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Articles

A Review of Tigecycline

References

  • Chopra I.Roberts M. Tetracycline antibiotics: mode of ac-tion, applications, molecular biology, and epidemiology of bac-terial resistance. Microbiol. Mol. Biol. Rev. 2001; 65: 232–260.
  • Poole K. Efflux-mediated antimicrobial resistance. J An-timicrob Chemother 2005; 56: 20–51.
  • Paulsen IT, Brown MH.Skurray RA. Proton-dependent multidrug efflux systems. Microbiol Rev 1996; 60: 575–608.
  • Bolhuis H, van Veen HW, Poolman Bet al. Mechanisms of multidrug transporters. FEMS Microbiol Rev 1997; 21: 55–84.
  • Kumar A.Schweizer HP. Bacterial resistance to antibiotics: active efflux and reduced uptake. Adv Drug Deliv Rev 2005; 57: 1486–1513.
  • Hooper DC. Efflux pumps and nosocomial antibiotic re-sistance: a primer for hospital epidemiologists. Clin Infect Dis 2005; 40: 1811–1817.
  • Hillen W.Berens C. Mechanisms underlying expression of Tn10 encoded tetracycline resistance. Annu Rev Microbiol 1994; 48: 345–369.
  • Levy SB (1984). Resistance to the tetracyclines. In Antimi-crobial drug resistance. (Bryan, L. E., Ed). Academic Press, Orlando, Fl.
  • Okusu H, Ma D.Nikaido H. AcrAB efflux pump plays a major role in the antibiotic resistance phenotype of Escherichia coli multiple-antibiotic-resistance (Mar) mutants. J Bacteriol 1996; 178: 306–308.
  • Poole K, Krebes K, McNally C et al. Multiple antibiotic re-sistance in Pseudomonas aeruginosa: evidence for involvement of an efflux operon. J Bacteriol 1993; 175: 7363–7372.
  • Masuda N, Sakagawa E, Ohya S et al. Substrate specifici-ties of MexAB-OprM, MexCD-OprJ, and MexXY-oprM efflux pumps in Pseudomonas aeruginosa. Antimicrob Agents Chemother 2000; 44: 3322–3327.
  • Chuanchuen R, Beinlich K, Hoang TT et al. Cross-resis-tance between triclosan and antibiotics in Pseudomonas aerug-inosa is mediated by multidrug efflux pumps: exposure of a susceptible mutant strain to triclosan selects nfxB mutants over-expressing MexCD-OprJ. Antimicrob Agents Chemother 2001; 45: 428–432.
  • Connell SR, Tracz DM, Nierhaus KH et al. Ribosomal pro-tection proteins and their mechanism of tetracycline resistance. Antimicrob Agents Chemother 2003; 47: 3675–3681.
  • Speer BS, Bedzyk L.Salyers AA. Evidence that a novel tetracycline resistance gene found on two Bacteroides trans-posons encodes an NADP-requiring oxidoreductase. J Bacteriol 1991; 173: 176–183.
  • Clewell DB, Flannagan SE.Jaworski DD. Unconstrained bacterial promiscuity: the Tn916-Tn1545 family of conjugative transposons. Trends Microbiol 1995; 3: 229–236.
  • Binet R.Maurelli AT. Fitness cost due to mutations in the 16S rRNA associated with spectinomycin resistance in Chlamy-dia psittaci 6BC. Antimicrob Agents Chemother 2005; 49: 4455–4464.
  • McOrist S. Obligate intracellular bacteria and antibiotic re-sistance. Trends Microbiol 2000; 8: 483–486.
  • Tally FT, Ellestad GA.Testa RT. Glycylcyclines: a new gen-eration of tetracyclines. J Antimicrob Chemother 1995; 35: 449–452.
  • Sum PE, Lee VJ, Testa RT et al. Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines. J Med Chem. 1994; 37: 184–188.
  • Sum PE, Petersen P. Synthesis and structure-activity rela-tionship of novel glycylcycline derivatives leading to the discovery of GAR-936. Bioorganic Med Chem Lett 1999; 9: 1459-1462.
  • Testa RT, Petersen PJ, Jacobus NV et al. In vitro and in vivo antibacterial activities of the glycylcyclines, a new class of semisynthetic tetracyclines. Antimicrob Agents Chemother1993; 37: 2270–2277.
  • Bauer G, Berens C, Projan SJ et al. Comparison of tetra-cycline and tigecycline binding to ribosomes mapped by di-methylsulphate and drug-directed Fe2+ cleavage of 16S rRNA. J Antimicrob Chemother 2004; 53: 592–599.
  • Bergeron J, Ammirati M, Danley D et al. Glycylcyclines bind to the high-affinity tetracycline ribosomal binding site and evade Tet(M)- and Tet(0)-mediated ribosomal protection. An-timicrob Agents Chemother 1996; 40: 2226–2228.
  • Rasmussen BA, Gluzman Y.Tally FP. Inhibition of protein synthesis occurring on tetracycline-resistant, TetM-protected ri-bosomes by a novel class of tetracyclines, the glycylcyclines. An-timicrob Agents Chemother. 1994; 38: 1658–1660.
  • Barden TC, Buckwalter BL, Testa RT et al. “Glycylcy-clines”. 3. 9-Aminodoxycyclinecarboxamides. J Med Chem 1994; 37: 3205–3211.
  • Orth P, Schnappinger D, Sum PE et al. Crystal structure of the tet repressor in complex with a novel tetracycline, 9-(N,N-dimethylglycylamido)- 6-demethyl-6-deoxy-tetracycline. J Mol Biol 1999; 285: 455–461.
  • Ruzin A, Keeney D, Bradford PA. AcrAB efflux pump plays a role in decreased susceptibility to tigecycline in Mor-ganella morganii. Antimicrob Agents Chemother 2005; 49: 791–793.
  • Dean CR, VisaIli MA, Projan SJ et al. Efflux-mediated re- sistance to tigecycline (GAR-936) in Pseudomonas aeruginosa PA01. Antimicrob Agents Chemother 2003; 47: 972–978.
  • (2006). Tigecycline - EUCAST clinical MIC breakpoints
  • (2006). Tygacil (tigecycline): package insert.
  • Petersen PJ, Bradford PA. Effect of medium age and sup-plementation with the biocatalytic oxygen-reducing reagent oxyrase on in vitro activities of tigecycline against recent clinical isolates. Antimicrob Agents Chemother 2005; 49: 3910–3918.
  • Bradford PA, Petersen PJ, Young Metal. Tigecycline MIC testing by broth dilution requires use of fresh medium or addition of the biocatalytic oxygen-reducing reagent oxyrase to standard-ize the test method. Antimicrob Agents Chemother 2005; 49: 3903–3909.
  • Brown SD.Traczewski MM. Comparative in vitro antimi-crobial activity of tigecycline, a new glycylcycline compound, in freshly prepared medium and quality control. J Clin Microbiol 2007; 45: 2173–2179.
  • Gales AC, Jones RN. Antimicrobial activity and spectrum of the new glycylcycline, GAR-936 tested against 1,203 recent clinical bacterial isolates. Diagn Microbiol Infect Dis 2000; 36: 19–36.
  • Ruzin A, Visalli MA, Keeney D et al. Influence of tran-scriptional activator RamA on expression of multidrug efflux pump AcrAB and tigecycline susceptibility in Klebsiella pneu-moniae. Antimicrob Agents Chemother 2005; 49: 1017–1022.
  • Visalli MA, Murphy E, Projan SJ et al. AcrAB multidrug ef-flux pump is associated with reduced levels of susceptibility to tigecycline (GAR-936) in Proteus mirabilis. Antimicrob Agents Chemother 2003; 47: 665–669.
  • Boucher HW, Wennersten CB.Eliopoulos GM. In vitro ac-tivities of the glycylcycline GAR-936 against Gram-positive bac-teria. Antimicrob Agents Chemother 2000; 44: 2225–2229.
  • Gales A, Jones R, Pfaller M. Two-year assessment of the pathogen frequency and antimicrobial resistance patterns among organisms isolated from skin and soft tissue infections in Latin American hospitals: results from the SENTRY antimicrobial sur-veillance program, 1997-98. SENTRY Study Group. Int J Infect Dis 2000; 4.
  • Bradford PA. Tigecycline: a first in class glycylcycline. Clin Microiol News 2004; 26: 163–168.
  • Projan SJ. Preclinical pharmacology of GAR-936, a novel glycylcycline antibacterial agent. Pharmacotherapy 2000; 20: 219S-223S; discussion 224S-228S.
  • Betriu C, Rodriguez-Avial I, Sanchez BA et al. In vitro ac-tivities of tigecycline (GAR-936) against recently isolated clinical bacteria in Spain. Antimicrob Agents Chemother. 2002; 46: 892–895.
  • Betriu C, Rodriguez-Avial I, Sanchez BA et al. Compara-tive in vitro activities of tigecycline (GAR-936) and other antimi-crobial agents against Stenotrophomonas maltophilia. J Antimicrob Chemother 2002; 50: 758–759.
  • Biedenbach DJ, Beach ML, Jones RN. In vitro antimi-crobial activity of GAR-936 tested against antibiotic-resistant Gram-positive blood stream infection isolates and strains pro-ducing extended-spectrum beta-lactamases. Diagn Microbiol In-fect Dis 2001; 40: 173–177.
  • Edlund C, Nord CE. In-vitro susceptibility of anaerobic bacteria to GAR-936, a new glycylcycline. Clin Microbiol Infect 2000; 6: 159–163.
  • Goldstein EJC, Citron DM, Merriam CV et al. Compara-tive in vitro activities of GAR-936 against aerobic and anaerobic animal and human bite wound pathogens. Antimicrob Agents Chemother 2000; 44: 2747–2751.
  • Henwood CJ, Gatward T, Warner M et al. Antibiotic re-sistance among clinical isolates of Acinetobacter in the UK, and in vitro evaluation of tigecycline (GAR-936). J Antimicrob Chemother 2002; 49: 479–487.
  • Mercier R-C, Kennedy C.Meadows C. Antimicrobial ac-tivity of tigecycline (GAR-936) against Enterococcus faecium and Staphylococcus aureus used alone and in combination. Pharmacotherapy 2002; 22: 1517–1523.
  • Milatovic D, Schmitz F-J, Verhoef J et al. Activities of the glycylcycline tigecycline (GAR-936) against 1,924 recent Euro-pean clinical bacterial isolates. Antimicrob Agents Chemother 2003; 47: 400–404.
  • Petersen PJ, Bradford PA, Weiss WJ et al. In vitro and in vivo activities of tigecycline (GAR-936), daptomycin, and com-parative antimicrobial agents against glycopeptide-intermediate Staphylococcus aureus and other resistant Gram-positive pathogens. Antimicrob Agents Chemother 2002; 46: 2595–2601.
  • Petersen PJ, Jacobus NV, Weiss WJ et al. In vitro and in vivo antibacterial activities of a novel glycylcycline, the 9-t-butylglycylamido derivative of minocycline (GAR-936). Antimi-crob Agents Chemother 1999; 43: 738–744.
  • Rhomberg PR, Jones RN. In vitro activity of 11 antimi-crobial agents, including gatifloxacin and GAR936, tested against clinical isolates of Mycobacterium marin um. Diagn Microbiol In-fect Dis 2002; 42: 145–147.
  • Roblin PM, Hammerschlag MR. In vitro activity of GAR-936 against Chlamydia pneumoniae and Chlamydia tra-chomatis. Int J Antimicrob Agents 2000; 16: 61–63.
  • Cercenado E, Cercenado S, Gomez JA, Souza E. In vitro activity of tigecycline (GAR-936), a novel glycylcycline, against vancomycin-resistant enterococci and staphylococci with dimin-ished susceptibility to glycopeptides. J Antimicrob Chemother 2003; 52: 138–139.
  • Zhanel GG, Palatnick L, Nichol KA et al. Antimicrobial re- si stance in Haemophilus influenzae and Moraxella catarrhalis respiratory tract isolates: results of the Canadian Respiratory Or-ganism Susceptibility Study, 1997 to 2002. Antimicrob Agents Chemother 2003; 47: 1875–1881.
  • Zhanel GG, Palatnick L, Nichol KA et al. Antimicrobial re-sistance in respiratory tract Streptococcus pneumoniae isolates: results of the Canadian Respiratory Organism Susceptibility Study, 1997 to 2002. Antimicrob Agents Chemother 2003; 47: 1867–1874.
  • Wallace Jr RJ, Brown-Elliot BA, Crist CJ et al. Compari-son of the in vitro activity of the glycylcycline tigecycline (for-merly GAR-936) with those of tetracycline, minocycline, and doxycycline against isolates of Nontuberculous mycobacteria. An-timicrob Agents Chemother 2002; 46: 3164–3167.
  • Hoellman DB, Pankuch GA, Jacobs MR et al. Antipneu-mococcal activity of GAR 936, a new glycylcycline, compared to those of nine other agents against penicillin susceptible and resistant pneumococci. Antimicrob Agents Chemother 2000; 44: 1085–1088.
  • Cercenado E, Cercenado S, Souza E. in vitro activities of tigecycline (GAR-936) and 12 other antimicrobial agents against 90 Eikenella corrodens clinical isolates. Antimicrob Agents Chemother 2003; 47: 2644–2645.
  • Keeney D, Ruzin A, Bradford PA. RamA, a transcriptional regulator, and AcrAB, an RND-type efflux pump, are associated with decreased susceptibility to tigecycline in Enterobacter cloa-cae. Microb Drug Resist 2007; 13: 1–6.
  • Navon-Venezia S, Leavitt A.Carmeli Y. High tigecycline resistance in multidrug-resistant Acinetobacter baumannii. J An-timicrob Chemother 2007; 59: 772–774.
  • Pachón-lbátiez ME, Jiménez-Mejias ME, Pichardo C et al. Activity of tigecycline (GAR-936) against Acinetobacter bau-mannii strains, including those resistant to imipenem. Antimi-crob Agents Chemother 2004; 48: 4479–4481.
  • Seifert H, Stefanik D, Wisplinghoff H. Comparative in vitro activities of tigecycline and 11 other antimicrobial agents against 215 epidemiologically defined multidrug-resistant Acine-tobacter baumannii isolates. J Antimicrob Chemother 2006; 58: 1099–1100.
  • Coelho JM, Turton JF, Kaufmann ME et al. Occurrence of carbapenem-resistant Acinetobacter baumannii clones at multi-ple hospitals in London and Southeast England. J Clin Microbiol 2006; 44: 3623–3627.
  • Lolans K, Rice TW, Munoz-Price LS et al. Multicity out-break of carbapenem-resistant Acinetobacter baumannii isolates producing the carbapenemase OXA-40. Antimicrob Agents Chemother 2006; 50: 2941–2945.
  • Bozdogan B, Esel D, Whitener C et al. Antibacterial sus-ceptibility of a vancomycin-resistant Staphylococcus aureus strain isolated at the Hershey Medical Center. J Antimicrob Chemother 2003; 52: 864–868.
  • Kenny GE, Cartwright FD. Susceptibilities of Mycoplasma hominis, M. pneumoniae, and Ureaplasma urealyticum to GAR-936, dalfopristin, dirithromycin, evernimicin, gatifloxacin, linezolid,moxifloxacin,quinupristin-dalfopristin,andtelithromycin compared to their susceptibilities to reference macrolides, tetracyclines, and quinolones. Antimicrob Agents Chemother 2001; 45: 2604–2608.
  • Edelstein PH, Weiss WJ, Edelstein MA. Activities of tige-cycline (GAR-936) against Legionella pneumophila in vitro and in guinea pigs with L. pneumophila pneumonia. Antimicrob Agents Chemother. 2003; 47: 533–540.
  • Ruzin A, Keeney D, Bradford PA. AdeABC multidrug ef-flux pump is associated with decreased susceptibility to tigecy-cline in Acinetobacter calcoaceticus-Acinetobacter baumannii complex. J Antimicrob Chemother 2007; 59: 1001–1004.
  • Keeney D, Ruzin A, McAleese F et al. MarA-mediated overexpression of the AcrAB efflux pump results in decreased susceptibility to tigecycline in Escherichia coli. J Antimicrob Chemother 2008; 61: 46–53.
  • Hirata T, Saito A, Nishino K et al. Effects of efflux trans-porter genes on susceptibility of Escherichia coli to tigecycline (GAR-936). Antimicrob Agents Chemother 2004; 48: 2179–2184.
  • Peleg AY, Potoski BA, Rea R et al. Acinetobacter bau-mannii bloodstream infection while receiving tigecycline: a cau-tionary report. J Antimicrob Chemother 2007; 59: 128–131.
  • Reid GE, Grim SA, Aldeza CA et al. Rapid development of Acinetobacter baumannii resistance to tigecycline. Pharma-cotherapy 2007; 27: 1198–1201.
  • Meagher AK, Ambrose PG, Grasela TH et al. Pharmaco-kinetic/pharmacodynamic profile for tigecycline-a new glycylcy-cline antimicrobial agent. Diagn Microbiol Infect Dis 2005; 52: 165–171.
  • Muralidharan G, Micalizzi M, Speth J et al. Pharmacoki-netics of tigecycline after single and multiple doses in healthy sub-jects. Antimicrob Agents Chemother 2005; 49: 220–229.
  • Hoffmann M, DeMaio W, Jordan RA et al. Metabolism, excretion, and pharmacokinetics of [14C]tigecycline, a first-in-class glycylcycline antibiotic, after intravenous infusion to healthy male subjects. Drug Metab Dispos 2007; 35: 1543–1553.
  • MacGowan AP. Tigecycline pharmacokinetic/pharmaco-dynamic update. J Antimicrob Chemother 2008; 62 Suppl 1: ill-16.
  • van Ogtrop ML, Andes D, Stamstad TJ et al. in vivo phar-macodynamic activities of two glycylcyclines (GAR-936 and WAY 152,288) against various Gram-positive and Gram-nega-tive bacteria. Antimicrob. Agents Chemother. 2000; 44: 943–949.
  • Conte JE, Jr., Golden JA, Kelly MG et al. Steady-state serum and intrapulmonary pharmacokinetics and pharmacody-namics of tigecycline. Int J Antimicrob Agents 2005; 25: 523–529.
  • Meagher AK, Passarell JA, Cirincione BB et al. Exposure-response analyses of tigecycline efficacy in patients with compli-cated skin and skin-structure infections. Antimicrob Agents Chemother 2007; 51: 1939–1945.
  • Babinchak T, Ellis-Grosse E, Dartois N et al. The efficacy and safety of tigecycline for the treatment of complicated intra-abdominal infections: analysis of pooled clinical trial data. Clin Infect Dis 2005; 41 Suppl 5: S354–367.
  • Ellis-Grosse EJ, Babinchak T, Dartois N et al. The efficacy and safety of tigecycline in the treatment of skin and skin-struc-ture infections: results of 2 double-blind phase 3 comparison studies with vancomycin-aztreonam. Clin Infect Dis 2005; 41 Suppl 5: S341-353.
  • Baines SD, Saxton K, Freeman J et al. Tigecycline does not induce proliferation or cytotoxin production by epidemic Clostridium difficile strains in a human gut model. J Antimicrob Chemother 2006; 58: 1062–1065.
  • Nord CE, Sillerstrom E, Wahlund E. Effect of tigecycline on normal oropharyngeal and intestinal microflora. Antimicrob Agents Chemother 2006; 50: 3375–3380.
  • Wilcox MH. Evidence for low risk of Clostridium difficile infection associated with tigecycline. Clin Microbiol Infect 2007; 13: 949–952.
  • Bergstrom CT, Lo M.Lipsitch M. Ecological theory sug-gests that antimicrobial cycling will not reduce antimicrobial re-sistance in hospitals. Proc Natl Acad Sci U S A 2004; 101: 13285–13290.
  • ji AJ, Saunders JP, Wadgaonkar ND et al. A novel an-tibiotic bone assay by liquid chromatography/tandem mass spec-trometry for quantitation of tigecycline in rat bone. J Pharm Biomed Anal 2007; 44: 970–979.

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