Genomes and Genes
Summary: Compounds based on ERYTHROMYCIN with the 3-cladinose replaced by a ketone. They bind the 23S part of 70S bacterial RIBOSOMES.
Publications208 found, 100 shown here
- Structures of the Escherichia coli ribosome with antibiotics bound near the peptidyl transferase center explain spectra of drug actionJack A Dunkle
Department of Molecular and Cell Biology, University of California, Berkeley, CA 94720, USA
Proc Natl Acad Sci U S A 107:17152-7. 2010..The present data further argue that the identity of nucleotides 752, 2609, and 2055 of 23S ribosomal RNA explain in part the spectrum and selectivity of antibiotic action...
- Macrolides and ketolides: azithromycin, clarithromycin, telithromycinJerry M Zuckerman
Jefferson Medical College, Philadelphia, PA, USA
Infect Dis Clin North Am 18:621-49, xi-. 2004..This article reviews the pharmacokinetics, antimicrobial activity, clinical use, and adverse effects of these antimicrobial agents...
- Ketek--the FDA perspectiveJanice Soreth
N Engl J Med 356:1675-6. 2007
- Multicenter study of the mechanisms of resistance and clonal relationships of Streptococcus agalactiae isolates resistant to macrolides, lincosamides, and ketolides in SpainJ J Gonzalez
Servicio de Microbiologia, Hospital Vall d Hebron, Pg Vall d Hebron 119 129, 08035 Barcelona, Spain
Antimicrob Agents Chemother 49:2525-7. 2005..The erm(B), erm(TR), and mef(A) genes were present in 62%, 30.4%, and 3.8% of the isolates, respectively. There was considerable clonal diversity among them...
- Hospitalization rates among patients with community-acquired pneumonia treated with telithromycin vs clarithromycin: results from two randomized, double-blind, clinical trialsMichael S Niederman
Department of Medicine, Winthrop University Hospital, Minneola, NY 11501, USA
Curr Med Res Opin 20:969-80. 2004..To compare hospitalization rates among patients with community-acquired pneumonia (CAP) treated with oral telithromycin and clarithromycin, based on pooled data from two randomized, double-blind, multinational clinical trials...
- Structure-activity relationships for six ketolide antibioticsW S Champney
Department of Biochemistry and Molecular Biology, J H Quillen College of Medicine, East Tennessee State University, Johnson City 37614, USA
Curr Microbiol 42:203-10. 2001Six structurally related 3-keto-substituted macrolide antibiotics (ketolides) were compared for concentration-dependent inhibitory effects on growth rate, viable cell number, and protein synthesis rates in Staphylococcus aureus cells...
- Ketolides-telithromycin, an example of a new class of antibacterial agentsA Bryskier
Aventis Pharma, Infectious Disease Group Clinical Pharmacology, Romainville, France
Clin Microbiol Infect 6:661-9. 2000b>Ketolides are new medicinal chemical entities. They are obtained by removing the 3-L-cladinose sugar moiety from erythronolide A and oxidation of the resulting 3-hydroxyl...
- The FDA and the case of KetekDavid B Ross
George Washington University School of Medicine and Health Sciences, Washington, DC, USA
N Engl J Med 356:1601-4. 2007
- TelithromycinJ A Balfour
Adis International Limited, Mairangi Bay, Auckland, New Zealand
Drugs 61:815-29; discussion 830-1. 2001..first member of a new family of the macrolide-lincosamide-streptogramin-B (MLS(B)) class of antimicrobials, the ketolides. It has a good spectrum of activity against respiratory pathogens, including penicillin- and erythromycin-..
- Activity of the ketolide telithromycin is refractory to Erm monomethylation of bacterial rRNAMingfu Liu
Department of Biochemistry and Molecular Biology, University of Southern Denmark, DK 5230 Odense M, Denmark
Antimicrob Agents Chemother 46:1629-33. 2002..In contrast to the macrolides, monomethylation only mildly affects the antimicrobial activities of the ketolides HMR 3647 (telithromycin) and HMR 3004, and these drugs remain 16 to 250 times as potent as clarithromycin and ..
- Increased susceptibility of Pseudomonas aeruginosa to macrolides and ketolides in eukaryotic cell culture media and biological fluids due to decreased expression of oprM and increased outer-membrane permeabilityJulien M Buyck
Pharmacologie Cellulaire et Moléculaire, Louvain Drug Research Institute, Universite Catholique de Louvain, Bruxelles, Belgium
Clin Infect Dis 55:534-42. 2012..Nevertheless, azithromycin is successfully used in cystic fibrosis patients, supposedly because of "nonantibiotic effects."..
- Ketolide resistance in Streptococcus pyogenes correlates with the degree of rRNA dimethylation by ErmStephen Douthwaite
Department of Biochemistry and Molecular Biology, University of Southern Denmark, Campusvej 55, DK 5230 Odense M, Denmark
Mol Microbiol 58:613-22. 2005..pyogenes with constitutive erm(A) subtype (TR) are resistant to macrolides, but remain susceptible to ketolides such as telithromycin. Paradoxically, some strains of S...
- Clinical pharmacokinetics of telithromycin, the first ketolide antibacterialJun Shi
Sanofi Aventis Pharmaceuticals, Bridgewater, New Jersey, USA
Clin Pharmacokinet 44:915-34. 2005..In conclusion, telithromycin has a well characterised and reproducible pharmacokinetic profile, with pharmacokinetic/pharmacodynamic relationships supporting an oral dosage regimen of 800 mg once daily...
- Bronchopulmonary disposition of the ketolide telithromycin (HMR 3647)C Muller-Serieys
Unite de Microbiologie, Hopital Bichat Claude Bernard, 75877 Paris, France
Antimicrob Agents Chemother 45:3104-8. 2001Telithromycin (HMR 3647) is the first member of a new family of antimicrobials, the ketolides, developed specifically for the treatment of community-acquired respiratory tract infections...
- Predicting antibacterial response from pharmacodynamic and pharmacokinetic profilesD P Nicolau
Hartford Hospital, Connecticut 06102 5037, USA
Infection 29:11-5. 2001..Azithromycin, ketolides, such as telithromycin (HMR 3647), streptogramins and fluoroquinolones exhibit concentration-dependent killing ..
- Telithromycin resistance in Streptococcus pneumoniae is conferred by a deletion in the leader sequence of erm(B) that increases rRNA methylationNicole Wolter
Respiratory and Meningeal Pathogens Research Unit, National Institute for Communicable Diseases, Private Bag X4, Sandringham 2131, South Africa
Antimicrob Agents Chemother 52:435-40. 2008..Elevated erm(B) expression results in a higher level of rRNA methylation that presumably hinders telithromycin binding to the ribosome...
- Antibiotic innovation may contribute to slowing the dissemination of multiresistant Streptococcus pneumoniae: the example of ketolidesLulla Opatowski
Unité de Pharmacoépidémiologie et Maladies Infectieuses, Institut Pasteur, Paris, France
PLoS ONE 3:e2089. 2008Despite increasingly frequent bacterial resistance to antibiotics, antibacterial innovation is rare. Ketolides constitute one of the very few new antibiotic classes active against Streptococcus pneumoniae developed during the last 25 ..
- Macrolides, ketolides, and glycylcyclines: azithromycin, clarithromycin, telithromycin, tigecyclineJerry M Zuckerman
Jefferson Medical College, 1025 Walnut Street, Philadelphia, PA 19107, USA
Infect Dis Clin North Am 23:997-1026, ix-x. 2009..Telithromycin is approved for the treatment of community-acquired pneumonia. Severe hepatotoxicity has been reported with the use of telithromycin...
- Pharmacokinetics and comparative effects of telithromycin (HMR 3647) and clarithromycin on the oropharyngeal and intestinal microfloraC Edlund
Huddinge University Hospital, Karolinska Institute, Södertörns högskola, University College, Stockholm, Sweden
J Antimicrob Chemother 46:741-9. 2000..Telithromycin seems to have a more favourable ecological profile compared with clarithromycin in terms of resistance development in the normal microflora...
- Investigating the entire course of telithromycin binding to Escherichia coli ribosomesOurania N Kostopoulou
Department of Biochemistry, School of Medicine, University of Patras, 26504 Patras, Greece
Nucleic Acids Res 40:5078-87. 2012..Our data correlate well with recent crystallographic data and rationalize the changes in the accessibility of ribosomes to telithromycin in response to ribosomal mutations and ionic changes...
- The macrolide-ketolide antibiotic binding site is formed by structures in domains II and V of 23S ribosomal RNAL H Hansen
Department of Molecular Biology, Odense University, Denmark
Mol Microbiol 31:623-31. 1999..These findings indicate how drug derivatization can improve the inhibition of bacteria that have macrolide resistance conferred by changes in the peptidyl transferase loop...
- Design, synthesis and antibacterial activity of novel ketolides bearing an aryltetrazolyl-substituted alkyl side chainQiu Ling Song
Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Huangpu Avenue 601, Guangzhou, China
J Antibiot (Tokyo) 64:571-81. 2011A set of 17 novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain were synthesized and evaluated for their antibacterial activities, which the aryltetrazolyl group was selected to replace the hetero-aryl moiety of the ..
- Revisiting the structures of several antibiotics bound to the bacterial ribosomeDavid Bulkley
Departments of Chemistry, Yale University, Howard Hughes Medical Institute, New Haven, CT 06511, USA
Proc Natl Acad Sci U S A 107:17158-63. 2010....
- Ketolides--the modern relatives of macrolides : the pharmacokinetic perspectiveMarkus Zeitlinger
Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria
Clin Pharmacokinet 48:23-38. 2009..b>Ketolides are structurally related to macrolides and were developed to overcome macrolide resistance, while sharing ..
- Ketolides: the future of the macrolides?Angela M Nilius
Infectious Diseases Research R47T, AP52 Abbott Laboratories, Abbott Park, Illinois 60064 3537, USA
Curr Opin Pharmacol 2:493-500. 2002..b>Ketolides, semi-synthetic derivatives of erythromycin, overcome the macrolide resistance mechanisms found in Streptococcus ..
- Benefit-risk assessment of telithromycin in the treatment of community-acquired pneumoniaSteven D Brown
Clinical Microbiology Institute, Wilsonville, Oregon 97070, USA
Drug Saf 31:561-75. 2008..Although serious and sometimes fatal events have occurred in patients receiving telithromycin therapy, current data indicate that telithromycin offers an acceptable benefit risk ratio in the treatment of mild to moderate CAP...
- Structure-activity relationships of ketolides vs. macrolidesS Douthwaite
Department of Biochemistry and Molecular Biology, Odense University, Denmark
Clin Microbiol Infect 7:11-7. 2001..The ketolides, of which telithromycin is the first to reach clinical development, represent a new generation of antimicrobials ..
- Macrolide-ketolide inhibition of MLS-resistant ribosomes is improved by alternative drug interaction with domain II of 23S rRNAS Douthwaite
Department of Molecular Biology, Odense University, DK 5230 Odense M, Denmark
Mol Microbiol 36:183-93. 2000....
- Structures of MLSBK antibiotics bound to mutated large ribosomal subunits provide a structural explanation for resistanceDaqi Tu
Department of Molecular Biophysics and Biochemistry, Yale University, New Haven, Connecticut 06520, USA
Cell 121:257-70. 2005..coli) that stacks between them. The structure of large subunit containing a three residue deletion mutant of L22 shows a change in the L22 structure and exit tunnel shape that illuminates its macrolide resistance phenotype...
- Telithromycin-associated hepatotoxicity: Clinical spectrum and causality assessment of 42 casesAllen D Brinker
Office of Surveillance and Epidemiology, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA
Hepatology 49:250-7. 2009..Concurrence in assignment of causality increased after agreement on definitions of categories and interactive discussions...
- Telithromycin use and spontaneous reports of hepatotoxicityDavid D Dore
Department of Community Health, Brown Medical School, Providence, RI 02903, USA
Drug Saf 30:697-703. 2007..Recent reports have described cases of telithromycin-related hepatotoxicity. The objective of this study is to quantify the effect of telithromycin use on the risk of hepatotoxicity...
- Increasing prevalence of antimicrobial resistance among isolates of Streptococcus pneumoniae from the PROTEKT surveillance study, and compatative in vitro activity of the ketolide, telithromycinDavid Felmingham
GR Micro Ltd, 7 9 William Road, London NW1 3ER, UK
J Antimicrob Chemother 50:25-37. 2002..pneumoniae and demonstrate the potential of telithromycin as a therapeutic option for the treatment of community-acquired respiratory tract infections caused by this organism...
- Pharmacodynamics of telithromycin In vitro against respiratory tract pathogensI Odenholt
Antibiotic Research Unit, Department of Infectious Diseases and Clinical Microbiology, University Hospital, Uppsala, Sweden
Antimicrob Agents Chemother 45:23-9. 2001..Overall, telithromycin exhibited long postantibiotic effects and postantibiotic sub-MIC effects for all strains investigated...
- Drugs of the 21st century: telithromycin (HMR 3647)--the first ketolideGrit Ackermann
Institute for Medical Microbiology and Epidemiology of Infectious Diseases, University of Leipzig, Liebigstrasse 24, 04103 Leipzig, Germany
J Antimicrob Chemother 51:497-511. 2003Telithromycin (HMR 3647) is the first ketolide introduced into clinical practice. Ketolides are semisynthetic derivates of erythromycin A that carry novel biological properties on the erythronolide A ring...
- Species-specific antibiotic-ribosome interactions: implications for drug developmentDaniel N Wilson
Max Planck Institute for Molecular Genetics, Ihnestrasse 73, D 14195 Berlin, Germany
Biol Chem 386:1239-52. 2005..structural data for the bacterial D50S-antibiotic complexes reveals that the mode of binding of the macrolides, ketolides, streptogramins and lincosamides is generally similar to that observed in the archaeal H50S structures...
- 23S rRNA base pair 2057-2611 determines ketolide susceptibility and fitness cost of the macrolide resistance mutation 2058A-->GPeter Pfister
Institut fur Medizinische Mikrobiologie, Universitat Zurich, Gloriastrasse 30 32, CH 8006 Zurich, Switzerland
Proc Natl Acad Sci U S A 102:5180-5. 2005..However, this mutation is associated with a disparate resistance phenotype: It confers high-level resistance to ketolides in mycobacteria but only marginally affects ketolide susceptibility in streptococci...
- Structural basis for the antibiotic activity of ketolides and azalidesFrank Schlünzen
Max Planck Research Unit for Ribosomal Structure, 22603, Hamburg, Germany
Structure 11:329-38. 2003..The additional molecule also interacts with two proteins, L4 and L22, implicated in macrolide resistance. These studies illuminated and rationalized the enhanced activity of the drugs against specific macrolide-resistant bacteria...
- Clinical and bacteriological efficacy and safety of 5 and 7 day regimens of telithromycin once daily compared with a 10 day regimen of clarithromycin twice daily in patients with mild to moderate community-acquired pneumoniaGuy Tellier
Zoom International Clinical Research Group, 290 Montigny Street, Saint Jerome, Quebec J7Z 5T3, Canada
J Antimicrob Chemother 54:515-23. 2004..Bacteriological efficacy was also compared...
- Structural insight into the antibiotic action of telithromycin against resistant mutantsRita Berisio
Max Planck Research Unit for Ribosomal Structure, Hamburg, Germany
J Bacteriol 185:4276-9. 2003..Comparisons to other clinically relevant macrolides provided structural insights into its enhanced activity against macrolide-resistant strains...
- Comparison of in vitro activities of ketolides, macrolides, and an azalide against the spirochete Borrelia burgdorferiKlaus Peter Hunfeld
Institute of Medical Microbiology, University Hospital of Frankfurt, D 60596 Frankfurt Main, Germany
Antimicrob Agents Chemother 48:344-7. 2004Two ketolides, three macrolides, and one azalide were tested in vitro against 17 isolates of the B. burgdorferi s.l. complex...
- Comparative activity of quinolones, macrolides and ketolides against Legionella species using in vitro broth dilution and intracellular susceptibility testingJanet E Stout
VA Pittsburgh Healthcare System, VA Medical Center, Infectious Disease Section, University Drive C, Pittsburgh, PA 15240, USA
Int J Antimicrob Agents 25:302-7. 2005..of quinolones (trovafloxacin, gemifloxacin, levofloxacin, ciprofloxacin, moxifloxacin and grepafloxacin), ketolides (ABT-773 and telithromycin) and macrolides (clarithromycin, azithromycin and erythromycin) were evaluated ..
- Activity of cefditoren against clinical isolates of Streptococcus pneumoniae showing non-susceptibility to penicillins, cephalosporins, macrolides, ketolides or quinolonesAsuncion Fenoll
Int J Antimicrob Agents 29:224-6. 2007
- Trends in anti-bacterial resistance among Streptococcus pneumoniae isolated in the USA, 2000-2003: PROTEKT US years 1-3Stephen G Jenkins
Clinical Microbiology Laboratories, Department of Pathology, Mount Sinai School of Medicine, Mount Sinai Medical Center, New York, NY 10029 6574, USA
J Infect 51:355-63. 2005..To determine geographic and temporal trends in anti-bacterial resistance among Streptococcus pneumoniae isolated from patients with respiratory tract infections as part of the PROTEKT US surveillance study (2000-2003)...
- Comparative in vitro activity of telithromycin against macrolide-resistant and -susceptible Streptococcus pneumoniae, Moraxella catarrhalis and Haemophilus influenzaeFiona Walsh
Department of Medical Microbiology, Medical School, University of Edinburgh, Edinburgh EH8 9AG, UK
J Antimicrob Chemother 53:793-6. 2004..The second objective was to identify the influence of the erm(B) and mef(A) genes on the susceptibility of Streptococcus pneumoniae to telithromycin...
- [in vitro activity of telithromycin against Haemophilus influenzae]H Dabernat
Laboratoire de Microbiologie, Hopital Purpan, 31059 Toulouse, France
Pathol Biol (Paris) 50:58-62. 2002..Distribution of diameter zones showed a similar pattern to that of MICs but correlation between MICs and diameter zones was poor with correlation coefficients inferior to 0.5 whatever the agar media used...
- Activities of telithromycin against 13,874 Streptococcus pneumoniae isolates collected between 1999 and 2003David J Farrell
GR Micro Limited, London, United Kingdom
Antimicrob Agents Chemother 48:1882-4. 2004..The telithromycin MICs for 10 isolates (0.07%) were >/=4 micro g/ml, and these 10 isolates contained erm(B); there was no evidence of reproducible clonal spread between centers...
- Impact of ketolides on resistance selection and ecologic effects during treatment for respiratory tract infectionsC E Nord
Huddinge University Hospital, Karolinska Institute, Stockholm, Sweden
Microb Drug Resist 10:255-63. 2004b>Ketolides are a new class of antibacterials that have been specifically developed for the treatment of community-acquired respiratory tract infections in an era of increasing resistance among major etiologic pathogens...
- Will resistance to ketolides develop in Streptococcus pneumoniae?R Leclercq
CHU de Caen, Service de Microbiologie, France
J Infect 44:11-6. 2002..The ketolides, of which telithromycin is the first to be registered for clinical use, represent a new class of antibacterials ..
- Pneumococcal resistance to macrolides, lincosamides, ketolides, and streptogramin B agents: molecular mechanisms and resistance phenotypesPaul H Edelstein
Dept of Pathology and Laboratory Medicine, University of Pennsylvania Medical Center, Philadelphia, PA, 19104 4283, USA
Clin Infect Dis 38:S322-7. 2004The macrolides, lincosamides, ketolides, and streptogramin B agents (the MLKS(B) antimicrobial agents) have related chemical structures and share similar molecular targets on the 50S ribosomal subunit of Streptococcus pneumoniae...
- Effect of efflux on telithromycin and macrolide susceptibility in Haemophilus influenzaeTatiana Bogdanovich
Department of Pathology, Hershey Medical Center, P O Box 850, Hershey, Pennsylvania 17033, USA
Antimicrob Agents Chemother 50:893-8. 2006..in 58 clinical strains of Haemophilus influenzae with various susceptibilities to macrolides, azalides, and ketolides. Efflux pumps were studied by measuring accumulation of radioactive [3H]telithromycin and [N-methyl-3H]..
- Antibiotic activity of telithromycin and comparators against bacterial pathogens isolated from 3,043 patients with acute exacerbation of chronic bronchitisSanjay Sethi
University at Buffalo SUNY, USA
Ann Clin Microbiol Antimicrob 4:5. 2005..Antibacterial resistance is increasing worldwide and little surveillance data exist concerning pathogens isolated from patients with AECB...
- Streptococcus pneumoniae and Streptococcus pyogenes isolated from a paediatric population in Great Britain and Ireland: the in vitro activity of telithromcycin versus comparatorsJ Shackcloth
GR Micro Limited, 7 9 William Road, London NW1 3ER, UK
J Infect 48:229-35. 2004..To determine the distribution of macrolide resistance genes within the erythromycin resistant population...
- Activity of five quinolones, three macrolides and telithromycin against 12 Haemophilus influenzae strains with different resistance phenotypesG A Pankuch
Department of Pathology, Hershey Medical Center, Hershey, PA 17033, USA
Clin Microbiol Infect 11:1040-4. 2005..0-8.0 mg/L), except for two strains without efflux systems (0.0125-0.5 mg/L) and two with efflux systems and ribosomal protein mutations (> 64.0 mg/L), and were bactericidal against eight to ten strains tested at 2 x MIC after 24 h...
- Tissue kinetics of telithromycin, the first ketolide antibacterialC Muller-Serieys
Hopital Bichat Claude Bernard, 75877 Paris Cedex 18, France
J Antimicrob Chemother 53:149-57. 2004..The tissue kinetics profile of telithromycin, together with its microbiological profile, makes it a promising new antibacterial for the treatment of community-acquired RTIs...
- Telithromycin: a ketolide antibiotic for treatment of respiratory tract infectionsJohn R Lonks
Division of Infectious Diseases, Brown Medical School and Miriam Hospital, Providence, RI 02912, USA
Clin Infect Dis 40:1657-64. 2005..Unique visual adverse effects occurred in 0.27%-2.1% of patients receiving telithromycin therapy. Its enhanced activity against some common respiratory pathogens makes it a valuable addition to the available macrolides...
- Demographic analysis of antimicrobial resistance among Streptococcus pneumoniae: worldwide results from PROTEKT 1999-2000Daryl Hoban
Health Sciences Centre, Department of Clinical Microbiology, Winnipeg, Man, Canada
Int J Infect Dis 9:262-73. 2005..The influence of demographic factors upon antimicrobial resistance among 3362 isolates of Streptococcus pneumoniae from 25 countries was investigated, using univariate comparison and multivariate logistic regression...
- Impact of carbon dioxide on the susceptibility of key respiratory tract pathogens to telithromycin and azithromycinSam K Bouchillon
Laboratories International for Microbiology Studies, Inc, Schaumburg, IL 60173 3817, USA
J Antimicrob Chemother 56:224-7. 2005....
- In vitro activity of telithromycin (HMR3647), a new ketolide, against clinical isolates of Mycoplasma pneumoniae in JapanT Yamaguchi
Department of Laboratory Medicine, Nagasaki University School of Medicine, Nagasaki 852 8501, Japan
Antimicrob Agents Chemother 44:1381-2. 2000..00097 microg/ml, justifying clinical studies to determine its efficacy for treatment of M. pneumoniae...
- In vivo efficacy of telithromycin (HMR3647) against Streptococcus pneumoniae and Haemophilus influenzaeH Okamoto
Department of Microbiology, Toho University School of Medicine, Omori Nishi, Ota ku, Tokyo, Japan
Antimicrob Agents Chemother 45:3250-2. 2001..In respiratory tract infections caused by erythromycin A-susceptible S. pneumoniae or Haemophilus influenzae in mice, telithromycin was more effective than clarithromycin and comparable to azithromycin...
- Telithromycin-resistant Streptococcus pneumoniaeFred Goldstein
Emerg Infect Dis 11:1489-90. 2005
- Risk of hepatotoxicity associated with the use of telithromycin: a signal detection using data mining algorithmsYan Chen
Division of Pharmacy Practice and Administrative Sciences, James L Winkle College of Pharmacy, University of Cincinnati Academic Health Center, Cincinnati, OH 45267, USA
Ann Pharmacother 42:1791-6. 2008..With the exception of case reports, limited data are available regarding the risk of hepatotoxicity associated with the use of telithromycin...
- Selection of resistance of telithromycin against Haemophilus influenzae, Moraxella catarrhalis and streptococci in comparison with macrolidesLorenzo Drago
Laboratory of Clinical Microbiology, Department of Clinical Sciences L Sacco Teaching Hospital, University of Milan, Via GB Grassi 74, 20157 Milan, Italy
J Antimicrob Chemother 54:542-5. 2004..The in vitro abilities of telithromycin, azithromycin and clarithromycin to select for resistance were compared by testing isolates of Haemophilus influenzae, Moraxella catarrhalis, Streptococcus pneumoniae and beta-haemolytic streptococci...
- Diversity of ribosomal mutations conferring resistance to macrolides, clindamycin, streptogramin, and telithromycin in Streptococcus pneumoniaeAnnie Canu
UFR des Sciences Pharmaceutiques, Caen, France
Antimicrob Agents Chemother 46:125-31. 2002..In six remaining mutants, no mutations in L22, L4, or 23S rRNA could be detected...
- Kinetic bactericidal activity of telithromycin, azithromycin and clarithromycin against respiratory pathogensL Drago
Laboratory of Clinical Microbiology, Department of Clinical Sciences L Sacco, University of Milan, Italy
APMIS 113:655-63. 2005..In conclusion, telithromycin proved to possess bactericidal activity against a wide range of respiratory pathogens, including strains resistant to common macrolides...
- Ketolide antimicrobial activity persists after disruption of interactions with domain II of 23S rRNAGuy W Novotny
Department of Biochemistry and Molecular Biology, University of Southern Denmark, DK 5230 Odense M, Denmark
Antimicrob Agents Chemother 48:3677-83. 2004b>Ketolides are the latest derivatives developed from the macrolide erythromycin to improve antimicrobial activity...
- Streptococcus pyogenes isolates with characterized macrolide resistance mechanisms in Spain: in vitro activities of telithromycin and cethromycinMaría Isabel Morosini
Servicio de Microbiologia, Hospital Universitario Ramon y Cajal, Ctra de Colmenar, Km 9, 1, 28034 Madrid, Spain
J Antimicrob Chemother 52:50-5. 2003..6%) or mef(A) plus erm(B) (4.2%) was also observed. Both ketolides displayed a significant in vitro activity against S. pyogenes regardless of the macrolide resistance mechanisms...
- Telithromycin- and fluoroquinolone-resistant Streptococcus pneumoniae in Taiwan with high prevalence of resistance to macrolides and beta-lactams: SMART program 2001 dataPo Ren Hsueh
Departments of Laboratory Medicine and Internal Medicine, National Taiwan University Hospital, National Taiwan University College of Medicine, Taipei, Taiwan
Antimicrob Agents Chemother 47:2145-51. 2003..However, the occurrence of telithromycin resistance is impressive and raises concerns for the future...
- In vitro activity of the new ketolide telithromycin compared with those of macrolides against Streptococcus pyogenes: influences of resistance mechanisms and methodological factorsP Bemer-Melchior
Department of Microbiology, Laennec University Hospital, Nantes, France
Antimicrob Agents Chemother 44:2999-3002. 2000..The effect of 5 to 6% CO(2) was remarkable on resistant strains, by increasing MICs of telithromycin from 1 to 6 twofold dilutions against D-E- and F-group isolates...
- Overcoming antimicrobial resistance: profile of a new ketolide antibacterial, telithromycinR Leclercq
CHU de Caen, Service de Microbiologie, Avenue Cote de Nacre, 14033 Caen Cedex, France
J Antimicrob Chemother 48:9-23. 2001..Telithromycin is the first of a new family of antibacterials--the ketolides--and has been designed specifically for the treatment of community-acquired respiratory tract infections (RTIs)...
- Activities of cethromycin and telithromycin against recent North American isolates of Streptococcus pneumoniaeJames H Jorgensen
Department of Pathology, University of Texas Health Science Center, San Antonio, Texas, USA
Antimicrob Agents Chemother 48:605-7. 2004The in vitro activities of two investigational ketolides, cethromycin (formerly ABT-773) and telithromycin, were determined for a selected group of 312 Streptococcus pneumoniae isolates from a national surveillance program...
- Comparative activities of telithromycin (HMR 3647), levofloxacin, and other antimicrobial agents against human mycoplasmasC M Bebear
Laboratoire de Bacteriologie, Universite Victor Segalen Bordeaux 2, 33076 Bordeaux Cedex, France
Antimicrob Agents Chemother 44:1980-2. 2000..Telithromycin MICs of </=0.25 microgram/ml were found for all isolates, except for Mycoplasma hominis, while levofloxacin was active at concentrations of </=1 microgram/ml against all species studied...
- Ketolides: new antimicrobials for community-acquired pneumoniaPatricia J Neafsey
Home Healthc Nurse 23:141-3. 2005
- Intrapulmonary concentrations of telithromycin: clinical implications for respiratory tract infections due to Streptococcus pneumoniaeC T Ong
Center for Anti Infective Research and Development, Hartford Hospital, CT 06102, USA
Chemotherapy 51:339-46. 2005..To assess the bronchopulmonary drug disposition of a novel ketolide, telithromycin (TEL), the epithelial lining fluid (ELF) and alveolar macrophage (AM) concentrations were utilized as a surrogate marker for lung penetration...
- Clinical use of antimicrobial pharmacodynamic profiles to optimise treatment outcomes in community-acquired bacterial respiratory tract infections: application to telithromycinDavid P Nicolau
Center for Anti Infective Research and Development, Hartford Hospital, Hartford, CT 06102 5037, USA
Expert Opin Pharmacother 5:229-35. 2004..Telithromycin possesses pharmacodynamic characteristics that make this novel ketolide an optimal choice for the empirical management of community-acquired respiratory tract infections...
- Expression of the mef(E) gene encoding the macrolide efflux pump protein increases in Streptococcus pneumoniae with increasing resistance to macrolidesAleksandra K Wierzbowski
Department of Medical Microbiology, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada
Antimicrob Agents Chemother 49:4635-40. 2005..In conclusion, increased expression of mef(E) is associated with higher levels of macrolide resistance in macrolide-resistant S. pneumoniae...
- Influence of carbon dioxide on the MIC of telithromycin for Streptococcus pneumoniae: an in vitro-in vivo studyEric Batard
Laboratoire d Antibiologie, UER de Medecine, 1 rue Gaston Veil, 44035 Nantes Cedex 01, France
Antimicrob Agents Chemother 49:464-6. 2005..2% of 346 Streptococcus pneumoniae ermB-positive strains. An increased telithromycin MIC in CO(2) was not correlated with loss of its activity in the murine sepsis/peritonitis model...
- In vitro activity of new ketolides against macrolide-susceptible and -resistant Staphylococcus aureus isolates with defined resistance gene statusFranz Josef Schmitz
J Antimicrob Chemother 49:580-2. 2002
- Pharmacodynamic activity of telithromycin at simulated clinically achievable free-drug concentrations in serum and epithelial lining fluid against efflux (mefE)-producing macrolide-resistant Streptococcus pneumoniae for which telithromycin MICs varyGeorge G Zhanel
Department of Medical Microbiology, University of Manitoba, Winnipeg, Manitoba, Canada
Antimicrob Agents Chemother 49:1943-8. 2005..In conclusion, free-telithromycin concentrations in serum and ELF simulating C(max)/MIC > or = 3.5 and AUC(0-24 h)/MIC > or = 25 completely eradicated (> or =4 log(10) killing) macrolide-resistant S. pneumoniae at 24 and 48 h...
- In vitro activities of new ketolide, telithromycin, and eight other macrolide antibiotics against Streptococcus pneumoniae having mefA and ermB genes that mediate macrolide resistanceKimiko Ubukata
Laboratory of Infectious Agents Surveillance, Kitasato Institute for Life Sciences, Kitasato University, 5 9 1 Sirokane, Minato ku, Tokyo 108 8641, Japan
J Infect Chemother 9:221-6. 2003..Most strains having the mefA and ermB genes were serotyped to 3, 6, 14, 19, and 23. These results suggest that TEL may be a useful chemotherapeutic agent for respiratory tract infections caused by S. pneumoniae...
- Effects of macrolides and ketolides on mycobacterial infectionsLuiz E Bermudez
Department of Biomedical Sciences, College of Veterinary Medicine, Oregon State University, Corvallis, OR 97331, USA
Curr Pharm Des 10:3221-8. 2004..b>Ketolides are a semi-synthetic derivative of erythromycin A, which differs from erythromycin A by substitution of a 3-keto ..
- Antipneumococcal activities of a ketolide (HMR 3647), a streptogramin (quinupristin-dalfopristin), a macrolide (erythromycin), and a lincosamide (clindamycin)A L Barry
The Clinical Microbiology Institute, Wilsonville, Oregon 97070, USA
Antimicrob Agents Chemother 42:945-6. 1998....
- 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 pneumoniaP H Edelstein
Departments of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 4283, USA
Antimicrob Agents Chemother 43:90-5. 1999..HMR 3647 is effective against L. pneumophila in vitro, in infected macrophages, and in a guinea pig model of Legionnaires' disease. HMR 3647 given once daily should be evaluated as a treatment for Legionnaires' disease in humans...
- In vitro activities of the novel ketolide telithromycin (HMR 3647) against erythromycin-resistant Streptococcus speciesJ Jalava
Antimicrobial Research Laboratory, National Public Health Institute, Turku, Finland
Antimicrob Agents Chemother 45:789-93. 2001..008 to 0.25 microg/ml). Our in vitro data show that for S. pyogenes strains which constitutively express the erm(B) methylase gene, MICs are so high that the strains might be clinically resistant to telithromycin...
- In vitro activity of telithromycin, a new ketolide, against Chlamydia pneumoniaeN Miyashita
Division of Respiratory Diseases, Department of Medicine, Kawasaki Medical School, 577 Matsushima, Kurashiki City, Okayama 701 0192, Japan
J Antimicrob Chemother 48:403-5. 2001..These results appear to indicate that telithromycin is an effective antibiotic that should play some role in the treatment of respiratory tract infections caused by C. pneumoniae...
- Comparative in vitro activity of telithromycin (HMR 3647), three macrolides, amoxycillin, cefdinir and levofloxacin against gram-positive clinical isolates in JapanH Okamoto
Department of Microbiology, Toho University School of Medicine, Omori Nishi, Ota ku, Tokyo, Japan
J Antimicrob Chemother 46:797-802. 2000..Against erythromycin A-susceptible or inducibly resistant Staphylococcus aureus and erythromycin A-susceptible and intermediate Enterococcus faecalis, telithromycin was highly active...
- Telithromycin: a new ketolide antimicrobial for treatment of respiratory tract infectionsH M Yassin
VA New Jersey Health Care System, East Orange, NJ and UMDNJ, New Jersey Medical School, Newark, NJ, USA
Expert Opin Investig Drugs 10:353-67. 2001..The most common adverse events were diarrhoea, nausea, headache and dizziness. Telithromycin should provide an effective, convenient and well-tolerated once-daily oral therapy for treatment of respiratory infections...
- Activity of telithromycin, a new ketolide antibacterial, against atypical and intracellular respiratory tract pathogensM R Hammerschlag
Division of Infectious Diseases, Department of Pediatrics, Box 49, SUNY Downstate Medical Center, 450 Clarkson Avenue, Brooklyn, NY 11203 2098, USA
J Antimicrob Chemother 48:25-31. 2001..Telithromycin (HMR 3647) is the first of a new family of antibacterials, the ketolides, and has been designed specifically for the treatment of community-acquired respiratory tract infections (RTIs)...
- Lung concentrations of telithromycin after oral dosingO A Khair
Department of Medical Microbiology, City Hospital NHS Trust, Birmingham B18 7QH, UK
J Antimicrob Chemother 47:837-40. 2001..03 mg/L), as well as the atypical microorganism Mycoplasma pneumoniae (0.001 mg/L), and suggest that telithromycin may be effective for the treatment of community-acquired pneumonia and chronic obstructive pulmonary disease...
- In vitro pharmacodynamics of the new ketolides HMR 3004 and HMR 3647 (Telithromycin) against Chlamydia pneumoniaeI Gustafsson
Departments of Infectious Diseases, University Hospital, Uppsala, Sweden
Antimicrob Agents Chemother 44:1846-9. 2000The ketolides HMR 3004 and HMR 3647 (telithromycin) are a new class of macrolides that have a potential clinical efficacy against intracellular pathogens...
- Antibacterial effect of telithromycin (HMR 3647) and comparative antibiotics against intracellular Legionella pneumophilaA L Baltch
Infectious Disease Section, Stratton VA Medical Center and Albany Medical College, NY 12208, USA
J Antimicrob Chemother 46:51-5. 2000..In conclusion, the ketolide telithromycin has excellent activity against intracellular L. pneumophila strain L-1033 and should be evaluated for therapy of legionnaires' disease...
- In vitro activities of the ketolides telithromycin (HMR 3647) and HMR 3004 compared to those of clarithromycin against slowly growing mycobacteria at pHs 6.8 and 7.4N Rastogi
Unite de la Tuberculose et des Mycobacteries, Institut Pasteur, 97165 Pointe à Pitre Cedex, Guadeloupe
Antimicrob Agents Chemother 44:2848-52. 2000The in vitro activities of HMR 3647 (telithromycin) and HMR 3004, two novel semisynthetic ketolides, were investigated and compared with that of the reference macrolide drug, clarithromycin, against 34 strains of slowly growing ..
- Efficacy and tolerability of once-daily telithromycin compared with high-dose amoxicillin for treatment of community-acquired pneumoniaL Hagberg
Dept of Infectious Diseases, Sahlgrenska University Hospital, Goteborg, Sweden
Infection 30:378-86. 2002..This randomized, double-blind study compared the efficacy and tolerability of the new ketolide antimicrobial telithromycin with that of high-dose amoxicillin in the treatment of community-acquired pneumonia (CAP)...
- Macrolide-resistance mechanisms in Streptococcus pneumoniae isolates from BelgiumJ Van Eldere
Department of Microbiology and Immunology, Katholieke Universiteit Leuven, Leuven, Belgium
Clin Microbiol Infect 11:332-4. 2005..No difference in the prevalence of different resistance mechanisms was observed compared to isolates collected in 1995-1997...
- In vitro activity of the new ketolide ABT-773 against community acquired respiratory tract isolates and Viridans StreptococciJose Maria Casellas
Centro de Estudios en Antimicrobianos, Buenos Aires, Argentina
Diagn Microbiol Infect Dis 42:107-12. 2002..ABT-773 exerted bactericidal activity against selected isolates of S. pneumoniae, M. catarrhalis and H. influenzae, however, it was only bacteriostatic against methicillin-susceptible S. aureus...
- PROTEKT years 1-3 (1999-2002): study design and methodologyI Harding
The Micron Group, Marmont Priory Farm, Upwell, Wisbech, Cambridgeshire PE14 9AR, UK
J Chemother 16:9-18. 2004
- Susceptibility to telithromycin in 1,011 Streptococcus pyogenes isolates from 10 central and Eastern European countriesKensuke Nagai
Department of Pathology, Hershey Medical Center, Hershey, Pennsylvania 17033, USA
Antimicrob Agents Chemother 46:546-9. 2002..3% of strains. Erm(A) [subclass erm(TR)] was most commonly encountered (60.5%), followed by mef(A) (23.4%) and erm(B) (14.5%). At <0.5 microg/ml, telithromycin was active against 98.5% of the strains tested...
- [Molecular analytical evaluation of macrolide- and ketolide-resistant Streptococcus pneumoniae--mechanism of action of telithromycin and resistance to it]Matsuhisa Inoue
Department of Microbiology, Kitasato University School of Medicine
Jpn J Antibiot 57:425-37. 2004..actions of TEL were considered to be derived from its novel chemical structure and might be characteristics of ketolides not possessed by macrolides. In the survey of PROTEKT in 1999 to 2002, among 13,864 strains of S...
- Activity of telithromycin against 26 quinolone-resistant pneumococci with known quinolone-resistance mechanismsK Nagai
Department of Pathology, Hershey Medical Center, Hershey, PA 17033, USA
Clin Microbiol Infect 7:703-5. 2001..Ciprofloxacin MICs (mg/L) were 8-64 compared to 1-32 (levofloxacin), 0.5 . or = 32 (sparfloxacin) and 0.125-4 (moxifloxacin). Telithromycin MIC50 and MIC90 values (mg/L) were 0.016 and 0.25, with only one strain having an MIC of 2 mg/L...
- In vitro activities of novel 2-fluoro-naphthyridine-containing ketolidesDarren Abbanat
Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ 08869, USA
Antimicrob Agents Chemother 49:309-15. 2005In vitro activities of erythromycin A, telithromycin, and two investigational ketolides, JNJ-17155437 and JNJ-17155528, were evaluated against clinical bacterial strains, including selected common respiratory tract pathogens...
- Binding site of the bridged macrolides in the Escherichia coli ribosomeLiqun Xiong
Center for Pharmaceutical Biotechnology, University of Illinois, 900 S Ashland Ave, Chicago, IL 60607, USA
Antimicrob Agents Chemother 49:281-8. 2005b>Ketolides represent the latest group of macrolide antibiotics. Tight binding of ketolides to the ribosome appears to correlate with the presence of an extended alkyl-aryl side chain...
- Pharmacodynamic profile of telithromycin against macrolide- and fluoroquinolone-resistant Streptococcus pneumoniae in a neutropenic mouse thigh modelPamela R Tessier
Center for Anti Infective Research and Development, Hartford Hospital, 80 Seymour St, Hartford, CT 06102 5037, USA
Antimicrob Agents Chemother 49:188-94. 2005..pneumoniae strains and bacterial inhibition (stasis) of telithromycin were predicted by ratios of the AUC for the free drug concentration/MIC of approximately 1,000 and 200, respectively...
- Mechanism of Induction of erm Genes By Ketolide AntibioticsNora Vazquez Laslop; Fiscal Year: 2010..However, recent data have shown that ketolides do induce expression of ermC...
- Assembly Properties of the 50S Ribosomal Subunit Under Pertubation ConditionsMichael Sykes; Fiscal Year: 2009..Additionally, Lincosamides, ketolides and streptogramin B antibiotics have each been shown to specifically inhibit assembly of the large subunit in E...
- GENERATION OF KETOLIDES BY COMBINATORIAL BIOSYNTHESISYongquan Xue; Fiscal Year: 1999..venezuelae through which pikromycin analogues can be generated rapidly and systematically; and 2) generate novel ketolides by creating a 'hybrid biosynthetic pathway that combines the pikromycin polyketide synthase (PikA) with a ..
- ENGINEERED BIOSYNTHESIS OF NOVEL KETOLIDE ANTIBIOTICSKevin Reynolds; Fiscal Year: 2000..PROPOSED COMMERCIAL APPLICATIONS: Ketolides hold promise as a solution to the increase in erythromycin- resistant bacterial pathogens, including ..
- Macrolide Discovery through GlycosylationAlex Romero; Fiscal Year: 2006..development and the potential for cross-resistance between our lead compounds and other leading macrolides/ketolides, an important criteria for assessing a compound's future marketability...
- ANTIBIOTIC INHIBITION OF BACTERIAL RIBOSOME FORMATIONWILLIAM CHAMPNEY; Fiscal Year: 2002..This investigation will explore the new observation that macrolide antibiotics as well as the ketolides, lincosamides, streptogramin B compounds and oxazolidinones can all inhibit the assembly of the large ribosomal ..
- Molecular Epidemiology, Virulence, and Genomic Characterization of UreaplasmasKen B Waites; Fiscal Year: 2010....
- BIOCHEMISTRY AND MOLECULAR GENETICS OF MITOMYCIN BIOSYNTDavid Sherman; Fiscal Year: 2003..Overall, this work will provide an important theoretical and experimental base for future combinatorial biology-based production of novel AHBA-derived natural products using molecular genetic technology. ..
- Leptomycin B Development for Cancer TherapyCharles Hutchinson; Fiscal Year: 2004..coelicolor, we will proceed with preclinical development of LMB or the discovery and development of an LMB analog in Phase II research. ..
- RIBOSOMAL PEPTIDYL TRANSFERASE CENTERAlexander Mankin; Fiscal Year: 2003..Understanding structure and function of the main catalytic center of the ribosome is indispensable for the rational design of new antibiotics and overcoming mechanisms of drug resistance. ..
- DM1-Monoclonal Antibody ConjugatesCharles Hutchinson; Fiscal Year: 2002..Therefore, a successful outcome of our research would meet the needs for preclinical and clinical development at a far lower cost than the current DM1 synthesis that is the only source of this cytotoxin. ..
- Genomic Analysis of Antibiotic BiosynthesisDavid Sherman; Fiscal Year: 2005..coelicolor genome. ..
- New mechanism of resistance to oxazolidinone antibiotics in Staphylococcus aureusAlexander S Mankin; Fiscal Year: 2010....
- New Ketolide Antibacterial DrugsCharles Hutchinson; Fiscal Year: 2005..A have excellent in vitro and in vivo antibacterial activity, comparable to or better than the leading ketolides in current clinical trials or approved by the FDA for specific uses...
- Novel Geldanamycin Analogs as Anti-tumor AgentsGary Ashley; Fiscal Year: 2005..By these studies, we will identify the best geldanamycin analog to carry forward into drug development, with the eventual aim of filing and IND application and performing clinical trials. ..
- Antibiotic Hypersusceptibility Mutations in BacteriaAlexander Mankin; Fiscal Year: 2005..In addition to identifying promising targets for potentiators, the project will help unravel new aspects of the mechanism of action of antibiotics and new features of bacterial physiology. ..
- COMBINATORIAL BIOSYNTHESIS AND THE PIKROMYCIN PATHWAYDavid Sherman; Fiscal Year: 2002....
- HAEMOPHILUS ANTIGEN REGULATION OF INFLAMMATION IN COPDSanjay Sethi; Fiscal Year: 2003..Identification of the integral bacterial and host components that contribute to immune-mediated inflammation in COPD will ultimately lead to novel therapeutic strategies to alter disease progression and improve outcome in COPD. ..
- Laulimalide Production GenesCharles Hutchinson; Fiscal Year: 2003..Success will lead to development of a fermentation-based process to make large amounts of laulimalide or one of its analogs for preclinical studies as an antitumor drug. ..
- Discodermolide Biosynthesis GenesCharles Hutchinson; Fiscal Year: 2002..Our research will also establish the technological base for a general approach to making many other currently scarce marine polyketides with anti-tumor activity available in large amounts for drug development. ..
- MYCOBACTERIAL ENVIRONMENT WITHIN MACROPHAGESLuiz Bermudez; Fiscal Year: 2003..We believe that the proposed studies will generate important information about the phagosome environment and the mycobacterial response to it. ..
- Innate Immunity and exacerbations of COPDSanjay Sethi; Fiscal Year: 2009..The overall goal of this research is to identify specific aspects of the innate defense of the lung that determine the frequency of exacerbations in COPD that will serve as potential therapeutic targets to reduce exacerbations. ..
- CRYSTALLOGRAPHIC STUDIES ON RIBOSOMAL PARTICLESADA E YONATH; Fiscal Year: 2010..These studies have already illuminated principles of drug selectivity, and provided significant basic knowledge of possible pathways of drug resistance, hence paving the way to improve therapeutic properties. ..
- Post Translation Regulation in MycobacteriaLuiz Bermudez; Fiscal Year: 2008..In case we confirm our hypothesis, future work will address the role of Ion in M. tuberculosis [unreadable] [unreadable] [unreadable]..