig-Schippers, M., Soriano, F. Antimicrob. Agents Chemother. (2001) [Pubmed]
  11. In vitro activity of gemifloxacin (SB 265805) against anaerobes. Goldstein, E.J., Citron, D.M., Warren, Y., Tyrrell, K., Merriam, C.V. Antimicrob. Agents Chemother. (1999) [Pubmed]
  12. In vitro activity of gemifloxacin (SB 265805; LB20304a) against human mycoplasmas. Hannan, P.C., Woodnutt, G. J. Antimicrob. Chemother. (2000) [Pubmed]
  13. Comparative in vitro activity and post-antibiotic effect of gemifloxacin against Legionella spp. Dubois, J., St-Pierre, C. J. Antimicrob. Chemother. (2000) [Pubmed]
  14. Multiple-dose pharmacokinetics and tolerability of gemifloxacin administered orally to healthy volunteers. Allen, A., Bygate, E., Vousden, M., Oliver, S., Johnson, M., Ward, C., Cheon, A., Choo, Y.S., Kim, I. Antimicrob. Agents Chemother. (2001) [Pubmed]
  15. Effect of calcium carbonate on bioavailability of orally administered gemifloxacin. Pletz, M.W., Petzold, P., Allen, A., Burkhardt, O., Lode, H. Antimicrob. Agents Chemother. (2003) [Pubmed]
  16. Pharmacodynamics of gemifloxacin against Streptococcus pneumoniae in an in vitro pharmacokinetic model of infection. MacGowan, A.P., Rogers, C.A., Holt, H.A., Wootton, M., Bowker, K.E. Antimicrob. Agents Chemother. (2001) [Pubmed]
  17. Activity of gemifloxacin against penicillin- and ciprofloxacin-resistant Streptococcus pneumoniae displaying topoisomerase- and efflux-mediated resistance mechanisms. Heaton, V.J., Goldsmith, C.E., Ambler, J.E., Fisher, L.M. Antimicrob. Agents Chemother. (1999) [Pubmed]
  18. Intracellular penetration and activity of gemifloxacin in human polymorphonuclear leukocytes. García, I., Pascual, A., Ballesta, S., Joyanes, P., Perea, E.J. Antimicrob. Agents Chemother. (2000) [Pubmed]
  19. Concentrations of gemifloxacin at the target site in healthy volunteers after a single oral dose. Islinger, F., Bouw, R., Stahl, M., Lackner, E., Zeleny, P., Brunner, M., Müller, M., Eichler, H.G., Joukhadar, C. Antimicrob. Agents Chemother. (2004) [Pubmed]
  20. In vitro activity of gemifloxacin (SB-265805, LB20304a) against Legionella pneumophila and its pharmacokinetics in guinea pigs with L. pneumophila pneumonia. Edelstein, P.H., Shinzato, T., Doyle, E., Edelstein, M.A. Antimicrob. Agents Chemother. (2001) [Pubmed]
  21. Antipneumococcal activity of DW-224a, a new quinolone, compared to those of eight other agents. Kosowska-Shick, K., Credito, K., Pankuch, G.A., Lin, G., Bozdogan, B., McGhee, P., Dewasse, B., Choi, D.R., Ryu, J.M., Appelbaum, P.C. Antimicrob. Agents Chemother. (2006) [Pubmed]
  22. Cleavable-complex formation by wild-type and quinolone-resistant Streptococcus pneumoniae type II topoisomerases mediated by gemifloxacin and other fluoroquinolones. Yague, G., Morris, J.E., Pan, X.S., Gould, K.A., Fisher, L.M. Antimicrob. Agents Chemother. (2002) [Pubmed]
  23. In vitro activities of the newer quinolones garenoxacin, gatifloxacin, and gemifloxacin against human mycoplasmas. Pereyre, S., Renaudin, H., Bébéar, C., Bébéar, C.M. Antimicrob. Agents Chemother. (2004) [Pubmed]
  24. Comparative in vitro activity of PGE 9262932 and fluoroquinolones against Canadian clinical Streptococcus pneumoniae isolates, including molecularly characterized ciprofloxacin-resistant isolates. Adam, H.J., Schurek, K.N., Decorby, M.R., Weshnoweski, B., Vashisht, R., Karlowsky, K., Hoban, D.J., Zhanel, G.G. J. Antimicrob. Chemother. (2006) [Pubmed]
  25. The in-vitro activity and tentative breakpoint of gemifloxacin, a new fluoroquinolone. Wise, R., Andrews, J.M. J. Antimicrob. Chemother. (1999) [Pubmed]
  26. Gemifloxacin inhibits cytokine secretion by lipopolysaccharide stimulated human monocytes at the post-transcriptional level. Araujo, F., Slifer, T., Li, S., Kuver, A., Fong, L., Remington, J. Clin. Microbiol. Infect. (2004) [Pubmed]
  27. Potent antipneumococcal activity of gemifloxacin is associated with dual targeting of gyrase and topoisomerase IV, an in vivo target preference for gyrase, and enhanced stabilization of cleavable complexes in vitro. Heaton, V.J., Ambler, J.E., Fisher, L.M. Antimicrob. Agents Chemother. (2000) [Pubmed]
  28. Urinary excretion and bactericidal activities of gemifloxacin and ofloxacin after a single oral dose in healthy volunteers. Naber, C.K., Hammer, M., Kinzig-Schippers, M., Sauber, C., Sörgel, F., Bygate, E.A., Fairless, A.J., Machka, K., Naber, K.G. Antimicrob. Agents Chemother. (2001) [Pubmed]
  29. Chiral separation of gemifloxacin in sodium-containing media using chiral crown ether as a chiral selector by capillary and microchip electrophoresis. Cho, S.I., Lee, K.N., Kim, Y.K., Jang, J., Chung, D.S. Electrophoresis (2002) [Pubmed]
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