Tigecycline: First class glycylcycline. a new choice for empiric therapy

Drug Discovery Today: Therapeutic Strategies

Volumn 3, Issue 2, 2006, Pages 137-144

  Jones, C Hal ^a   Petersen, Peter J ^a  

^a WYETH RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AZTREONAM; CEFEPIME; CEFTAZIDIME; CEFTOBIPROLE; CILASTATIN PLUS IMIPENEM; DALFOPRISTIN PLUS QUINUPRISTIN; DAPTOMYCIN; GLYCYLCYCLINE DERIVATIVE; IMIPENEM; LEVOFLOXACIN; LINEZOLID; MINOCYCLINE; PIPERACILLIN PLUS TAZOBACTAM; PRIMAXIM; TETRACYCLINE; TIGECYCLINE; VANCOMYCIN;

ABDOMINAL INFECTION; ANTIBACTERIAL ACTIVITY; ANTIBIOTIC RESISTANCE; ANTIBIOTIC SENSITIVITY; AREA UNDER THE CURVE; CLINICAL TRIAL; DIARRHEA; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG CHOICE; DRUG CLEARANCE; DRUG CONTRAINDICATION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; ESCHERICHIA COLI; FOOD AND DRUG ADMINISTRATION; GASTROINTESTINAL DISEASE; GASTROINTESTINAL SYMPTOM; HUMAN; IC 50; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; MINIMUM INHIBITORY CONCENTRATION; NAUSEA; NONHUMAN; NUCLEOTIDE SEQUENCE; REVIEW; SINGLE DRUG DOSE; SKIN INFECTION; STREPTOCOCCUS PNEUMONIAE; VOMITING;

EID: 33746816592     PISSN: 17406773     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ddstr.2006.06.009     Document Type: Review

References (40)

1. Projan S.J. Why is big pharma getting out of antibacterial drug discovery?. Curr. Opin. Microbiol. 6 (2003) 427-430
2. Weber J.T. Community-associated methicillin-resistant Staphylococcus aureus. Clin. Infect. Dis. 41 (2005) S269-S272
3. Jones C.H., and Petersen P.J. Tigecycline: a review of preclinical and clinical studies of the first-in-class glycylcycline antibiotic. Drugs Today Barc. 41 (2005) 637-659
4. Tenover F.C., et al. Vancomycin-resistant Staphylococcus aureus isolate from a patient in Pennsylvania. Antimicrob. Agents Chemother. 48 (2004) 275-280
5. Hujer K.M., et al. Identification of a new allelic variant of the Acinetobacter baumannii cephalosporinase, ADC-7 beta-lactamase: defining a unique family of class C enzymes. Antimicrob. Agents Chemother. 49 (2005) 2941-2948
6. Bratu S., et al. Rapid spread of carbapenem-resistant Klebsiella pneumoniae in New York City: a new threat to our antibiotic armamentarium. Arch. Intern. Med. 165 (2005) 1430-1435
7. Dowzicky M., et al. Characterization of isolates associated with emerging resistance to quinupristin/dalfopristin (Synercid) during a worldwide clinical program. Diagn. Microbiol. Infect. Dis. 37 (2000) 57-62
8. Pillai S.K., et al. Linezolid resistance in Staphylococcus aureus: characterization and stability of resistant phenotype. J. Infect. Dis. 186 (2002) 1603-1607
9. Mangili A., et al. Daptomycin-resistant, methicillin-resistant Staphylococcus aureus bacteremia. Clin. Infect. Dis. 40 (2005) 1058-1060
10. Roberts M.C. Tetracycline therapy: update. Clin. Infect Dis. 36 (2003) 462-467
11. Sum P.-E., and Petersen P. Synthesis and structure-activity relationship of novel glycylcycline derivatives leading to the discovery of GAR-936. Bioorg. Med. Chem. Lett. 9 (1999) 1459-1462
12. Petersen P.J., et al. In vitro and in vivo antimicrobial activities of a novel glycylcycline, the 9-t-butylglycylamido derivative of minocycline (GAR-936). Antimicrob. Agents Chemother. 43 (1999) 738-744
13. Bradford P.A., et al. In vitro activity of tigecycline against isolates from patients enrolled in phase 3 clinical trials for complicated skin and skin structure infections and complicated intra-abdominal infections. Clin. Infect. Dis. 41 (2005) S315-S332
14. Hoban D., et al. In vitro activity of tigecycline against 6792 gram-negative and gram-positive clinical isolates from the global tigecycline evaluation and surveillance trial (TEST Program 2004). Diagn. Microbiol. Infect. Dis. 52 (2005) 215-227
15. Jones C.H., et al. Diagnostic PCR analysis of the occurrence of methicillin and tetracycline Resistance genes among Staphylococcus aureus isolates from phase 3 clinical trials of tigecycline for complicated skin and skin structure infections. Antimicrob. Agents Chemother. 50 (2006) 505-510
16. Rasmussen B.A., et al. Inhibition of protein synthesis occurring on tetracycline-resistant, tet-m protected ribosomes by a novel class of tetracyclines, the glycylcyclines. Antimicrob. Agents Chemother. 38 (1994) 1658-1660
17. Bergeron J., et al. Glycylcyclines bind to the high-affinity tetracycline ribosomal binding site and evade Tet(M)- and Tet(O)-mediated ribosomal protection. Antimicrob. Agents Chemother. 40 (1996) 2226-2228
18. Olson M.W., et al. Functional, biophysical and structural basis for antibacterial activity of tigecycline. Antimicrob. Agents Chemother. 50 (2006) 2156-2166
19. Bauer G., et al. Comparison of tetracycline and tigecycline binding to ribosomes mapped by dimethylsulphate and drug-directed Fe2+ cleavage of 16S rRNA. J. Antimicrob. Chemother. 53 (2004) 592-599
20. Bradford P.A., et al. Tigecycline MIC testing by broth dilution requires use of fresh medium or addition of the biocatalytic oxygen-reducing reagent oxyrase to standardize the test method. Antimicrob. Agents Chemother. 49 (2005) 3903-3909
21. Petersen P.J., and Bradford P.A. Effect of medium age and supplementation with the biocatalytic oxygen-reducing reagent oxyrase on in vitro activities of tigecycline against recent clinical isolates. Antimicrob. Agents Chemother. 49 (2005) 3910-3918
22. CLSI, Performance standards for antimicrobial susceptibility testing: M100-S15, Fifteenth informational supplement. Clinical Laboratory Standards Institute, Wayne, PA. Vol. 25. 2005.
23. Labthavikul P., et al. In vitro activity of tigecycline against Staphylococcus epidermidis growing in an adherent-cell biofilm model. Antimicrob. Agents Chemother. 47 (2003) 3967-3969
24. Babinchak T., et al. The efficacy and safety of tigecycline in the treatment of complicated intra-abdominal infections: analysis of pooled clinical trial data. Clin. Infect. Dis. 41 Suppl. 5 (2005) S354-S367
25. Dean C.R., et al. Efflux-mediated resistance to tigecycline (GAR-936) in Pseudomonas aeruginosa PAO1. Antimicrob. Agents Chemother. 47 (2003) 972-978
26. Zhanel G.G., et al. Antimicrobial resistance in respiratory tract Streptococcus pneumoniae isolates: results of the Canadian respiratory organism susceptibility study, 1997 to 2002. Antimicrob. Agents Chemother. 47 (2003) 1867-1874
27. McAleese F., et al. A novel MATE family efflux pump contributes to the reduced susceptibility of laboratory-derived Staphylococcus aureus mutants to tigecycline. Antimicrob. Agents Chemother. 49 (2005) 1865-1871
28. Visalli M.A., et al. AcrAB multidrug efflux pump is associated with reduced levels of susceptibility to tigecycline (GAR-936) in Proteus mirabilis. Antimicrob. Agents Chemother. 47 (2003) 665-669
29. Ruzin A., et al. AcrAB efflux pump plays a role in decreased susceptibility to tigecycline in Morganella morganii. Antimicrob. Agents Chemother. 49 (2005) 791-793
30. Poole K. Efflux-mediated multiresistance in gram-negative bacteria. Clin. Microbiol. Infect. 10 (2004) 12-26
31. Ruzin, A. et al. (2004) AcrAB efflux-mediated decreased susceptibility to tigecycline in Enterobacter spp. Interscience Conference on Antimicrobial Agents and Chemotherapy, ASM Press
32. Ruzin A., et al. Influence of transcriptional activator RamA on expression of multidrug efflux pump AcrAB and tigecycline susceptibility in Klebsiella pneumoniae. Antimicrob. Agents Chemother. 49 (2005) 1017-1022
33. Meagher A.K., et al. Pharmacokinetic/pharmacodynamic profile for tigecycline - a new glycylcycline antimicrobial agent. Diagn. Microbiol. Infect. Dis. 52 (2005) 165-171 (part of DMID symposium section)
34. Conte Jr. J.E., et al. Steady-state serum and intrapulmonary pharmacokinetics and pharmacodynamics of tigecycline. Int. J. Antimicrob. Agents. 25 (2005) 523-529
35. Van Ogtrop M.L., et al. In vivo pharmacodynamic activities of two glycylcyclines (GAR-936 and WAY 152, 288) against various gram-positive and gram-negative bacteria. Antimicrob. Agents Chemother. 44 (2000) 943-949
36. Lefort A., et al. Activity and diffusion of tigecycline (GAR-936) in experimental enterococcal endocarditis. Antimicrob. Agents Chemother. 47 (2003) 216-222
37. McDonald P.J., et al. Persistent effect of antibiotics on Staphylococcus aureus after exposure for limited periods of time. J. Inf. Dis. 135 (1977) 217-223
38. Ellis-Grosse E., et al. The efficacy and safety of tigecycline in the treatment of skin and skin structure infections: results of two double-blind phase 3 comparison studies with vancomycin/aztreonam. Clin. Infect. Dis. 41 (2005) S341-S353
39. Bosso J.A. The antimicrobial armamentarium: evaluating current and future treatment options. Pharmacotherapy 25 10 Pt 2 (2005) 55S-62S
40. Green S.L., et al. Linezolid and reversible myelosuppression. JAMA 285 (2001) 1291