E-4868, (-)-7[3-(R)-amino-2-(S)-methyl-1-azetidinyl]-1-(2,4- difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-3-quinolinecarboxylic acid, is a new fluoroquinolone with a 7-azetidin ring substituent. The in vitro activity against clinical isolates was compared with that of ciprofloxacin, ofloxacin and fleroxacin. In general, activity of E-4868 against aerobic and facultative anaerobic Gram-negative bacilli was equal to or slightly less active than ciprofloxacin with the exception of Morganella morganii and Proteus spp., E-4868 MIC90, 1 and 0.5 microgram/ml, respectively. E-4868 activity was two- to eight-fold higher than ciprofloxacin against Gram-positive cocci. For anaerobic species, E-4868 activity was comparable to that of ciprofloxacin, although against the Bacteroides fragilis group E-4868 was four-fold more active than ciprofloxacin.

01 Jan 1995·DrugsQ1 · MEDICINE

Quinolone Activity against Anaerobes

Q1 · MEDICINE

Review

Author: Appelbaum, P C

Currently available quinolones are either inactive or marginally active against anaerobic bacteria. This review summarises the in vitro activity of currently available as well as experimental quinolones against clinically significant anaerobic bacteria. Quinolones with low activity against anaerobes include ciprofloxacin, ofloxacin, levofloxacin, fleroxacin, pefloxacin, enoxacin, lomefloxacin and probably E 4868 and NM 441. Compounds with intermediate anaerobe activity include sparfloxacin, grepafloxacin, PD 131628 and AM 1155. Quinolones that are very active against anaerobes include clinafloxacin and DU 6859a. CP 99,219, a naphthyridone, is also very active against anaerobes. Toxicity problems have necessitated the withdrawal of some quinolones shown to have intermediate activity (temafloxacin and tosufloxacin) and the discontinuation of the development of some investigational agents (Win 57273 and BAY Y 3118) with high activity. Conclusions regarding the therapeutic value of quinolones against human anaerobic infections await further clinical toxicological and pharmacokinetic studies.

01 Jun 1994·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

Comparative activities of eight quinolones against members of the Bacteroides fragilis group

Q2 · MEDICINE

Article

Author: Borobio, M V ; Conejo, M ; Suarez, A I ; Ramirez, E ; Perea, E J

The in vitro activities of five new quinolones (clinafloxacin [CI-960 or PD-127391], BAY Y 3118, E-4868, E-5065, and E-5068) against 100 Bacteroides fragilis group bacterial isolates were compared with those of ciprofloxacin, ofloxacin, and sparfloxacin. Overall, E-5068 was the most active in vitro (MIC for 90% of isolates tested [MIC90], 0.25 microgram/ml); this was followed by clinafloxacin and BAY Y 3118 (MIC90, 0.5 microgram/ml). Ciprofloxacin, sparfloxacin, and ofloxacin were the least active (MIC90s, 64, 16, and 16 micrograms/ml, respectively). B. fragilis and Bacteroides caccae were more susceptible than the other members of the B. fragilis group to all of the quinolones tested.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Preclinical	EU	Esteve Pharmaceuticals S.A.	-

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