Tedizolid for the management of human infections: In vitro characteristics

Clinical Infectious Diseases

Volumn 58, Issue SUPPL. 1, 2014, Pages

  Locke, Jeffrey B ^a   Zurenko, Gary E ^b   Shaw, Karen Joy ^a   Bartizal, Kenneth ^a  

^a Cubist Pharmaceuticals   (United States)

^b ZML Consulting LLC   (United States)

Author keywords

cfr; MRSA; oxazolidinone; resistance; tedizolid

Indexed keywords

LINEZOLID; METHYLTRANSFERASE; RIBOSOME PROTEIN; RNA 23S; TEDIZOLID;

ANTIBIOTIC RESISTANCE; ANTIBIOTIC SENSITIVITY; ANTIMICROBIAL ACTIVITY; ARTICLE; BACTERIAL MUTATION; BACTERIAL STRAIN; DRUG POTENCY; HUMAN; IN VITRO STUDY; INFECTION; METHYLATION; NONHUMAN; PATHOGENESIS; PRACTICE GUIDELINE; PRIORITY JOURNAL; PROTEIN SYNTHESIS INHIBITION; QUALITY CONTROL; RIBOSOME SUBUNIT; STAPHYLOCOCCUS AUREUS;

CFR; MRSA; OXAZOLIDINONE; RESISTANCE; TEDIZOLID;

ACETAMIDES; ANTI-BACTERIAL AGENTS; DRUG RESISTANCE, BACTERIAL; GENE TRANSFER, HORIZONTAL; HUMANS; ORGANOPHOSPHATES; OXAZOLES; OXAZOLIDINONES; POINT MUTATION; RIBOSOMAL PROTEINS; RNA, RIBOSOMAL, 23S; STAPHYLOCOCCAL INFECTIONS; STAPHYLOCOCCUS AUREUS; TRNA METHYLTRANSFERASES;

EID: 84892147772     PISSN: 10584838     EISSN: 15376591     Source Type: Journal    
DOI: 10.1093/cid/cit616     Document Type: Article

References (47)

1. Moellering RC Jr. MRSA: The first half century. J Antimicrob Chemother 2012; 67:4-11
2. Gould IM, Cauda R, Esposito S, Gudiol F, Mazzei T, Garau J. Management of serious meticillin-resistant Staphylococcus aureus infections: What are the limits? Int J Antimicrob Agents 2011; 37:202-9
3. Bush K. Improving known classes of antibiotics: An optimistic approach for the future. Curr Opin Pharmacol 2012; 12:527-34
4. McCusker KP, Fujimori DG. The chemistry of peptidyltransferase center-targeted antibiotics: Enzymatic resistance and approaches to countering resistance. ACS Chem Biol 2012; 7:64-72
5. Kanafani ZA, Corey GR. Tedizolid (TR-701): A new oxazolidinone with enhanced potency. Expert Opin Investig Drugs 2012; 21:515-22
6. Shaw KJ, Barbachyn MR. The oxazolidinones: Past, present, and future. Ann N Y Acad Sci 2011; 1241:48-70
7. Im WB, Choi SH, Park JY, Choi SH, Finn J, Yoon SH. Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent. Eur J Med Chem 2011; 46:1027-39
8. Prokocimer P, De Anda C, Fang E, Mehra P, Das A. Tedizolid phosphate vs linezolid for treatment of acute bacterial skin and skin structure infections: The ESTABLISH-1 randomized trial. JAMA 2013; 309:559-69
9. Fang E, De Anda C, Das A, Prokocimer P. Efficacy and safety results from the ESTABLISH 2 ABSSSI study comparing IV and oral tedizolid phosphate and linezolid. Poster presented at: 23rd European Congress of Clinical Microbiology and Infectious Diseases (ECCMID); 27-30April, 2013; Berlin, Germany
10. ClinTrials.gov. Pulmonary disposition of TR-700 following once-daily oral 200 mg. Available at: Http://www.clinicaltrials.gov/ct2/show/ NCT01271998. Accessed 23 October 2012
11. Locke JB, Finn J, Hilgers M, et al. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother 2010; 54:5337-43
12. Choi S, Im W, Rhee J. The new oxazolidinone, TR-700 (DA-7157): Effects of pH, inoculum, serum and media on antibacterial activity. Presented at: 47th Interscience Conference on Antimicrobial Agents and Chemotherapy; 17-20 September 2007; Chicago, IL. Poster F1-1690
13. Cunningham ML, Kwan BP, Nelson KJ, Bensen DC, Shaw KJ. Distinguishing on-target versus off-target activity in early antibacterial drug discovery using a macromolecular synthesis assay. J Biomol Screen 2013; 18:1018-26
14. Yum JH, Choi SH, Yong D, et al. Comparative in vitro activities of torezolid (DA-7157) against clinical isolates of aerobic and anaerobic bacteria in South Korea. Antimicrob Agents Chemother 2010; 54:5381-6
15. Schaadt R, Sweeney D, Shinabarger D, Zurenko G. In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent. Antimicrob Agents Chemother 2009; 53:3236-9
16. Brown SD, Traczewski MM. Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges. Antimicrob Agents Chemother 2010; 54:2063-9
17. Lemaire S, Van Bambeke F, Appelbaum PC, Tulkens PM. Cellular pharmacokinetics and intracellular activity of torezolid (TR-700): Studies with human macrophage (THP-1) and endothelial (HUVEC)cell lines. J Antimicrob Chemother 2009; 64:1035-43
18. Vera-Cabrera L, Espinoza-González NA, Welsh O, Ocampo-Candiani JCastro-Garza J. Activity of novel oxazolidinones against Nocardia brasiliensis growing within THP-1 macrophages. J Antimicrob Chemother 2009; 64:1013-7
19. Housman ST, Pope JS, Russomanno J, et al. Pulmonary disposition of tedizolid following administration of once-daily oral 200-milligram tedizolid phosphate in healthy adult volunteers. Antimicrob Agents Chemother 2012; 56:2627-34
20. Das D, Lambert A, Tulkens PM, Muccioli GG, Van Bambeke F. Study of the cellular uptake and subcellular distribution of the oxazolidinone tedizolid (TZD) in murine J774 macrophages: Lack of association with mitochondria. Presented at: 52nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 9-12 September 2012; San Francisco, CA. Poster A-1291
21. Leach KL, Swaney SM, Colca JR, et al. The site of action of oxazolidinone antibiotics in living bacteria and in human mitochondria. Mol Cell 2007; 26:393-402
22. Zurenko G, Todd WM, Hafkin BA, Myers B, Kaufman C, Bock J. Development of linezolid-resistant Enterococcus faecium in two compassionate use program patients treated with linezolid [abstract 848]. In: Program and abstracts of the 39th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 1999:118
23. Tsiodras S, Gold HS, Sakoulas G, et al. Linezolid resistance in a clinical isolate of Staphylococcus aureus. Lancet 2001; 358:207-8
24. Gonzales RD, Schreckenberger PC, Graham MB, Kelkar S, Denbesten Kquinn JP. Infections due to vancomycin-resistant Enterococcus faecium resistant to linezolid. Lancet 2001; 357:1179
25. Long KS, Vester B. Resistance to linezolid caused by modifications at its binding site on the ribosome. Antimicrob Agents Chemother 2012; 56:603-12
26. Flamm RK, Farrell DJ, Mendes RE, Ross JE, Sader HS, Jones RN. LEADER Surveillance program results for 2010: An activity and spectrum analysis of linezolid using 6801 clinical isolates from the United States (61 medical centers). Diagn Microbiol Infect Dis 2012; 74:54-61
27. Gu B, Kelesidis T, Tsiodras S, Hindler J, Humphries RM. The emerging problem of linezolid-resistant Staphylococcus. J Antimicrob Chemother 2013; 68:4-11
28. Livermore DM, Mushtaq S,Warner M,Woodford N. Activity of oxazolidinone TR-700 against linezolid-susceptible and -resistant staphylococci and enterococci. J Antimicrob Chemother 2009; 63:713-5
29. Quiles-Melero I, García-Perea A, de Pablos M, Gómez-Gil R, Mingorance J. Resistance to linezolid in a methicillin-susceptible Staphylococcus aureus clinical isolate without previous exposure to oxazolidinones. Int J Med Microbiol 2012; 302:145-7
30. Locke JB, Hilgers M, Shaw KJ. Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin. Antimicrob Agents Chemother 2009; 53:5275-8
31. Schwarz S, Werckenthin C, Kehrenberg C. Identification of a plasmidborne chloramphenicol-florfenicol resistance gene in Staphylococcus sciuri. Antimicrob Agents Chemother 2000; 44:2530-3
32. Toh SM, Xiong L, Arias CA, et al. Acquisition of a natural resistance gene renders a clinical strain of methicillin-resistant Staphylococcus aureus resistant to the synthetic antibiotic linezolid. Mol Microbiol 2007; 64:1506-14
33. Locke JB, Rahawi S, LaMarre J, Mankin AS, Shaw KJ. Genetic environment and stability of cfr in methicillin-resistant Staphylococcus aureus CM05. Antimicrob Agents Chemother 2012; 56:332-40
34. Locke JB, Zuill DE, Sahm DF, Dean J, Denys GA, Shaw KJ. Identification and characterization of linezolid-resistant Staphylococcus aureus 3133832, the first known clinical isolate possessing the cfr multidrug resistance gene. Presented at: 23rd European Congress of Clinical Microbiology and Infectious Diseases (ECCMID); 27-30 April 2013; Berlin, Germany. O449
35. LaMarre JM, Locke JB, Shaw KJ, Mankin AS. Low fitness cost of the multidrug resistance gene cfr. Antimicrob Agents Chemother 2011; 55:3714-9
36. Smith LK, Mankin AS. Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors. Antimicrob Agents Chemother 2008; 52:1703-12
37. Shaw KJ, Poppe S, Schaadt R, et al. In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains. Antimicrob Agents Chemother 2008; 52:4442-7
38. Locke JB, Hilgers M, Shaw KJ. Novel ribosomal mutations in Staphylococcus aureus strains identified through selection with the oxazolidinones linezolid and torezolid (TR-700). Antimicrob Agents Chemother 2009; 53:5265-74
39. Betriu C, Morales G, Rodríguez-Avial I, et al. Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain. Antimicrob Agents Chemother 2010; 54:2212-5
40. Jones RN, Moet GJ, Sader HS, Mendes RE, Castanheira M. TR-700 in vitro activity against and resistance mutation frequencies among Grampositive pathogens. J Antimicrob Chemother 2009; 63:716-20
41. Locke JB, Morales G, Hilgers M, et al. Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with cooccurring mutations in ribosomal protein L3. Antimicrob Agents Chemother 2010; 54:5352-5
42. Cercenado E, Marín M, Gama B, Iglesias C, Bouza E. In vitro activity of tedizolid and radezolid against linezolid-resistant Gram-positive clinical isolates with genetically characterized resistance mechanisms. Presented at: 52nd Interscience Conference on Antimicrobial Agents and Chemotherapy; 9-12 September 2012; San Francisco, CA. Poster C2-142
43. Prokocimer P, Bien P, DeAnda C, Pillar CM, Bartizal K. In vitro activity and microbiological efficacy of tedizolid (TR-700) against Grampositive clinical isolates from a phase 2 study of oral tedizolid phosphate (TR-701) in patients with complicated skin and skin structure infections. Antimicrob Agents Chemother 2012; 56:4608-13
44. Clinical and Laboratory Standards Institute (CLSI). Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically; Approved Standard, 9th ed. Wayne, PA: Clinical and Laboratory Standards Institute, 2012
45. Clinical and Laboratory Standards Institute (CLSI). Performance Standards for Antimicrobial Disk Susceptibility Tests, Approved Standard, 11th ed.Wayne, PA: Clinical and Laboratory Standards Institute, 2012
46. Clinical and Laboratory Standards Institute (CLSI). Development of In Vitro Susceptibility Testing Criteria and Quality Control Parameters; Approved Guideline, 3rd ed. Wayne, PA: Clinical and Laboratory Standards Institute, 2012
47. Clinical and Laboratory Standards Institute. Performance Standards for Antimicrobial Susceptibility Testing, 22nd Informational Supplement. Wayne, PA: Clinical and Laboratory Standards Institute, 2012