Oxazolidinones: A review

Drugs

Volumn 59, Issue 1, 2000, Pages 7-16

  Diekema, Daniel J ^a   Jones, Ronald N ^a  

^a UNIVERSITY OF IOWA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AZTREONAM; CHLORAMPHENICOL; CLINDAMYCIN; EPEREZOLID; GENTAMICIN; GLYCOPEPTIDE; LINCOMYCIN; LINEZOLID; OXAZOLIDINONE DERIVATIVE; STREPTOGRAMIN; VANCOMYCIN;

ANTIMICROBIAL ACTIVITY; BACTERIAL INFECTION; BACTERIOSTASIS; CLINICAL TRIAL; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG MECHANISM; DRUG TOLERABILITY; EXPERIMENTAL MODEL; GASTROINTESTINAL SYMPTOM; HEADACHE; HUMAN; IN VIVO STUDY; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; NONHUMAN; PHASE 3 CLINICAL TRIAL; PROTEIN SYNTHESIS INHIBITION; RASH; REVIEW; STREPTOCOCCUS PNEUMONIAE; STRUCTURE ANALYSIS;

BACTERIA (MICROORGANISMS); METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; POSIBACTERIA; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PNEUMONIAE;

EID: 0034058145     PISSN: 00126667     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003495-200059010-00002     Document Type: Review

References (68)

1. 1. Spink WW, Ferris V. Quantitative action of penicillin inhibitor from penicillin-resistant strains of staphylococci. Science 1945; 102: 221
2. 2. Panlilio AL, Culver DH, Gaynes RP, et al. Methicillin-resistant S. aureus in US hospitals, 1975-1991. Infect Control Hosp Epidemiol 1992; 13: 582-6
3. 3. Schwalbe RS, Stapleton JT, Gilligan PH. Emergence of vancomycin resistance in coagulase-negative staphylococci. N Engl J Med 1987; 316: 927-31
4. 4. Centers for Disease Control and Prevention. Update: Staphylococcus aureus with reduced susceptibility to vancomycin -United States, 1997. MMWR Morb Mortal Wkly Rep 1997; 46: 813-5
5. 5. Jones RN, Sader HS, Erwin ME, et al. Emerging multiply resistant enterococci among clinical isolates. I. Prevalence data from 97 medical center surveillance study in the United States. Diag Microbiol Infect Dis 1995; 21: 85-93
6. 6. Doern GV, Pfaller MA, Kugler K, et al. Prevalence of antimicrobial resistance among respiratory tract isolates of Streptococcus pneumoniae in North America: 1997 results from the SENTRY antimicrobial surveillance program. Clin Infect Dis 1998; 27: 764-8
7. 7. Bochud P, Calandra T, Francioli P. Bacteremia due to viridans streptococci in neutropenic patients: a review. Am J Med 1994; 97: 256-64
8. 8. Pfaller MA, Jones RN, Doern GV, et al. Bacterial pathogens isolated from patients with bloodstream infection: frequencies of occurrence and antimicrobial susceptibility patterns from the SENTRY antimicrobial surveillance program (United States and Canada, 1997). Antimicrob Agents Chemother 1998; 42: 1762-70
9. 9. Banerjee SN, Emori TG, Culver DH, et al. Secular trends in nosocomial primary bloodstream infections in the United States, 1980-1989. Am J Med 1991; 91 Suppl. 3B: 86S-89S
10. 10. Marshall SA, Wilke WW, Pfaller MA, et al. Staphylococcus aureus and coagulase-negative staphylococci from blood stream infections: frequency of occurrence, antimicrobial susceptibility, and molecular (mec A) characterisation of oxacillin resistance in the SCOPE program. Diagn Microbiol Infect Dis 1998; 30: 205-14
11. 11. Moellering RC. Vancomycin-resistant enterococci. Clin Infect Dis 1998; 26: 1196-9
12. 12. Jones RN, Barrett MS. Antimicrobial activity of SCH 27899, oligosaccharide member of the everninomycin class with a wide Gram-positive spectrum. Clin Microbiol Infect 1995; 1: 35-43
13. 13. Linden PK, Pasculle AW, McDevitt D, et al. Effect of quinupristin-dalfopristin on the outcome of vancomycin-resistant Enterococcus faecium bacteraemia: Comparison with a control cohort. J Antimicrob Chemother 1997; 39 Suppl. A: 145-51
14. 14. Jones RN, Barrett MS, Erwin ME. In vitro activity and spectrum of LY333328, a novel glycopeptide derivative. Antimicrob Agents Chemother 1997; 41: 488-93
15. 15. Chambers HF. In vitro and in vivo antistaphylococcal activities of 1-695,256, a carbapenem with high affinity for the penicillin-binding protein PBP 2a. Antimicrob Agents Chemother 1995; 39: 462-6
16. 16. Rosen H, Silver L, Hammond M. L-786,392: a releasable pharmacophore carbapenem active on MRS, VISA, and VRE. Abstracts of the 36th Annual General Meeting of the Infectious Diseases Society of America; 1998 Nov 12-15: Denver (CO). Alexandria (VA): Infectious Diseases Society of America, 1998
17. 17. Alborn WE, Allen NE, Preston DA. Daptomycin disrupts membrane potential in growing Staphylococcus aureus. Antimicrob Agents Chemother 1991; 35: 2282-7
18. 18. Ford CW, Hamel JC, Stapert D, et al. Oxazolidinones: new antibacterial agents. Trends Microbiol 1997; 5: 196-200
19. 19. Moellering Jr RC. A novel antimicrobial agent joins the battle against resistant bacteria. Ann Intern Med 1999; 130: 155-7
20. 20. Slee AM, Wuonola MA, McRipley RJ, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother 1987; 31: 1791-7
21. 21. Brickner SJ. Oxazolidinone antibacterial agents. Curr Pharm Design 1996; 2: 175-94
22. 22. Brickner SJ, Hutchinson DK, Barbachyn MR, et al. Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections. J Med Chem 1996; 39: 673-9
23. 23. Eustice DC, Feldman PA, Zajaz I, et al. Mechanism of action of DuP-721: inhibition of an early event during initiation of protein synthesis. Antimicrob Agents Chemother 1988; 32: 1218-22
24. 24. Daly JS, Eliopoulos GM, Reiszner I, et al. Mechanism of action and in vitro studies of DuP-105 and DuP-721, new oxazolidinone antibacterials. J Antimicrob Chemother 1988; 21: 721-30
25. 25. Shinabarger DL, Marotti KR, Murray RW, et al. Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions. Antimicrob Agents Chemother 1997; 41: 2132-6
26. 26. Lin AH, Murray RW, Vidmar TJ, et al. The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother 1997; 41: 2127-31
27. 27. Swaney SM, Aoki H, Clelia Ganoza M, et al. The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria. Antimicrob Agents Chemother 1998; 42: 3251-5
28. 28. Zurenko GE, Yagi BH, Schaadt RD, et al. In vitro activities of U-100592 and U-100766, novel oxazolidinone antibacterial agents. Antimicrob Agents Chemother 1996; 40: 839-45
29. 29. Murray RW, Schaadt RD, Zurenko GE, et al. Ribosomes from an oxazolidinone-resistant mutunt confer resistance to eperezolid in a Staphylococcus aureus cell-free transcription-translation assay. Antimicrob Agents Chemother 1998; 42: 947-50
30. 30. Kaatz GW, Seo SM. In vitro activities of oxazolidinone compounds U-100592 and U-100766 against Staphylococcus aureus and Staphylococcus epidermidis. Antimicrob Agents Chemother 1996; 40; 799-801
31. 31. Swaney SM, Shinabarger DL, Schaadt RD, et al. Oxazolidinone resistance is associated with a mutation in the peptidyl transferase region of 23S rRNA [abstract C-104]. In: Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
32. 32. Jones RN, Johnson DM, Erwin ME. In vitro antimicrobial activities and spectra of U-100592 and U-100766, two novel fluorinated oxazolidinones. Antimicrob Agents Chemother 1996; 40: 720-6
33. 33. Mulazimoglu L, Drenning SD, Yu VL. In vitro activities of two novel oxazolidinones (U-100592 and U-100766), a new fluoroquinolone (trovafloxacin), and dalfopristin-quinupristin against Staphylococcus aureus and Staphylococcus epidermidis. Antimicrob Agents Chemother 1996; 40: 2428-30
34. 34. Jorgensen JH, McElmeel ML, Trippy CW. In vitro activities of the oxazolidinone antibiotics U-100592 and U-100766 against Staphylococcus aureus and coagulase-negative Staphylococcus species. Antimicrob Agents Chemother 1997; 41: 465-7
35. 35. Rybak MJ, Cappelletty DM, Moldovan T, et al. Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus faecalis, and Enterococcus faecium. Antimicrob Agents Chemother 1998; 42: 721-4
36. 36. Spangler SK, Jacobs MR, Appelbaum PC. Activities of RPR 106972 (a new oral streptogramin), cefditoren (a new oral cephalosporin), two new oxazolidinones (U-100592 and U-100766), and other oral and parenteral agents against 203 penicillin-susceptible and -resistant pneumococci. Antimicrob Agents Chemother 1996; 40: 481-4
37. 37. Mason EO, Lamberth LB, Kaplan SL. In vitro activities of oxazolidinones U-100592 and U-100766 against penicillin-resistant and cephalosporin-resistant strains of Streptococcus pneumoniae. Antimicrob Agents Chemother 1996; 40: 1039-40
38. 38. Mercier RC, Penzak SR, Rybak MJ. In vitro activities of an investigational quinolone, glycylcycline, glycopeptide, streptogramin, and oxazolidinone tested alone and in combinations against vancomycin-resistant Enterococcus faecium. Antimicrob Agents Chemother 1997; 41: 2573-5
39. 39. Bostic GD, Perri MB, Thal LA, et al. Comparative in vitro and bactericidal activity of oxazolidinone antibiotics against multidrug-resistant enterococci. Diagn Microbiol Infect Dis 1998; 30: 109-12
40. 40. Eliopoulos GM, Wennersten CB, Gold HS, et al. In vitro activities of new oxazolidinone antimicrobial agents against enterococci. Antimicrob Agents Chemother 1996; 40: 1745-7
41. 41. Biedenbach DJ, Jones RN. Disk diffusion test interpretive criteria and quality control recommendation for testing linezolid (U-1007660 and eperezolid (U-100592) with commercially prepared reagents. J Clin Microbiol 1997; 35: 3198-202
42. 42. Data on file, Upjohn Co., 1997
43. 43. Salmon SA, Portis EL, Case CA, et al. Minimum inhibitory concentration determinations for oxazolidinone antimicrobial agents and comparator agents against strains of Rhodococcus equi [abstract E-129]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
44. 44. Schulin T, Wennersten CB, Ferraro MJ, et al. Susceptibilities of Legionella spp. to newer antimicrobials in vitro. Antimicrob Agents Chemother 1998; 42: 1520-3
45. 45. Goldstein EJ, Citron DM, Gerardo SH, et al. Linezolid compared with other macrolides against Pasteurella species [abstract E-147]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy: 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
46. 46. Di Pentima MC, Mason Jr EO, Kaplan SL. In vitro antibiotic synergy against Flavobacterium meningosepticum: implications for therapeutic options. Clin Infect Dis 1998; 26: 1169-76
47. 47. Yagi BH, Zurenko GE. In vitro activity of linezolid and eperezolid, two novel oxazolidinone antimicrobial agents, against anaerobic bacteria. Anaerobe 1997; 3: 301-6
48. 48. Ashtekar DR, Costa-Periera R, Shrinivasan T, et al. Oxazolidinones, a new class of synthetic antituberculous agent; in vitro and in vivo activities of DuP-721 against Mycobacterium tuberculosis. Diagn Microbiol Infect Dis 1991; 14: 465-71
49. 49. Peters J, Kondo KL, Lee RK, et al. In vitro activity of oxazolidinones against Mycobacterium avium complex. J. Antimicrob Chemother 1995; 35: 675-9
50. 50. Wu M, Aralor P, Nash K, et al. Linezolid, a new oxazolidinone, has activity in vitro and in macrophage culture system against Mycobacterium avium complex (MAC) [abstract E-142]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
51. 51. Barbachyn MR, Hutchinson DK, Brickner SJ, et al. Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity. J Med Chem 1996; 39: 680-5
52. 52. Cynamon MH, Klemens SP, Sharpe CA, et al. Activities of several novel oxazolidinones against Mycobacterium tuberculosis in a murine model. Antimicrob Agents Chemother 1999; 43: 1189-91
53. 53. Ford CW, Hamel JC, Wilson DM, et al. In vivo activities of U-100592 and U-100766, novel oxazolidinone antimicrobial agents, against experimental bacterial infections. Antimicrob Agents Chemother 1996; 40: 1508-13
54. 54. Batts DH, Stalker DJ, Peel BG, et al. U-100592 phase I, multiple-oral dose, randomized, placebo-controlled, safety, tolerance and pharmacokineties in healthy volunteers for 14.25 days using bulk drugs in capsules [abstract]. In: Program and Abstracts of the 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17-20: Washington (DC). Washington (DC): American Society for Microbiology, 1995
55. 55. Stalker DJ, Wajszczuk CP, Batts DH. Linezolid safety, tolerance, and pharmacokineties following oral dosing twice daily for 14.5 days [abstract A-115]. In: Program and Abstracts of the 37th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1997 Sep 28-Oct 1: Washington (DC). Washington (DC): American Society for Microbiology, 1997
56. 56. Stalker DJ, Wajszczuk CP, Batts DH. Linezolid safety, tolerance, and pharmacokinetics after intravenous dosing twice daily for 7.5 days [abstract A-116]. In: Program and Abstracts of the 37th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1997 Sep 28-Oct 1: Washington (DC). Washington (DC): American Society for Microbiology, 1997
57. 57. Brier ME, Stalker DJ, Aronoff GR, et al. Pharmacokinetics of linezolid in subjects with various degrees of renal function and on dialysis [abstract A-54]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
58. 58. Stalker DJ, Kearns GL, James L, et al. Pharmacokinetics of linezolid in pediatric patients [abstract 749]. In: Program and Abstracts of the 36th meeting of the Infectious Diseases Society of America; 1998 Nov 12-15: Denver (CO). Alexandria (VA): Infectious Diseases Society of America, 1998
59. 59. Andes D, Vesga O, Batts D, et al. Pharmacodynamic activity of an oxazolidinone in an animal infection model [abstract F-233]. In: Program and Abstracts of the 36th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1996 Sep 15-18: Washington (DC). Washington (DC): American Society for Microbiology, 1996
60. 60. Andes D, Van Ogtrop ML, Craig WA. Pharmacodynamic activity of a new oxazolidinone, linezolid, in an animal infection model [abstract A-9]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
61. 61. Batts DH. Linezolid clinical development program: end of phase II results [abstract]. 2nd European Congress of Chemotherapy: 1998 May 10-13, Hamburg
62. 62. Birmingham MC, Zimmer GS, Hafkin B, et al. Initial results of linezolid in patients with multidrug-resistant Gram-positive infections [abstract MN-26]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
63. 63. Hyatt JM, Ballow CH, Forrest A, et al. Safety and efficacy of linezolid in eradication of nasal Staphylococcus aureus [abstract A-4]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
64. 64. Perl TM, Cullen JJ, Pfaller MA, et al. A randomized, double-blind, placebo-controlled trial of intranasal mupirocin ointment for prevention of S. aureus surgical site infections [abstract 88]. In: Abstracts of the 36th Annual Meeting of the Infectious Diseases Society of America; 1998 Nov 12-15: Denver (CO). Alexandria (VA): Infectious Diseases Society of America, 1998
65. 65. Dresser LD, Rybak MJ. The pharmacologic and bacteriologic properties of oxazolidinones, a new class of synthetic antimicrobials. Pharmacotherapy 1998; 18: 456-62
66. 66. Martin JP, Herberg JT, Slatter JG, et al. Although a novel microtiter-plate assay demonstrates that linezolid is a weak, competitive (reversible) inhibitor of human monoamine oxidase (MAO A), no clinical evidence of MAO A inhibition in clinical trials has been observed [abstract A-85]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
67. 67. Gadwood RC, Walker EA, Thomasco LM, et al. Synthesis and antibacterial activity of azolylphenyl oxazolidinones having carbon-bound 1,3-thiazolyl rings [abstract F-139]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998
68. 68. Endermann R, Bartel S, Guarnieri W, et al. Synthesis and antibacterial activity of novel heteroaryl oxazolidinones. III: activities against clinically important Gram-positive pathogens [abstract F-129]. In: Program and Abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1998 Sep 24-27: Washington (DC). Washington (DC): American Society for Microbiology, 1998