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Chemical Compound Review

Garenoxacin     1-cyclopropyl-8- (difluoromethoxy)-7-[(1R)...

Synonyms: Ganefloxacin, PubChem22423, CHEMBL215303, AG-E-42403, SureCN2103727, ...
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Disease relevance of T-3811MEa


Psychiatry related information on T-3811MEa


High impact information on T-3811MEa


Chemical compound and disease context of T-3811MEa


Biological context of T-3811MEa

  • Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects [2].
  • Increases in systemic exposure to garenoxacin in terms of AUC and C(max) were approximately dose proportional over the 100- to 400-mg dose range but demonstrated increases that were somewhat greater than the dose increments at the 800- and 1200-mg doses [2].
  • In particular, after dosing of 20 mg/kg (as T-3811), the viable cell counts in CSF were significantly less than those in the nontreated group (P < 0.01) [15].
  • A secondary objective was to determine the time after dose administration that garenoxacin was no longer detected in breast milk so as to define when a mother may resume breastfeeding if it was interrupted for garenoxacin administration [16].
  • CONCLUSIONS: The relative bioavailability of garenoxacin was not affected by administration as crushed tablets, regardless of enteral feeding [17].

Anatomical context of T-3811MEa


Associations of T-3811MEa with other chemical compounds

  • These in vitro observations suggest that garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus [21].
  • After the administration of any dose of T-3811ME (5, 10, and 20 mg/kg as T-3811), the viable cell counts in CSF decreased in a dose-dependent manner [15].
  • The detection was carried out using a diode array detector at 254nm and in a fluorescence detector at wavelengths of excitation and emission of 292nm and 392nm for linezolid and sulfamethoxazole, and 292nm and 408nm for garenoxacin, respectively [14].
  • Multivariate calibration methods (partial least squares calibration, back propagation multilayer perceptrons networks, radial basis functions and generalized regression neural networks) were applied to the simultaneous fluorometric quantification of levofloxacin, garenoxacin and grepafloxacin, without previous separation steps [22].

Gene context of T-3811MEa

  • RESULTS: MIC90 values of garenoxacin for the MSSA and MRSA strains were 0.03 and 2 mg/L, respectively [23].
  • We conclude that garenoxacin has excellent activity against H. influenzae, although progressive acquired resistance was observed by step-by-step mutation in the QRDR of gyrA and parC [24].
  • Additional studies indicate that (R)-5b (T-3811, CAS 194804-75-6) exhibits excellent antibacterial activity against a wide range of organisms including anaerobes and common respiratory pathogens, while demonstrating a high selectivity against the mammalian homolog topoisomerases [25].

Analytical, diagnostic and therapeutic context of T-3811MEa


  1. Fluoroquinolone-resistant Streptococcus pneumoniae in Spain: activities of garenoxacin against clinical isolates including strains with altered topoisomerases. Morosini, M.I., Loza, E., del Campo, R., Almaraz, F., Baquero, F., Cantón, R. Antimicrob. Agents Chemother. (2003) [Pubmed]
  2. Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects. Gajjar, D.A., Bello, A., Ge, Z., Christopher, L., Grasela, D.M. Antimicrob. Agents Chemother. (2003) [Pubmed]
  3. Garenoxacin treatment of experimental endocarditis caused by viridans group streptococci. Anguita-Alonso, P., Rouse, M.S., Piper, K.E., Steckelberg, J.M., Patel, R. Antimicrob. Agents Chemother. (2006) [Pubmed]
  4. Quinolone-resistant Haemophilus influenzae: determination of mutant selection window for ciprofloxacin, garenoxacin, levofloxacin, and moxifloxacin. Li, X., Mariano, N., Rahal, J.J., Urban, C.M., Drlica, K. Antimicrob. Agents Chemother. (2004) [Pubmed]
  5. Efficacy of garenoxacin in treatment of experimental endocarditis due to Staphylococcus aureus or viridans group streptococci. Entenza, J.M., Vouillamoz, J., Glauser, M.P., Moreillon, P. Antimicrob. Agents Chemother. (2004) [Pubmed]
  6. Pharmacological evaluation of garenoxacin, a novel des-F(6)-quinolone antimicrobial agent: effects on the central nervous system. Nakamura, T., Fukuda, H., Morita, Y., Soumi, K., Kawamura, Y. The Journal of toxicological sciences. (2003) [Pubmed]
  7. Cellular accumulation and activity of quinolones in ciprofloxacin-resistant j774 macrophages. Michot, J.M., Heremans, M.F., Caceres, N.E., Mingeot-Leclercq, M.P., Tulkens, P.M., Van Bambeke, F. Antimicrob. Agents Chemother. (2006) [Pubmed]
  8. DX-619, a novel des-fluoro(6) quinolone manifesting low frequency of selection of resistant Staphylococcus aureus mutants: quinolone resistance beyond modification of type II topoisomerases. Strahilevitz, J., Truong-Bolduc, Q.C., Hooper, D.C. Antimicrob. Agents Chemother. (2005) [Pubmed]
  9. Antimicrobial activities of garenoxacin (BMS 284756) against Asia-Pacific region clinical isolates from the SENTRY program, 1999 to 2001. Christiansen, K.J., Bell, J.M., Turnidge, J.D., Jones, R.N. Antimicrob. Agents Chemother. (2004) [Pubmed]
  10. In vitro activities of new antimicrobials against Nocardia brasiliensis. Vera-Cabrera, L., Gonzalez, E., Choi, S.H., Welsh, O. Antimicrob. Agents Chemother. (2004) [Pubmed]
  11. Activities of garenoxacin (BMS-284756) and other agents against anaerobic clinical isolates. Hecht, D.W., Osmolski, J.R. Antimicrob. Agents Chemother. (2003) [Pubmed]
  12. Re-evaluation of quality control guidelines for gatifloxacin and garenoxacin (BMS284756) when susceptibility testing Haemophilus influenzae and Streptococcus pneumoniae. Anderegg, T.R., Biedenbach, D.J., Jones, R.N. Diagn. Microbiol. Infect. Dis. (2003) [Pubmed]
  13. In vitro antibacterial activity and pharmacodynamics of new quinolones. Dalhoff, A., Schmitz, F.J. Eur. J. Clin. Microbiol. Infect. Dis. (2003) [Pubmed]
  14. Simultaneous determination and validation of antimicrobials in plasma and tissue of actinomycetoma by high-performance liquid chromatography with diode array and fluorescence detection. Cavazos-Rocha, N., Vera-Cabrera, L., Welsh-Lozano, O., Waksman-de-Torres, N., de la Luz Salazar-Cavazos, M. Journal of pharmaceutical and biomedical analysis (2007) [Pubmed]
  15. Evaluation of T-3811ME (BMS-284756), a new des-F(6)-quinolone, for treatment of meningitis caused by penicillin-resistant Streptococcus pneumoniae in rabbits. Takahata, M., Yamada, H., Morita, T., Furubou, S., Minami, S., Todo, Y., Watanabe, Y., Narita, H. Antimicrob. Agents Chemother. (2002) [Pubmed]
  16. Characterization of the penetration of garenoxacin into the breast milk of lactating women. Amsden, G.W., Nicolau, D.P., Whitaker, A.M., Maglio, D., Bello, A., Russo, R., Barros, A., Gajjar, D.A. Journal of clinical pharmacology. (2004) [Pubmed]
  17. Nasogastric administration of garenoxacin as crushed tablets with and without concomitant enteral feeding in healthy subjects. Krishna, G., Noveck, R., Vargas, R., Grasela, D., Wang, Z. Drugs in R&D (2007) [Pubmed]
  18. Concentrations of garenoxacin in plasma, bronchial mucosa, alveolar macrophages and epithelial lining fluid following a single oral 600 mg dose in healthy adult subjects. Andrews, J., Honeybourne, D., Jevons, G., Boyce, M., Wise, R., Bello, A., Gajjar, D. J. Antimicrob. Chemother. (2003) [Pubmed]
  19. Comparison of the minimum inhibitory, mutant prevention and minimum bactericidal concentrations of ciprofloxacin, levofloxacin and garenoxacin against enteric Gram-negative urinary tract infection pathogens. Hansen, G.T., Blondeau, J.M. Journal of chemotherapy (Florence, Italy) (2005) [Pubmed]
  20. Concentrations of the des-F(6)-quinolone garenoxacin in plasma and joint cartilage of immature rats. Kastner, M., Rahm, U., Baumann-Wilschke, I., Bello, A., Stahlmann, R. Arch. Toxicol. (2004) [Pubmed]
  21. Mutant prevention concentration of garenoxacin (BMS-284756) for ciprofloxacin-susceptible or -resistant Staphylococcus aureus. Zhao, X., Eisner, W., Perl-Rosenthal, N., Kreiswirth, B., Drlica, K. Antimicrob. Agents Chemother. (2003) [Pubmed]
  22. Fluorometric determination of mixtures of quinolones by means of partial least squares and neural networks. Jurado, J.M., Ocaña, J.A. Analytical sciences : the international journal of the Japan Society for Analytical Chemistry (2007) [Pubmed]
  23. Comparative activity of garenoxacin and other agents by susceptibility and time-kill testing against Staphylococcus aureus, Streptococcus pyogenes and respiratory pathogens. Noviello, S., Ianniello, F., Leone, S., Esposito, S. J. Antimicrob. Chemother. (2003) [Pubmed]
  24. In vitro activities of garenoxacin (BMS-284756) against Haemophilus influenzae isolates with different fluoroquinolone susceptibilities. Pérez-Vázquez, M., Román, F., Aracil, B., Cantón, R., Campos, J. Antimicrob. Agents Chemother. (2003) [Pubmed]
  25. Synthesis, antibacterial activity, and toxicity of 7-(isoindolin-5-yl)-4-oxoquinoline-3-carboxylic acids. Discovery of the novel des-F(6)-quinolone antibacterial agent garenoxacin (T-3811 or BMS-284756). Hayashi, K., Takahata, M., Kawamura, Y., Todo, Y. Arzneimittel-Forschung. (2002) [Pubmed]
  26. Population pharmacokinetics and pharmacodynamics of garenoxacin in patients with community-acquired respiratory tract infections. Van Wart, S., Phillips, L., Ludwig, E.A., Russo, R., Gajjar, D.A., Bello, A., Ambrose, P.G., Costanzo, C., Grasela, T.H., Echols, R., Grasela, D.M. Antimicrob. Agents Chemother. (2004) [Pubmed]
  27. Metabolism and disposition of novel des-fluoro quinolone garenoxacin in experimental animals and an interspecies scaling of pharmacokinetic parameters. Hayakawa, H., Fukushima, Y., Kato, H., Fukumoto, H., Kadota, T., Yamamoto, H., Kuroiwa, H., Nishigaki, J., Tsuji, A. Drug Metab. Dispos. (2003) [Pubmed]
  28. Bactericidal activity of garenoxacin tested by kill-curve methodology against wild type and QRDR mutant strains of Streptococcus pneumoniae. Anderegg, T.R., Jones, R.N. Diagn. Microbiol. Infect. Dis. (2004) [Pubmed]
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