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Chemical Compound Review

Levviax     (1R,2R,4R,6S,7R,8R,10R,13R,14S )-7-[(2S,3R...

Synonyms: Ketek, Telithromycin, AC1NUWEH, CHEMBL1136, HMR-3647, ...
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Disease relevance of RU66647


High impact information on RU66647


Chemical compound and disease context of RU66647


Biological context of RU66647

  • HMR 3647 displayed Michaelis-Menten saturation kinetics with a mean Vmax of 2315 ng/2.5 x 10(6) PMNs/5 min and a mean Km of 117 mg/liter (144 microM) [11].
  • Telithromycin (HMR 3647) had an IC50 = 0.08 microg/ml, and HMR 3832 was least effective with an IC50 = 0.11 microg/ml [12].

Anatomical context of RU66647


Associations of RU66647 with other chemical compounds

  • E. faecalis strains that had erythromycin MICs of 128 to > 512 micrograms/ml showed HMR 3647 MICs in the range of 0.03 to 16 micrograms/ml and HMR 3004 MICs in the range of 0.03 to 64 micrograms/ml [16].
  • In vitro activities of ketolide HMR 3647, macrolides, and clindamycin against Coryneform bacteria [17].
  • All methicillin-resistant S. aureus strains tested were resistant to erythromycin and had HMR 3647 and HMR 3004 MICs of > 64 micrograms/ml [16].

Gene context of RU66647


Analytical, diagnostic and therapeutic context of RU66647


  1. A ketolide resistance mutation in domain II of 23S rRNA reveals the proximity of hairpin 35 to the peptidyl transferase centre. Xiong, L., Shah, S., Mauvais, P., Mankin, A.S. Mol. Microbiol. (1999) [Pubmed]
  2. In vitro activities of the ketolide HMR 3647 against recent gram-positive clinical isolates and Haemophilus influenzae. Barry, A.L., Fuchs, P.C., Brown, S.D. Antimicrob. Agents Chemother. (1998) [Pubmed]
  3. In vitro development of resistance to telithromycin (HMR 3647), four macrolides, clindamycin, and pristinamycin in Streptococcus pneumoniae. Davies, T.A., Dewasse, B.E., Jacobs, M.R., Appelbaum, P.C. Antimicrob. Agents Chemother. (2000) [Pubmed]
  4. In vitro activities of ketolides HMR 3647 [correction of HRM 3647] and HMR 3004 [correction of HRM 3004], levofloxacin, and other quinolones and macrolides against Neisseria spp. and Moraxella catarrhalis. Sáez-Nieto, J.A., Vázquez, J.A. Antimicrob. Agents Chemother. (1999) [Pubmed]
  5. Pharmacodynamics of telithromycin In vitro against respiratory tract pathogens. Odenholt, I., Löwdin, E., Cars, O. Antimicrob. Agents Chemother. (2001) [Pubmed]
  6. Bronchopulmonary disposition of the ketolide telithromycin (HMR 3647). Muller-Serieys, C., Soler, P., Cantalloube, C., Lemaitre, F., Gia, H.P., Brunner, F., Andremont, A. Antimicrob. Agents Chemother. (2001) [Pubmed]
  7. Pharmacokinetics of the new ketolide telithromycin (HMR 3647) administered in ascending single and multiple doses. Namour, F., Wessels, D.H., Pascual, M.H., Reynolds, D., Sultan, E., Lenfant, B. Antimicrob. Agents Chemother. (2001) [Pubmed]
  8. Effect of proinflammatory cytokines on the interplay between roxithromycin, HMR 3647, or HMR 3004 and human polymorphonuclear neutrophils. Vazifeh, D., Bryskier, A., Labro, M.T. Antimicrob. Agents Chemother. (2000) [Pubmed]
  9. Postantibiotic suppression of growth of erythromycin A-susceptible and -resistant gram-positive bacteria by the ketolides telithromycin (HMR 3647) and HMR 3004. Munckhof, W.J., Borlace, G., Turnidge, J.D. Antimicrob. Agents Chemother. (2000) [Pubmed]
  10. HMR 3647 human-like treatment of experimental pneumonia due to penicillin-resistant and erythromycin-resistant Streptococcus pneumoniae. Piroth, L., Desbiolles, N., Mateo-Ponce, V., Martin, L., Lequeu, C., Charles, P.E., Portier, H., Chavanet, P. J. Antimicrob. Chemother. (2001) [Pubmed]
  11. Interactions between HMR 3647, a new ketolide, and human polymorphonuclear neutrophils. Vazifeh, D., Preira, A., Bryskier, A., Labro, M.T. Antimicrob. Agents Chemother. (1998) [Pubmed]
  12. Structure-activity relationships for six ketolide antibiotics. Champney, W.S., Tober, C.L. Curr. Microbiol. (2001) [Pubmed]
  13. In vitro activity of the ketolide HMR 3647 (RU 6647) for Legionella spp., its pharmacokinetics in guinea pigs, and use of the drug to treat guinea pigs with Legionella pneumophila pneumonia. Edelstein, P.H., Edelstein, M.A. Antimicrob. Agents Chemother. (1999) [Pubmed]
  14. The new ketolide HMR3647 accumulates in the azurophil granules of human polymorphonuclear cells. Miossec-Bartoli, C., Pilatre, L., Peyron, P., N'Diaye, E.N., Collart-Dutilleul, V., Maridonneau-Parini, I., Diu-Hercend, A. Antimicrob. Agents Chemother. (1999) [Pubmed]
  15. Telithromycin (HMR 3647) achieves high and sustained concentrations in tonsils of patients undergoing tonsillectomy. Gehanno, P., Sultan, E., Passot, V., Nabet, P., Danon, J., Romanet, P., Attal, P. Int. J. Antimicrob. Agents (2003) [Pubmed]
  16. In vitro activities of two ketolides, HMR 3647 and HMR 3004, against gram-positive bacteria. Malathum, K., Coque, T.M., Singh, K.V., Murray, B.E. Antimicrob. Agents Chemother. (1999) [Pubmed]
  17. In vitro activities of ketolide HMR 3647, macrolides, and clindamycin against Coryneform bacteria. Martínez-Martínez, L., Pascual, A., Suárez, A.I., Perea, E.J. Antimicrob. Agents Chemother. (1998) [Pubmed]
  18. Structures of ketolides and macrolides determine their mode of interaction with the ribosomal target site. Douthwaite, S., Champney, W.S. J. Antimicrob. Chemother. (2001) [Pubmed]
  19. In vitro activities of the new ketolide antibiotics HMR 3004 and HMR 3647 against Streptococcus pneumoniae in Germany. Reinert, R.R., Bryskier, A., Lütticken, R. Antimicrob. Agents Chemother. (1998) [Pubmed]
  20. Synthesis and antibacterial activity of HMR 3647 a new ketolide highly potent against erythromycin-resistant and susceptible pathogens. Denis, A., Agouridas, C., Auger, J.M., Benedetti, Y., Bonnefoy, A., Bretin, F., Chantot, J.F., Dussarat, A., Fromentin, C., D'Ambrières, S.G., Lachaud, S., Laurin, P., Le Martret, O., Loyau, V., Tessot, N., Pejac, J.M., Perron, S. Bioorg. Med. Chem. Lett. (1999) [Pubmed]
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