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Chemical Compound Review

AGN-PC-00D297     1-cyclopropyl-7-(5,8- diazabicyclo[4.3.0]no...

Synonyms: AG-K-19144, SureCN1883937, ACN-S002094, QC-9959, AC1L1HRG, ...
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Disease relevance of C07663

  • The clinical cure rate at test-of-cure for hospital-acquired cIAI was higher with moxifloxacin (82%, 22 of 27) versus comparator (55%, 17 of 31; P = 0.05); rates were similar for community-acquired infections (80% [124 of 156] versus 82% [136 of 165], respectively) [1].
  • RATIONALE: Moxifloxacin has promising preclinical activity against Mycobacterium tuberculosis, but has not been evaluated in multidrug treatment of tuberculosis in humans [2].
  • CONCLUSIONS: This study showed the fast diffusion of moxifloxacin into the lungs in ventilated patients with severe respiratory infection [3].
  • The bactericidal activity of moxifloxacin in patients with pulmonary tuberculosis [4].
  • OBJECTIVE: Our objective was to construct a population pharmacokinetic model for moxifloxacin disposition in plasma and bronchial secretions in patients with severe bronchopneumonia who were mechanically ventilated [3].

Psychiatry related information on C07663

  • Compliance for therapy, i.e., the percentage of tablets taken (> 85%), was 90.2 and 75.0%, numerically higher in moxifloxacin triple therapy group than in quadruple therapy group, but without statistical difference (p = .065) [5].

High impact information on C07663


Chemical compound and disease context of C07663


Biological context of C07663


Anatomical context of C07663


Associations of C07663 with other chemical compounds

  • To confirm that this substitution of moxifloxacin for isoniazid permits a shorter duration of treatment, a second study was performed in which mice were assessed for relapse after treatment with combination therapy for 3, 4, 5, or 6 months [21].
  • The anti-inflammatory activities of three quinolones, levofloxacin, moxifloxacin, and gatifloxacin, were investigated with an in vitro model of transendothelial migration (TEM) [22].
  • A two-compartment in vitro pharmacokinetic-pharmacodynamic model, with full computer-controlled devices, was used to accurately simulate human plasma pharmacokinetic profiles after multidose oral regimens of ciprofloxacin (750 mg every 12 h) and moxifloxacin (400 mg every 24 h) during 48 h [23].
  • Comparative in vitro activities of linezolid, quinupristin-dalfopristin, moxifloxacin, and trovafloxacin against erythromycin-susceptible and -resistant streptococci [24].
  • To characterize the penetration of moxifloxacin (BAY 12-8039) into peripheral target sites, the present study aimed at measuring unbound moxifloxacin concentrations in the interstitial space fluid by means of microdialysis, an innovative clinical sampling technique [25].

Gene context of C07663


Analytical, diagnostic and therapeutic context of C07663

  • Clinical trials of existing broad-spectrum agents such as the fluoroquinolone moxifloxacin are proceeding, on the basis of efficacy in models of infection and preliminary clinical data [30].
  • Patients with cIAI were stratified by disease severity (APACHE II score) and randomized to either IV/PO moxifloxacin (400 mg q24 hours) or comparator (IV piperacillin-tazobactam [3.0/0.375 g q6 hours] +/- PO amoxicillin-clavulanate [800 mg/114 mg q12 hours]), each for 5 to 14 days [1].
  • The mean postdose change from baseline QTc (Bazett) intervals for the 24-hour period after treatment with moxifloxacin ranged from 16.34 to 17.83 ms (P < .001, compared with placebo) [31].
  • CONCLUSIONS: Together, these findings suggest that rifapentine, moxifloxacin, and, perhaps, therapeutic DNA vaccination have the potential to improve on the current treatment of latent TB infection [6].
  • At the time of expected moxifloxacin maximum concentration, several electrocardiographic recordings were obtained at rest and during the course of a submaximal exercise test [12].


  1. Randomized controlled trial of moxifloxacin compared with piperacillin-tazobactam and amoxicillin-clavulanate for the treatment of complicated intra-abdominal infections. Malangoni, M.A., Song, J., Herrington, J., Choudhri, S., Pertel, P. Ann. Surg. (2006) [Pubmed]
  2. Moxifloxacin versus ethambutol in the first 2 months of treatment for pulmonary tuberculosis. Burman, W.J., Goldberg, S., Johnson, J.L., Muzanye, G., Engle, M., Mosher, A.W., Choudhri, S., Daley, C.L., Munsiff, S.S., Zhao, Z., Vernon, A., Chaisson, R.E. Am. J. Respir. Crit. Care Med. (2006) [Pubmed]
  3. Population pharmacokinetics of moxifloxacin in plasma and bronchial secretions in patients with severe bronchopneumonia. Simon, N., Sampol, E., Albanese, J., Martin, C., Arvis, P., Urien, S., Lacarelle, B., Bruguerolle, B. Clin. Pharmacol. Ther. (2003) [Pubmed]
  4. The bactericidal activity of moxifloxacin in patients with pulmonary tuberculosis. Gosling, R.D., Uiso, L.O., Sam, N.E., Bongard, E., Kanduma, E.G., Nyindo, M., Morris, R.W., Gillespie, S.H. Am. J. Respir. Crit. Care Med. (2003) [Pubmed]
  5. Efficacy of moxifloxacin-based triple therapy as second-line treatment for Helicobacter pylori infection. Cheon, J.H., Kim, N., Lee, D.H., Kim, J.M., Kim, J.S., Jung, H.C., Song, I.S. Helicobacter (2006) [Pubmed]
  6. Rifapentine, moxifloxacin, or DNA vaccine improves treatment of latent tuberculosis in a mouse model. Nuermberger, E., Tyagi, S., Williams, K.N., Rosenthal, I., Bishai, W.R., Grosset, J.H. Am. J. Respir. Crit. Care Med. (2005) [Pubmed]
  7. Are broad-spectrum fluoroquinolones more likely to cause Clostridium difficile-associated disease? Dhalla, I.A., Mamdani, M.M., Simor, A.E., Kopp, A., Rochon, P.A., Juurlink, D.N. Antimicrob. Agents Chemother. (2006) [Pubmed]
  8. Moxifloxacin, Ofloxacin, Sparfloxacin, and Ciprofloxacin against Mycobacterium tuberculosis: Evaluation of In Vitro and Pharmacodynamic Indices That Best Predict In Vivo Efficacy. Shandil, R.K., Jayaram, R., Kaur, P., Gaonkar, S., Suresh, B.L., Mahesh, B.N., Jayashree, R., Nandi, V., Bharath, S., Balasubramanian, V. Antimicrob. Agents Chemother. (2007) [Pubmed]
  9. 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]
  10. In vitro activities of newer quinolones against bacteroides group organisms. Snydman, D.R., Jacobus, N.V., McDermott, L.A., Ruthazer, R., Goldstein, E., Finegold, S., Harrell, L., Hecht, D.W., Jenkins, S., Pierson, C., Venezia, R., Rihs, J., Gorbach, S.L. Antimicrob. Agents Chemother. (2002) [Pubmed]
  11. Levofloxacin: an updated review of its use in the treatment of bacterial infections. Hurst, M., Lamb, H.M., Scott, L.J., Figgitt, D.P. Drugs (2002) [Pubmed]
  12. Effect of a single oral dose of moxifloxacin (400 mg and 800 mg) on ventricular repolarization in healthy subjects. Démolis, J.L., Kubitza, D., Tennezé, L., Funck-Brentano, C. Clin. Pharmacol. Ther. (2000) [Pubmed]
  13. Moxifloxacin in uncomplicated skin and skin structure infections. Muijsers, R.B., Jarvis, B. Drugs (2002) [Pubmed]
  14. Activities of mutant prevention concentration-targeted moxifloxacin and levofloxacin against Streptococcus pneumoniae in an in vitro pharmacodynamic model. Allen, G.P., Kaatz, G.W., Rybak, M.J. Antimicrob. Agents Chemother. (2003) [Pubmed]
  15. Effect of probenecid on the kinetics of a single oral 400mg dose of moxifloxacin in healthy male volunteers. Stass, H., Sachse, R. Clinical pharmacokinetics. (2001) [Pubmed]
  16. Selection of a moxifloxacin dose that suppresses drug resistance in Mycobacterium tuberculosis, by use of an in vitro pharmacodynamic infection model and mathematical modeling. Gumbo, T., Louie, A., Deziel, M.R., Parsons, L.M., Salfinger, M., Drusano, G.L. J. Infect. Dis. (2004) [Pubmed]
  17. Uptake and intracellular activity of moxifloxacin in human neutrophils and tissue-cultured epithelial cells. Pascual, A., García, I., Ballesta, S., Perea, E.J. Antimicrob. Agents Chemother. (1999) [Pubmed]
  18. Penetration of moxifloxacin into healthy and inflamed subcutaneous adipose tissues in humans. Joukhadar, C., Stass, H., Müller-Zellenberg, U., Lackner, E., Kovar, F., Minar, E., Müller, M. Antimicrob. Agents Chemother. (2003) [Pubmed]
  19. Influence of efflux transporters on the accumulation and efflux of four quinolones (ciprofloxacin, levofloxacin, garenoxacin, and moxifloxacin) in J774 macrophages. Michot, J.M., Seral, C., Van Bambeke, F., Mingeot-Leclercq, M.P., Tulkens, P.M. Antimicrob. Agents Chemother. (2005) [Pubmed]
  20. Discrepancy between uptake and intracellular activity of moxifloxacin in a Staphylococcus aureus-human THP-1 monocytic cell model. Paillard, D., Grellet, J., Dubois, V., Saux, M.C., Quentin, C. Antimicrob. Agents Chemother. (2002) [Pubmed]
  21. Moxifloxacin-containing regimens of reduced duration produce a stable cure in murine tuberculosis. Nuermberger, E.L., Yoshimatsu, T., Tyagi, S., Williams, K., Rosenthal, I., O'Brien, R.J., Vernon, A.A., Chaisson, R.E., Bishai, W.R., Grosset, J.H. Am. J. Respir. Crit. Care Med. (2004) [Pubmed]
  22. Effects of fluoroquinolones on the migration of human phagocytes through Chlamydia pneumoniae-infected and tumor necrosis factor alpha-stimulated endothelial cells. Uriarte, S.M., Molestina, R.E., Miller, R.D., Bernabo, J., Farinati, A., Eiguchi, K., Ramirez, J.A., Summersgill, J.T. Antimicrob. Agents Chemother. (2004) [Pubmed]
  23. Activities of ciprofloxacin and moxifloxacin against Stenotrophomonas maltophilia and emergence of resistant mutants in an in vitro pharmacokinetic-pharmacodynamic model. Ba, B.B., Feghali, H., Arpin, C., Saux, M.C., Quentin, C. Antimicrob. Agents Chemother. (2004) [Pubmed]
  24. Comparative in vitro activities of linezolid, quinupristin-dalfopristin, moxifloxacin, and trovafloxacin against erythromycin-susceptible and -resistant streptococci. Betriu, C., Redondo, M., Palau, M.L., Sánchez, A., Gómez, M., Culebras, E., Boloix, A., Picazo, J.J. Antimicrob. Agents Chemother. (2000) [Pubmed]
  25. Penetration of moxifloxacin into peripheral compartments in humans. Müller, M., Stass, H., Brunner, M., Möller, J.G., Lackner, E., Eichler, H.G. Antimicrob. Agents Chemother. (1999) [Pubmed]
  26. Anti-inflammatory effects of moxifloxacin on activated human monocytic cells: inhibition of NF-kappaB and mitogen-activated protein kinase activation and of synthesis of proinflammatory cytokines. Weiss, T., Shalit, I., Blau, H., Werber, S., Halperin, D., Levitov, A., Fabian, I. Antimicrob. Agents Chemother. (2004) [Pubmed]
  27. Moxifloxacin but not ciprofloxacin or azithromycin selectively inhibits IL-8, IL-6, ERK1/2, JNK, and NF-{kappa}B activation in a cystic fibrosis epithelial cell line. Blau, H., Klein, K., Shalit, I., Halperin, D., Fabian, I. Am. J. Physiol. Lung Cell Mol. Physiol. (2007) [Pubmed]
  28. Moxifloxacin inhibits cytokine-induced MAP kinase and NF-kappaB activation as well as nitric oxide synthesis in a human respiratory epithelial cell line. Werber, S., Shalit, I., Fabian, I., Steuer, G., Weiss, T., Blau, H. J. Antimicrob. Chemother. (2005) [Pubmed]
  29. Acyl glucuronidation of fluoroquinolone antibiotics by the UDP-glucuronosyltransferase 1A subfamily in human liver microsomes. Tachibana, M., Tanaka, M., Masubuchi, Y., Horie, T. Drug Metab. Dispos. (2005) [Pubmed]
  30. Prospects for new antitubercular drugs. Duncan, K., Barry, C.E. Curr. Opin. Microbiol. (2004) [Pubmed]
  31. Effects of three fluoroquinolones on QT interval in healthy adults after single doses. Noel, G.J., Natarajan, J., Chien, S., Hunt, T.L., Goodman, D.B., Abels, R. Clin. Pharmacol. Ther. (2003) [Pubmed]
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