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Chemical Compound Review

Doribax     (4R,5R,6S)-6-(1- hydroxyethyl)-4-methyl-7...

Synonyms: Doripenem, Doribax (TN), SureCN37471, CHEMBL491571, BCPP000252, ...
 
 
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Disease relevance of S-4661

  • Doripenem versus Pseudomonas aeruginosa in vitro: activity against characterized isolates, mutants, and transconjugants and resistance selection potential [1].
  • ESBL production did not raise the MICs of doripenem for Escherichia coli transconjugants, and studies with known expression mutants confirmed that neither inducible nor depressed AmpC beta-lactamase expression was protective in Enterobacter cloacae, Citrobacter freundii, Serratia marcescens, or Morganella morganii [2].
  • Comparative activities of doripenem versus isolates, mutants, and transconjugants of Enterobacteriaceae and Acinetobacter spp. with characterized beta-lactamases [2].
  • Similarly, MICs of doripenem for both AmpC-inducible and -derepressed Enterobacter isolates were 0.06 to 0.5 microg/ml [2].
  • Resistance to all carbapenems, including doripenem (MICs of mostly 16 to 64 microg/ml, compared with 0.25 to 1 microg/ml for typical strains), was seen in Acinetobacter isolates with metallo-beta-lactamases or OXA-carbapenemases [2].
 

High impact information on S-4661

 

Chemical compound and disease context of S-4661

 

Biological context of S-4661

 

Anatomical context of S-4661

  • The accumulation of neutrophils in the uterus in the S-4661-treated group was less marked and the number of bacteria significantly lower than those in the untreated group [12].
  • The antibacterial activity of S-4661, a new parenteral carbapenem antibiotic, was assessed against the major urological pathogens isolated from patients with complicated urinary tract infections [15].
  • In mice, the doripenem level was highest in the blood plasma, followed by the kidney, liver, lung, heart and spleen [14].
 

Associations of S-4661 with other chemical compounds

 

Gene context of S-4661

  • Study of the synergism between carbapenems and vancomycin or teicoplanin against MRSA, focusing on S-4661, a carbapenem newly developed in Japan [17].
  • Empiric therapy with doripenem, as with other antipseudomonal carbapenems, may be useful in hospital and intensive care unit settings where multidrug resistance has emerged, especially in Gram-negative enteric pathogens [11].
 

Analytical, diagnostic and therapeutic context of S-4661

  • S-4661, a new injectable carbapenem antibiotic, has favourable pharmacokinetic properties and is not hydrolysed by dehydropeptidase I [12].
  • Doripenem caused no changes in the EEG and behavior in rats at 400mg/kg [16].
  • The concentrations of doripenem in plasma, urine and tissue samples were determined by bioassay [14].

References

  1. Doripenem versus Pseudomonas aeruginosa in vitro: activity against characterized isolates, mutants, and transconjugants and resistance selection potential. Mushtaq, S., Ge, Y., Livermore, D.M. Antimicrob. Agents Chemother. (2004) [Pubmed]
  2. Comparative activities of doripenem versus isolates, mutants, and transconjugants of Enterobacteriaceae and Acinetobacter spp. with characterized beta-lactamases. Mushtaq, S., Ge, Y., Livermore, D.M. Antimicrob. Agents Chemother. (2004) [Pubmed]
  3. In vitro activity of doripenem against Pseudomonas aeruginosa and Burkholderia cepacia isolates from both cystic fibrosis and non-cystic fibrosis patients. Traczewski, M.M., Brown, S.D. Antimicrob. Agents Chemother. (2006) [Pubmed]
  4. In vitro activity of doripenem (S-4661) against multidrug-resistant gram-negative bacilli isolated from patients with cystic fibrosis. Chen, Y., Garber, E., Zhao, Q., Ge, Y., Wikler, M.A., Kaniga, K., Saiman, L. Antimicrob. Agents Chemother. (2005) [Pubmed]
  5. In vitro and in vivo antibacterial activities of S-4661, a new carbapenem. Tsuji, M., Ishii, Y., Ohno, A., Miyazaki, S., Yamaguchi, K. Antimicrob. Agents Chemother. (1998) [Pubmed]
  6. Comparative in vitro antimicrobial activity of a new carbapenem, doripenem: tentative disc diffusion criteria and quality control. Brown, S.D., Traczewski, M.M. J. Antimicrob. Chemother. (2005) [Pubmed]
  7. Application of logistic growth model to pharmacodynamic analysis of in vitro bactericidal kinetics. Yano, Y., Oguma, T., Nagata, H., Sasaki, S. Journal of pharmaceutical sciences. (1998) [Pubmed]
  8. Comparative activity of doripenem and three other carbapenems tested against Gram-negative bacilli with various beta-lactamase resistance mechanisms. Jones, R.N., Sader, H.S., Fritsche, T.R. Diagn. Microbiol. Infect. Dis. (2005) [Pubmed]
  9. Delayed resistance selection for doripenem when passaging Pseudomonas aeruginosa isolates with doripenem plus an aminoglycoside. Huynh, H.K., Biedenbach, D.J., Jones, R.N. Diagn. Microbiol. Infect. Dis. (2006) [Pubmed]
  10. Antimicrobial activity of doripenem (S-4661): a global surveillance report (2003). Fritsche, T.R., Stilwell, M.G., Jones, R.N. Clin. Microbiol. Infect. (2005) [Pubmed]
  11. Doripenem. Anderson, D.L. Drugs of today (Barcelona, Spain : 1998) (2006) [Pubmed]
  12. In vitro and in vivo antibacterial activities of a new injectable carbapenem, S-4661, against gynaecological pathogens. Mikamo, H., Izumi, K., Hua, Y.X., Hayasaki, Y., Sato, Y., Tamaya, T. J. Antimicrob. Chemother. (2000) [Pubmed]
  13. A novel 1 beta-methylcarbapenem antibiotic, S-4661. Synthesis and structure-activity relationships of 2-(5-substituted pyrrolidin-3-ylthio)-1 beta-methylcarbapenems. Iso, Y., Irie, T., Nishino, Y., Motokawa, K., Nishitani, Y. J. Antibiot. (1996) [Pubmed]
  14. Pharmacokinetics and tissue penetration of a new carbapenem, doripenem, intravenously administered to laboratory animals. Hori, T., Nakano, M., Kimura, Y., Murakami, K. In Vivo (2006) [Pubmed]
  15. In vitro antibacterial activity of S-4661, a new parenteral carbapenem, against urological pathogens isolated from patients with complicated urinary tract infections. Nomura, S., Nagayama, A. Journal of chemotherapy (Florence, Italy) (2002) [Pubmed]
  16. Absence of convulsive liability of doripenem, a new carbapenem antibiotic, in comparison with beta-lactam antibiotics. Horiuchi, M., Kimura, M., Tokumura, M., Hasebe, N., Arai, T., Abe, K. Toxicology (2006) [Pubmed]
  17. Study of the synergism between carbapenems and vancomycin or teicoplanin against MRSA, focusing on S-4661, a carbapenem newly developed in Japan. Kobayashi, Y. J. Infect. Chemother. (2005) [Pubmed]
 
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