Pharmacokinetics of tigecycline after single and multiple doses in healthy subjects

Antimicrobial Agents and Chemotherapy

Volumn 49, Issue 1, 2005, Pages 220-229

  Muralidharan, Gopal ^a,b   Micalizzi, Marlynne ^a   Speth, John ^a   Raible, Donald ^a   Troy, Steven ^a  

^a PFIZER INC   (United States)

^b Lotus Labs Private Ltd   (India)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIBIOTIC AGENT; GLYCYLGLYCINE; ONDANSETRON; PLACEBO; TETRACYCLINE DERIVATIVE; TIGECYCLINE;

ADULT; AEROBIC BACTERIUM; ANAEROBIC BACTERIUM; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG CLEARANCE; DRUG SAFETY; DRUG TOLERABILITY; GRAM NEGATIVE BACTERIUM; GRAM POSITIVE BACTERIUM; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; NAUSEA; NORMAL HUMAN; PENICILLIN RESISTANCE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; STREPTOCOCCUS PNEUMONIAE; TANDEM MASS SPECTROMETRY; VALIDATION PROCESS; VANCOMYCIN RESISTANT ENTEROCOCCUS; VOMITING;

ADOLESCENT; ADULT; ANTI-BACTERIAL AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; DRUG ADMINISTRATION SCHEDULE; HALF-LIFE; HUMANS; MALE; MINOCYCLINE;

EID: 11244353707     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.49.1.220-229.2005     Document Type: Article

References (26)

1. Betriu, C., I. Rodriguez-Avial, B. A. Sanchez, M. Gomez, J. Alvarez, J. J. Picazo, et al. 2002. In vitro activities of tigecycline (GAR-936) against recently isolated clinical bacteria in Spain. Antimicrob. Agents Chemother. 46:892-895.
2. Chin, T., and J. L. Lach. 1975. Drug diffusion and bioavailability: tetracycline metallic chelation. Am. J. Hosp. Pharm. 32:625-629.
3. Chopra, I. 2002. New developments in tetracycline antibiotics: glycylcyclines and tetracycline efflux pump inhibitors. Drug Resist. Update 5:119-125.
4. Cubeddu, L. X., I. S. Hoffmann, N. T. Fuenmayor, and A. L. Finn. 1990. Efficacy of ondansetron (GR 38032F) and the role of serotonin in cisplatin-induced nausea and vomiting. N. Engl. J. Med. 322:810-816.
5. Deshpande, L. M., A. C. Gales, and R. N. Jones. 2001. GAR-936 (9-t-butylglycylamido-minocycline) susceptibility test development for streptococci, Haemophilus influenzae and Neisseria gonorrhoeae: preliminary guidelines and interpretive criteria. Int. J. Antimicrob. Agents 18:29-35.
6. Edelstein, P. H., W. J. Weiss, and M. A. Edelstein. 2003. Activities of tigecycline (GAR-936) against Legionella pneumophila in vitro and in guinea pigs with L. pneumophila pneumonia. Antimicrob. Agents Chemother. 47:533-540.
7. Fey, G., M. Reiss, and H. Kersten. 1973. Interaction of tetracyclines with ribosomal subunits from Escherichia coli: a fluorometric investigation. Biochemistry 12:1160-1164.
8. Gabler, W. L. 1991. Fluxes and accumulation of tetracyclines by human blood cells. Res. Commun. Chem. Pathol. Pharmacol. 72:39-51.
9. Gales, A. C., and R. N. Jones. 2000. Antimicrobial activity and spectrum of the new glycylcycline, GAR-936, tested against 1,203 recent clinical bacterial isolates. Diagn. Microbiol. Infect. Dis. 36:19-36.
10. Hoellman, D. B., G. A. Pankuch, M. R. Jacobs, and P. C. Appelbaum. 2000. Antipneumococcal activities of GAR-936 (a new glycylcycline) compared to those of nine other agents against penicillin-susceptible and -resistant pneumococci. Antimicrob. Agents Chemother. 44:1085-1088.
11. Lefort, A., M. Lafaurie, L. Massias, Y. Petegnief, A. Saleh-Mghir, C. Muller-Serieys, D. Le Guludec, and B. Fantin. 2003. Activity and diffusion of tigecycline (GAR-936) in experimental enterococcal endocarditis. Antimicrob. Agents Chemother. 47:216-222.
12. Macdonald, H., R. G. Kelly, E. S. Allen, J. F. Noble, and L. A. Kanegis. 1973. Pharmacokinetic studies on minocycline in man. Clin. Pharmacol. Ther. 14:852-861.
13. Milatovic, D., F. J. Schmitz, J. Verhoef, and A. C. Fluit. 2003. Activities of the glycylcycline tigecycline (GAR-936) against 1,924 recent European clinical bacterial isolates. Antimicrob. Agents Chemother. 47:400-404.
14. Muralidharan, G., P. Mojaverian, M. Micalizzi, J. Speth, S. Tse, R. Stroshane, J. Getsy, and P. Mayer. 2000. The effects of age and gender on the pharmacokinetics, safety and tolerability of GAR-936, a novel glycylcycline antibiotic, in healthy subjects. Program Abstr. 40th Intersci. Conf. Antimicrob. Agents Chemother., abstr. 500.
15. Murray, J., S. Wilson, S. Klein, A. Yellin, and E. Loh. 2003. The clinical response to tigecycline in the treatment of complicated intra-abdominal infections in hospitalized patients: a phase 2 clinical trial. Program Abstr. 43rd Intersci. Conf. Antimicrob. Agents Chemother., abstr. L-739.
16. Petersen, P. J., H. E. Hartman, T. Z. Wang, R. G. Dushin, and P. A. Bradford. 2002. Time kill kinetics and postiantibiotic (PAE) effects of the AC98 novel semisynthetic cyclic glycopeptide antibiotic derivative WAY-176446. Program Abstr. 42nd Intersci. Conf. Antimicrob. Agents Chemother., abstr. F-354.
17. Petersen, P. J., N. V. Jacobus, W. J. Weiss, P. E. Sum, and R. T. Testa. 1999. In vitro and in vivo antibacterial activities of a novel glycylcycline, the 9-t-butylglycylamido derivative of minocycline (GAR-936). Antimicrob. Agents Chemother. 43:738-744.
18. Petersen, P. J., W. J. Weiss, P. Labthavikul, and B. P. A. 1998. The post-antibiotic effect and time-kill kinetics of the glycylcyclines, GAR-936 (TBG-MINO) and (PAM-MINO). Program Abstr. 38th Intersci. Conf. Antimicrob. Agents Chemother., abstr. F-132.
19. Postier, R. G., S. L. Green, S. R. Klein, E. J. Ellis-Grosse, E. Loh, et al. 2004. Results of a multicenter, randomized, open-label efficacy and safety study of two doses of tigecycline for complicated skin and skin-structure infections in hospitalized patients. Clin. Ther. 26:704-714.
20. Roblin, P. M., and M. R. Hammerschlag. 2000. In vitro activity of GAR-936 against Chlamydia pneumoniae and Chlamydia trachomatis. Int. J. Antimicrob. Agents 16:61-63.
21. Sesoko, S., K. Umemura, and M. Nakashima. 2002. Pharmacokinetics (PK), safety, and tolerability of tigecycline (GAR-936) in healthy Japanese males. Program Abstr. 42nd Intersci. Conf. Antimicrob. Agents Chemother., abstr. A-1403.
22. Testa, R. T., P. J. Petersen, N. V. Jacobus, P. E. Sum, V. J. Lee, and F. P. Tally. 1993. In vitro and in vivo antibacterial activities of the glycylcyclines, a new class of semisynthetic tetracyclines. Antimicrob. Agents Chemother. 37:2270-2277.
23. Tombs, N. L. 1999. Tissue distribution of Gar-936, a broad-spectrum antibiotic, in male rats. Program Abstr. 39th Intersci. Conf. Antimicrob. Agents Chemother., abstr. 413.
24. van Ogtrop, M. L., D. Andes, T. J. Stamstad, B. Conklin, W. J. Weiss, W. A. Craig, and O. Vesga. 2000. In vivo pharmacodynamic activities of two glycylcyclines (GAR-936 and WAY 152,288) against various gram-positive and gram-negative bacteria. Antimicrob. Agents Chemother. 44:943-949.
25. Wallace, R. J., Jr., B. A. Brown-Elliott, C. J. Crist, L. Mann, and R. W. Wilson. 2002. Comparison of the in vitro activity of the glycylcycline tigecycline (formerly GAR-936) with those of tetracycline, minocycline, and doxycycline against isolates of nontuberculous mycobacteria. Antimicrob. Agents Chemother. 46:3164-3167.
26. Zhanel, G. G., K. Homenuik, K. Nichol, A. Noreddin, L. Vercaigne, J. Embil, A. Gin, J. A. Karlowsky, and D. J. Hoban. 2004. The glycylcyclines: a comparative review with the tetracyclines. Drugs 64:63-88.