Bogdanovich, Tatiana;
Esel, Duygu;
Kelly, Linda M.;
Bozdogan, Bülent;
Credito, Kim;
Lin, Gengrong;
Smith, Kathy;
Ednie, Lois M.;
Hoellman, Dianne B.;
Appelbaum, Peter C.
Antistaphylococcal Activity of DX-619, a New Des-F(6)-Quinolone, Compared to Those of Other Agents
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Medientyp:
E-Artikel
Titel:
Antistaphylococcal Activity of DX-619, a New Des-F(6)-Quinolone, Compared to Those of Other Agents
Beteiligte:
Bogdanovich, Tatiana;
Esel, Duygu;
Kelly, Linda M.;
Bozdogan, Bülent;
Credito, Kim;
Lin, Gengrong;
Smith, Kathy;
Ednie, Lois M.;
Hoellman, Dianne B.;
Appelbaum, Peter C.
Erschienen:
American Society for Microbiology, 2005
Erschienen in:Antimicrobial Agents and Chemotherapy
Beschreibung:
<jats:title>ABSTRACT</jats:title>
<jats:p>
The in vitro activity of DX-619, a new des-F(6)-quinolone, was tested against staphylococci and compared to those of other antimicrobials. DX-619 had the lowest MIC ranges/MIC
<jats:sub>50</jats:sub>
s/MIC
<jats:sub>90</jats:sub>
s (μg/ml) against 131
<jats:italic>Staphylococcus aureus</jats:italic>
strains (≤0.002 to 2.0/0.06/0.5) and 128 coagulase-negative staphylococci (0.004 to 0.25/0.016/0.125). Among strains tested, 76
<jats:italic>S. aureus</jats:italic>
strains and 51 coagulase-negative staphylococci were resistant to ciprofloxacin. DX-619 had the lowest MIC
<jats:sub>50</jats:sub>
/MIC
<jats:sub>90</jats:sub>
values against 127 quinolone-resistant staphylococci (0.125/0.5), followed by sitafloxacin (0.5/4), moxifloxacin (2/8), gatifloxacin (4/16), levofloxacin (16/>32), and ciprofloxacin (>32/>32). Raised quinolone MICs were associated with mutations in GyrA (S84L) and single or double mutations in GrlA (S80F or Y; E84K, G, or V) in all
<jats:italic>S. aureus</jats:italic>
strains tested. A recent vancomycin-resistant
<jats:italic>S.
aureus</jats:italic>
(VRSA) strain (Hershey) was resistant to available quinolones and was inhibited by DX-619 at 0.25 μg/ml and
sitafloxacin at 1.0 μg/ml. Vancomycin (except VRSA), linezolid,
ranbezolid, tigecycline, and quinupristin-dalfopristin were active
against all strains, and teicoplanin was active against
<jats:italic>S.
aureus</jats:italic>
but less active against coagulase-negative staphylococci.
DX-619 produced resistant mutants with MICs of 1 to >32μ
g/ml after <50 days of selection compared to 16 to>
32 μg/ml for ciprofloxacin, sitafloxacin,
moxifloxacin, and gatifloxacin. DX-619 and sitafloxacin were also more
active than other tested drugs against selected mutants and had the
lowest mutation frequencies in single-step resistance selection. DX-619
and sitafloxacin were bactericidal against six quinolone-resistant
(including the VRSA) and seven quinolone-susceptible strains tested,
whereas gatifloxacin, moxifloxacin, levofloxacin, and ciprofloxacin
were bactericidal against 11, 10, 7, and 5 strains at 4× MIC
after 24 h, respectively. DX-619 was also bactericidal
against one other VRSA strain, five vancomycin-intermediate
<jats:italic>S.
aureus</jats:italic>
strains, and four vancomycin-intermediate
coagulase-negative staphylococci. Linezolid, ranbezolid, and
tigecycline were bacteriostatic and quinupristin-dalfopristin,
teicoplanin, and vancomycin were bactericidal against two, eight, and
nine strains, and daptomycin and oritavancin were rapidly bactericidal
against all strains, including the VRSA. DX-619 has potent in vitro
activity against staphylococci, including methicillin-, ciprofloxacin-,
and vancomycin-resistant
strains.
</jats:p>