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Antimicrobial Agents and Chemotherapy, August 1999, p. 2010-2016, Vol. 43, No. 8
Medical Research Laboratories, Lederle
(Japan), Ltd., Shiki-shi, Saitama-ken 353-8511, Japan
Received 31 December 1998/Returned for modification 19 April
1999/Accepted 4 June 1999
LJC 11,036 is the active metabolite of L-084, a novel oral
carbapenem that exhibits potent broad-spectrum activity. Antibacterial activities of LJC 11,036 against clinical isolates from respiratory infections, such as Streptococcus pneumoniae
(n = 52), Streptococcus pyogenes
(n = 19), Haemophilus influenzae
(n = 50), Klebsiella pneumoniae
(n = 53), and Moraxella catarrhalis
(n = 53), and from urinary-tract infections, such as
Escherichia coli (n = 53) (MICs at which
90% of the isolates were inhibited [MIC90s], 0.1,
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.
In Vitro Antibacterial Activity of LJC 11,036, an Active
Metabolite of L-084, a New Oral Carbapenem Antibiotic with
Potent Antipneumococcal Activity
0.006, 0.39, 0.05, 0.05, and 0.05 µg/ml, respectively), were 2- to
64-fold higher than those of imipenem, cefdinir, and faropenem.
Moreover, against these bacterial species, except for H. influenzae, the MIC90s of LJC 11,036 were 4- to
512-fold lower than those of levofloxacin. LJC 11,036 showed
bactericidal activity equal or superior to that of imipenem.
Bactericidal activity against penicillin-resistant S. pneumoniae (PRSP) did not vary with the phase of growth. LJC 11,036 had potent activity against various
-lactamase-producing strains, excluding carbapenemase
producers. Against renal dehydropeptidase-I, LJC 11,036 was more stable
than imipenem. Furthermore, LJC 11,036 produced in vitro postantibiotic
sub-MIC effects against PRSP HSC-3 (6.0 h at one-fourth the MIC) and
H. influenzae LJ5 (9.2 h at one-half the MIC). LJC
11,036 showed high binding affinities for PBP1A, -1B, -2A/2X, -2B, and
-3 of PRSP and for PBP1B, -2, -3A, and -3B of H. influenzae.
*
Corresponding author. Mailing address: Medical Research
Laboratories, Lederle (Japan), Ltd., 1-6-34 Kashiwa-cho,
Shiki-shi, Saitama-ken 353-8511, Japan. Phone: (048)
487-6622. Fax: (048) 474-1598.
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