Pharmacokinetics and whole-blood bactericidal activity against mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers

Journal of Infectious Diseases

Volumn 202, Issue 5, 2010, Pages 745-751

  Wallis, Robert S ^a,d   Jakubiec, Wesley M ^b   Kumar, Vikas ^a   Silvia, Annette M ^a   Paige, Darcy ^a   Dimitrova, Dessislava ^a   Li, Xiaoxi ^a   Ladutko, Lynn ^b   Campbell , Sheldon ^b,c   Friedland, Gerald ^c   Mitton Fry, Mark ^a   Miller, Paul F ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b Veterans Affairs Connecticut Healthcare   (United Kingdom)

^c YALE UNIVERSITY   (United States)

^d PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG METABOLITE; LINEZOLID; OXAZOLIDINONE DERIVATIVE; PNU 100480; UNCLASSIFIED DRUG;

ARTICLE; BACTERICIDAL ACTIVITY; CLINICAL TRIAL; CONCENTRATION RESPONSE; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG TOLERABILITY; HUMAN; HUMAN EXPERIMENT; LOOSE FECES; MAXIMUM PLASMA CONCENTRATION; MINIMUM INHIBITORY CONCENTRATION; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE;

EID: 77955706291     PISSN: 00221899     EISSN: None     Source Type: Journal    
DOI: 10.1086/655471     Document Type: Article

References (30)

1. World Health Organization (WHO). Global tuberculosis control: a short update to the 2009 report. Report WHO/HTM/TB/2009.426. Geneva: WHO, 2009. Available at: http://www.who.int/tb/publications/ global-report/2009/update/tbu- 9.pdf. Accessed 23 June 2010.
2. Condos R, Hadgiangelis N, Leibert E, Jacquette G, Harkin T, Rom WN. Case series report of a linezolid-containing regimen for extensively drug-resistant tuberculosis. Chest 2008; 134:187-192.
3. Fortun J, Martin-Dávila P, Navas E, et al. Linezolid for the treatment of multidrug-resistant tuberculosis. J Antimicrob Chemother 2005; 56: 180-185.
4. Koh WJ, Kwon OJ, Gwak H, et al. Daily 300 mg dose of linezolid for the treatment of intractable multidrug-resistant and extensively drugresistant tuberculosis. J Antimicrob Chemother 2009; 64:388-391.
5. Migliori GB, Eker B, Richardson MD, et al. A retrospective TBNET assessment of linezolid safety, tolerability and efficacy in multidrugresistant tuberculosis. Eur Respir J 2009; 34:387-393.
6. Nam HS, Koh WJ, Kwon OJ, Cho SN, Shim TS. Daily half-dose linezolid for the treatment of intractable multidrug-resistant tuberculosis. Int J Antimicrob Agents 2009; 33:92-93.
7. Ntziora F, Falagas ME. Linezolid for the treatment of patients with [corrected] mycobacterial infections [corrected] a systematic review. Int J Tuberc Lung Dis 2007; 11:606-611.
8. Park IN, Hong SB, Oh YM, et al. Efficacy and tolerability of daily-half dose linezolid in patients with intractable multidrug-resistant tuberculosis. J Antimicrob Chemother 2006; 58:701-704.
9. von der Lippe B, Sandven P, Brubakk O. Efficacy and safety of linezolid in multidrug resistant tuberculosis (MDR-TB)-a report of ten cases. J Infect 2006; 52:92-96.
10. Yew WW, Chau CH, Wen KH. Linezolid in the treatment of 'difficult' multidrug-resistant tuberculosis. Int J Tuberc Lung Dis 2008; 12: 345-346.
11. Williams KN, Brickner SJ, Stover CK, et al. Addition of PNU-100480 to first-line drugs shortens the time needed to curemurine tuberculosis. Am J Respir Crit Care Med 2009; 180:371-376.
12. Williams KN, Stover CK, Zhu T, et al. Promising anti-tuberculosis activity of the oxazolidinone PNU-100480 relative to linezolid in the murine model. Antimicrob Agents Chemother 2008; 53:1314-1319.
13. Barbachyn MR, Hutchinson DK, Brickner SJ, et al. Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity. J Med Chem 1996; 39:680-685.
14. Cynamon MH, Klemens SP, Sharpe CA, Chase S. Activities of several novel oxazolidinones against Mycobacterium tuberculosis in a murine model. Antimicrob Agents Chemother 1999; 43:1189-1191.
15. Janulionis E, Sofer C, Song HY, Wallis RS. Lack of activity of oral clofazimine against intracellular M. tuberculosis in whole-blood culture. Antimicrob Agents Chemother 2004; 48:3133-3135.
16. Wallis RS, Palaci M, Vinhas S, et al. A whole blood bactericidal assay for tuberculosis. J Infect Dis 2001; 183:1300-1303.
17. Wallis RS, Vinhas SA, Johnson JL, et al. Whole blood bactericidal activity during treatment of pulmonary tuberculosis. J Infect Dis 2003; 187: 270-278.
18. Pfizer. Zyvox package insert. New York: Pfizer, 2010. http://media .pfizer.com/files/products/uspi-zyvox.pdf. Accessed 23 June 2010.
19. Donald PR, Diacon AH. The early bactericidal activity of anti-tuberculosis drugs: a literature review. Tuberculosis (Edinb) 2008; 88: S75-S83.
20. Dietze R, Hadad DJ, McGee B, et al. Early and extended early bactericidal activity of linezolid in pulmonary tuberculosis. Am J Respir Crit Care Med 2008; 178:1180-1185.
21. Wilkinson RJ, DesJardin LE, Islam N, et al. An increase in expression of a Mycobacterium tuberculosis mycolyl transferase gene (fbpB) occurs early after infection of human monocytes. Mol Microbiol 2001; 39: 813-821.
22. Brill KJ, Li Q, Larkin R, et al. Human natural killer cells mediate kill ing of intracellular Mycobacterium tuberculosis H37Rv via granule-independent mechanisms. Infect Immun 2001; 69:1755-1765.
23. Cheon SH, Kampmann B, Hise AG, et al. Bactericidal activity in whole blood as a potential surrogate marker of immunity after vaccination against tuberculosis. Clin Diagn Lab Immunol 2002; 9:901-907.
24. Wallis RS, Wang C, Doherty TM, et al. Biomarkers for tuberculosis disease activity, cure, and relapse. Lancet Infect Dis 2010; 10:68-69.
25. Wallis RS, Weyer K, Fourie PB. Acquired rifamycin resistance: pharmacology and biology. Expert Rev Anti Infect Ther 2008; 6:223-230.
26. Ahmad Z, Peloquin C, Tyagi S, Grosset JH, Nuermberger EL. PA-824 exhibits time-dependent bactericidal activity in a murine tuberculosis model [abstract A1-607]. In: Program and abstracts of the 49th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco).Washington, D.C.: American Society for Microbiology, 2009:49.
27. Jayaram R, Shandil RK, Gaonkar S, et al. Isoniazid pharmacokineticspharmacodynamics in an aerosol infection model of tuberculosis. Antimicrob Agents Chemother 2004; 48:2951-2957.
28. Jayaram R, Gaonkar S, Kaur P, et al. Pharmacokinetics-pharmacodynamics of rifampin in an aerosol infection model of tuberculosis. Antimicrob Agents Chemother 2003; 47:2118-2124.
29. Nagiec EE, Wu L, Swaney SM, et al. Oxazolidinones inhibit cellular proliferation via inhibition of mitochondrial protein synthesis. Antimicrob Agents Chemother 2005; 49:3896-3902.
30. McKee EE, Ferguson M, Bentley AT, Marks TA. Inhibition of mammalian mitochondrial protein synthesis by oxazolidinones. Antimicrob Agents Chemother 2006; 50:2042-2049.