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1135871-27-0

1135871-27-0 structure
1135871-27-0 structure
  • Name: Tigecycline mesylate
  • Chemical Name: Tigecycline mesylate
  • CAS Number: 1135871-27-0
  • Molecular Formula: C30H43N5O11S
  • Molecular Weight: 681.754
  • Catalog: Signaling Pathways Anti-infection Bacterial
  • Create Date: 2018-03-26 00:16:02
  • Modify Date: 2024-01-11 12:49:03
  • Tigecycline mesylate a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline mesylate is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline mesylate has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline mesylate has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline mesylate appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline mesylate for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline mesylate was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline mesylate dose [3].Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infectionFDA Approved Date: June 17, 2005 Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache

Name Tigecycline mesylate
Synonyms 2-Naphthacenecarboxamide, 4,7-bis(dimethylamino)-9-[[2-[(1,1-dimethylethyl)amino]acetyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-, (4S,4aS,5aR,12aS)-, methanesulfonate (1:1) (salt)
(4S,4aS,5aR,12aS)-4,7-Bis(dimethylamino)-3,10,12,12a-tetrahydroxy-9-{[N-(2-methyl-2-propanyl)glycyl]amino}-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-2-tetracenecarboxamide methanesulfonate (1:1)
Description Tigecycline mesylate a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline mesylate is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline mesylate has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline mesylate has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline mesylate appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline mesylate for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline mesylate was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline mesylate dose [3].Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infectionFDA Approved Date: June 17, 2005 Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
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References

[1]. Seputiene V, et al. Tigecycline - how powerful is it in the fight against antibiotic-resistant bacteria? Medicina (Kaunas). 2010;46(4):240-8.

[2]. Bhattacharya M, et al. Tigecycline. J Postgrad Med. 2009 Jan-Mar;55(1):65-8.

[3]. Moreno BB, et al. Tigecycline therapy for infections due to carbapenemase-producing Klebsiella pneumoniae in critically ill patients. Scand J Infect Dis. 2013 Dec 20.

Molecular Formula C30H43N5O11S
Molecular Weight 681.754
Exact Mass 681.268005
Storage condition 2-8℃