Abstract
LJC 10,627 is a new parenteral carbapenem antibiotic. LJC 10,627 stability against human renal dehydropeptidase-I was compared with that of imipenem. Hydrolysis of this compound was not detectable by spectrophotometrical assay. Even after a 2-h incubation of antibiotics with this enzyme at 30 degrees C, the concentration of LJC 10,627 remained at 92.3% of the initial concentration, whereas imipenem completely disappeared. Thus, it was found that this compound was highly stable against human renal dehydropeptidase-I. Furthermore, LJC 10,627 had a low affinity for this enzyme, as indicated by the high Ki value (0.38 mM).
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Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Birnbaum J., Kahan F. M., Kropp H., MacDonald J. S. Carbapenems, a new class of beta-lactam antibiotics. Discovery and development of imipenem/cilastatin. Am J Med. 1985 Jun 7;78(6A):3–21. doi: 10.1016/0002-9343(85)90097-x. [DOI] [PubMed] [Google Scholar]
- Kropp H., Sundelof J. G., Hajdu R., Kahan F. M. Metabolism of thienamycin and related carbapenem antibiotics by the renal dipeptidase, dehydropeptidase. Antimicrob Agents Chemother. 1982 Jul;22(1):62–70. doi: 10.1128/aac.22.1.62. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Mitsuhashi S. In-vitro and in-vivo antibacterial activity of imipenem against clinical isolates of bacteria. J Antimicrob Chemother. 1983 Dec;12 (Suppl 500):53–64. doi: 10.1093/jac/12.suppl_d.53. [DOI] [PubMed] [Google Scholar]
- Neu H. C., Chin N. X., Saha G., Labthavikul P. In vitro activity against aerobic and anaerobic gram-positive and gram-negative bacteria and beta-lactamase stability of RS-533, a novel carbapenem. Antimicrob Agents Chemother. 1986 Dec;30(6):828–834. doi: 10.1128/aac.30.6.828. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Neu H. C., Novelli A., Chin N. X. In vitro activity and beta-lactamase stability of a new carbapenem, SM-7338. Antimicrob Agents Chemother. 1989 Jul;33(7):1009–1018. doi: 10.1128/aac.33.7.1009. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ubukata K., Hikida M., Yoshida M., Nishiki K., Furukawa Y., Tashiro K., Konno M., Mitsuhashi S. In vitro activity of LJC10,627, a new carbapenem antibiotic with high stability to dehydropeptidase I. Antimicrob Agents Chemother. 1990 Jun;34(6):994–1000. doi: 10.1128/aac.34.6.994. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Waley S. G. A spectrophotometric assay of beta-lactamase action on penicillins. Biochem J. 1974 Jun;139(3):789–790. doi: 10.1042/bj1390789. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wise R. In vitro and pharmacokinetic properties of the carbapenems. Antimicrob Agents Chemother. 1986 Sep;30(3):343–349. doi: 10.1128/aac.30.3.343. [DOI] [PMC free article] [PubMed] [Google Scholar]