scholarly journals Oritavancin Disrupts Membrane Integrity of Staphylococcus aureus and Vancomycin-Resistant Enterococci To Effect Rapid Bacterial Killing

2010 ◽  
Vol 54 (12) ◽  
pp. 5369-5371 ◽  
Author(s):  
Adam Belley ◽  
Geoffrey A. McKay ◽  
Francis F. Arhin ◽  
Ingrid Sarmiento ◽  
Sylvain Beaulieu ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Cell Death ◽  
Membrane Integrity ◽  
Clinical Development ◽  
Bacterial Membrane ◽  
Gram Positive ◽  
Bacterial Killing ◽  
Skin Structure ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant

ABSTRACT Oritavancin is an investigational lipoglycopeptide in clinical development for the treatment of acute bacterial skin and skin structure infections. In this study, we demonstrate that oritavancin causes bacterial membrane depolarization and permeabilization leading to cell death of Gram-positive pathogens and that these effects are attributable to the 4′-chlorobiphenylmethyl group of the molecule.

scholarly journals New Gram-Positive Agents: the Next Generation of Oxazolidinones and Lipoglycopeptides

2016 ◽  
Vol 54 (9) ◽  
pp. 2225-2232 ◽  
Author(s):  
Matthew P. Crotty ◽  
Tamara Krekel ◽  
Carey-Ann D. Burnham ◽  
David J. Ritchie
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Resistance ◽  
Next Generation ◽  
Gram Positive ◽  
Content Type ◽  
Skin Structure ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant ◽  
The U.S

The growing problem of antimicrobial resistance among bacterial pathogens, including methicillin-resistantStaphylococcus aureus(MRSA) and vancomycin-resistant enterococci (VRE), has reached a critical state. Tedizolid phosphate, dalbavancin, and oritavancin have recently been approved by the U.S. Food and Drug Administration (FDA) for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and represent the next generation of oxazolidinones and lipoglycopeptides. All three agents exhibitin vitroactivity and clinical efficacy against MRSA. Tedizolid phosphate and oritavancin demonstratein vitroactivity against VRE. These new Gram-positive agents are reviewed here.

scholarly journals In Vitro and In Vivo Activities of DA-7867, a New Oxazolidinone, against Aerobic Gram-Positive Bacteria

2005 ◽  
Vol 49 (6) ◽  
pp. 2498-2500 ◽  
Author(s):  
Eun Jeong Yoon ◽  
Yeong Woo Jo ◽  
Sung Hak Choi ◽  
Tae Ho Lee ◽  
Jae Keol Rhee ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pneumoniae ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Infection Models ◽  
Vancomycin Resistant

ABSTRACT In vitro and in vivo activities of DA-7867 were assessed against methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, and penicillin-resistant Streptococcus pneumoniae. All isolates were inhibited by DA-7867 at ≤0.78 μg/ml, a four-times-lower concentration than that of inhibition by linezolid. For murine infection models, DA-7867 also exhibited greater efficacy than linezolid against all isolates tested.

scholarly journals Activities of Oxadiazole Antibacterials against Staphylococcus aureus and Other Gram-Positive Bacteria

2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Sara Ceballos ◽  
Choon Kim ◽  
Derong Ding ◽  
Shahriar Mobashery ◽  
Mayland Chang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Content Type ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant ◽  
Mrsa Strains

ABSTRACT The activities of four oxadiazoles were investigated with 210 methicillin-resistant Staphylococcus aureus (MRSA) strains. MIC50 and MIC90 values of 1 to 2 and 4 μg/ml, respectively, were observed. We also evaluated the activity of oxadiazole ND-421 against other staphylococci and enterococci and in the presence of oxacillin for selected MRSA strains. The MIC for ND-421 is lowered severalfold in combination with oxacillin, as they synergize. The MIC90 of ND-421 against vancomycin-resistant enterococci is ≤1 μg/ml.

scholarly journals Assessment by Time-Kill Methodology of the Synergistic Effects of Oritavancin in Combination with Other Antimicrobial Agents against Staphylococcus aureus

2008 ◽  
Vol 52 (10) ◽  
pp. 3820-3822 ◽  
Author(s):  
Adam Belley ◽  
Eve Neesham-Grenon ◽  
Francis F. Arhin ◽  
Geoffrey A. McKay ◽  
Thomas R. Parr ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Agents ◽  
Synergistic Effects ◽  
Clinical Development ◽  
Synergistic Activity ◽  
Gram Positive ◽  
Vancomycin Resistant ◽  
Time Kill

ABSTRACT Oritavancin is a semisynthetic lipoglycopeptide in clinical development for serious gram-positive infections. This study describes the synergistic activity of oritavancin in combination with gentamicin, linezolid, moxifloxacin, or rifampin in time-kill studies against methicillin-susceptible, vancomycin-intermediate, and vancomycin-resistant Staphylococcus aureus.

scholarly journals In VivoAntibacterial Activity of MRX-I, a New Oxazolidinone

2014 ◽  
Vol 58 (4) ◽  
pp. 2418-2421 ◽  
Author(s):  
Cong-Ran Li ◽  
Qian-Qian Zhai ◽  
Xiu-Kun Wang ◽  
Xin-Xin Hu ◽  
Guo-Qing Li ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pneumoniae ◽  
Local Infection ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Content Type ◽  
Vancomycin Resistant Enterococci ◽  
Infection Models ◽  
Vancomycin Resistant

ABSTRACTMRX-I is a potent oxazolidinone antibiotic against Gram-positive pathogens, including methicillin-resistantStaphylococcus aureus(MRSA), penicillin-resistantStreptococcus pneumoniae(PRSP), penicillin-intermediateS. pneumoniae(PISP), and vancomycin-resistant enterococci (VRE). In this study, thein vivoefficacy of orally administered MRX-I was evaluated using linezolid as a comparator. MRX-I showed the same or better efficacy than linezolid in both systemic and local infection models against the tested strains.

scholarly journals Survival of Enterococci and Staphylococci on Hospital Fabrics and Plastic

2000 ◽  
Vol 38 (2) ◽  
pp. 724-726 ◽  
Author(s):  
Alice N. Neely ◽  
Matthew P. Maley
Keyword(s):  
Staphylococcus Aureus ◽  
Antibiotic Sensitivity ◽  
Critical Aspect ◽  
Gram Positive ◽  
Consistent Effect ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Control Procedures ◽  
Contact Control ◽  
Vancomycin Resistant

The transfer of gram-positive bacteria, particularly multiresistantStaphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), among patients is a growing concern. One critical aspect of bacterial transfer is the ability of the microorganism to survive on various common hospital surfaces. The purpose of this study was to determine the survival of 22 gram-positive bacteria (vancomycin-sensitive and -resistant enterococci and methicillin-sensitive and -resistant staphylococci) on five common hospital materials: smooth 100% cotton (clothing), 100% cotton terry (towels), 60% cotton–40% polyester blend (scrub suits and lab coats), 100% polyester (privacy drapes), and 100% polypropylene plastic (splash aprons). Swatches were inoculated with 104to 105 CFU of a microorganism, assayed daily by placing the swatches in nutritive media, and examining for growth after 48 h. All isolates survived for at least 1 day, and some survived for more than 90 days on the various materials. Smaller inocula (102) survived for shorter times but still generally for days. Antibiotic sensitivity had no consistent effect on survival. The long survival of these bacteria, including MRSA and VRE, on commonly used hospital fabrics, such as scrub suits, lab coats, and hospital privacy drapes, underscores the need for meticulous contact control procedures and careful disinfection to limit the spread of these bacteria.

scholarly journals In Vitro Activities of the Rx-01 Oxazolidinones against Hospital and Community Pathogens

2008 ◽  
Vol 52 (5) ◽  
pp. 1653-1662 ◽  
Author(s):  
Laura Lawrence ◽  
Paul Danese ◽  
Joe DeVito ◽  
Francois Franceschi ◽  
Joyce Sutcliffe
Keyword(s):  
Staphylococcus Aureus ◽  
Moraxella Catarrhalis ◽  
Multidrug Resistant ◽  
Gram Positive ◽  
Gram Negative ◽  
Vancomycin Resistant Enterococci ◽  
The Family ◽  
Vancomycin Resistant ◽  
Gram Negative Organisms

ABSTRACT Rx-01_423 and Rx-01_667 are two members of the family of oxazolidinones that were designed using a combination of computational and medicinal chemistry and conventional biological techniques. The compounds have a two- to eightfold-improved potency over linezolid against serious gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), multidrug-resistant streptococci, and vancomycin-resistant enterococci. This enhanced potency extends to the coverage of linezolid-resistant gram-positive microbes, especially multidrug-resistant enterococci and pneumococci. Compounds from this series expand the spectrum compared with linezolid to include fastidious gram-negative organisms like Haemophilus influenzae and Moraxella catarrhalis. Like linezolid, the Rx-01 compounds are bacteriostatic against MRSA and enterococci but are generally bactericidal against S. pneumoniae and H. influenzae.

scholarly journals Mode of Action of Van-M-02, a Novel Glycopeptide Inhibitor of Peptidoglycan Synthesis, in Vancomycin-Resistant Bacteria

2009 ◽  
Vol 54 (2) ◽  
pp. 960-962 ◽  
Author(s):  
Kenji Miura ◽  
Hidenori Yamashiro ◽  
Kouichi Uotani ◽  
Satoshi Kojima ◽  
Takashi Yutsudo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Inhibitory Activity ◽  
Mode Of Action ◽  
Resistant Bacteria ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Peptidoglycan Synthesis ◽  
Vancomycin Resistant Enterococci ◽  
Resistant Strains ◽  
Vancomycin Resistant

ABSTRACT Van-M-02, a novel glycopeptide, was revealed to exert potent activities against Gram-positive bacteria, including vancomycin-resistant enterococci (VRE) and vancomycin-resistant Staphylococcus aureus (VRSA). A crude assay system was then used to study the mode of action of Van-M-02 as a peptidoglycan synthesis model of both vancomycin-susceptible and -resistant strains. The results suggested that Van-M-02 inhibits the synthesis of lipid intermediates irrespective of their termini. This inhibitory activity may contribute to the anti-VRE and anti-VRSA activities observed.

scholarly journals In Vitro Activities of LY333328 and Comparative Agents against Nosocomial Gram-Positive Pathogens Collected in a 1997 Global Surveillance Study

2000 ◽  
Vol 44 (5) ◽  
pp. 1370-1374 ◽  
Author(s):  
Michael L. Zeckel ◽  
David A. Preston ◽  
Bradley S. Allen
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pneumoniae ◽  
Enterococcus Faecalis ◽  
Enterococcus Faecium ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant

ABSTRACT The in vitro activity of LY333328 was evaluated for 1,479 nosocomial gram-positive pathogens isolated in 12 countries during 1997. LY333328 MICs at which 90% of the isolates tested were inhibited for Enterococcus faecalis (n = 351),Enterococcus faecium (n = 100),Staphylococcus aureus (n = 593), coagulase-negative Staphylococcus species (n = 325), and Streptococcus pneumoniae(n = 110) were 1, 1, 2, 2, and 0.015 μg/ml, respectively. LY333328 demonstrated potent activity against isolates of vancomycin-resistant enterococci, oxacillin-resistant staphylococci, and penicillin-resistant pneumococci.

scholarly journals The Threat of the Emergence of Antimicrobial-Resistant Gram-Positive Pathogens in Canada

1994 ◽  
Vol 5 (suppl c) ◽  
pp. 9C-14C ◽  
Author(s):  
Donald E Low ◽  
Barbara M Willey ◽  
Allison J McGeer
Keyword(s):  
Staphylococcus Aureus ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
The United States ◽  
Multiple Resistance ◽  
Third Generation ◽  
Gram Positive ◽  
Gram Negative ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant ◽  
Third Generation Cephalosporins

Since the early 1980s, much attention has been focused on the emergence or resistance in nosocomially acquired Gram-negative pathogens. However, in the 1990s we are witnessing in North America the development and spread or multiple resistance in Gram-positive pathogens in the hospital selling as well as in the community. Methicillin resistant Staphylococcus aureus and vancomycin-resistant enterococci are now endemic in many urban centres in the United States, although less so in Canada. In some states, penicillin -resistant Streptococcus pneumoniae in the community selling has gone from rates of less than 5% in 1988 to 50% in 1994, including: resistance to third-generation cephalosporins and carbapenems. Although these same pathogens have now been identified in Canada, we may still be in a position to limit or prevent their spread.

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