Disposition, metabolism and mass balance of delafloxacin in healthy human volunteers following intravenous administration

被引:20
|
作者
McEwen, Andrew [1 ]
Lawrence, Laura [2 ]
Hoover, Randy [2 ]
Stevens, Lloyd [3 ]
Mair, Stuart [3 ]
Ford, Gill [1 ]
Williams, Dylan [1 ]
Wood, Stuart [1 ]
机构
[1] Quotient Biores, Dept Metab, Pegasus Way, Rushden NN106ER, Northants, England
[2] Melinta Therapeut Inc, New Haven, CT USA
[3] Quotient Clin, Nottingham, England
关键词
Delafloxacin; human; metabolism; quinolone;
D O I
10.3109/00498254.2015.1042946
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. The pharmacokinetics and disposition of delafloxacin was investigated following a single intravenous (300 mg, 100 mu Ci) dose to healthy male subjects. 2. Mean C-max, AUC(0-infinity), T-max and t(1/2) values for delafloxacin were 8.98 mu g/mL, 21.31 mu g h/mL, 1 h and 2.35 h, respectively, after intravenous dosing. 3. Radioactivity was predominantly excreted via the kidney with 66% of the radioactive dose recovered in the urine. Approximately 29% of the radioactivity was recovered in the faeces, giving an overall mean recovery of 94% administered radioactivity. 4. The predominant circulating components were identified as delafloxacin and a direct glucuronide conjugate of delafloxacin.
引用
收藏
页码:1054 / 1062
页数:9
相关论文
共 50 条
  • [41] Absorption, disposition and metabolic pathway of amiselimod (MT-1303) in healthy volunteers in a mass balance study
    Kifuji, Takayuki
    Inoue, Shinsuke
    Furukawa, Megumi
    Madera, Begonya Perez
    Goto, Takahiro
    Kumagai, Hiroshi
    Mair, Stuart J.
    Kawaguchi, Atsuhiro
    XENOBIOTICA, 2019, 49 (09) : 1033 - 1043
  • [42] Metabolism and Disposition of Tribendimidine and Its Metabolites in Healthy Chinese Volunteers
    Yuan, Guiyan
    Xu, Jie
    Qu, Tingting
    Wang, Benjie
    Zhang, Rui
    Wei, Chunmin
    Guo, Ruichen
    DRUGS IN R&D, 2010, 10 (02) : 83 - 90
  • [43] Metabolism and disposition of tribendimidine and its metabolites in healthy Chinese volunteers
    Yuan G.
    Xu J.
    Qu T.
    Wang B.
    Zhang R.
    Wei C.
    Guo R.
    Drugs in R & D, 2010, 10 (2) : 83 - 90
  • [44] Disposition and metabolism of 14C-rifapentine in healthy volunteers
    Reith, K
    Keung, A
    Toren, PC
    Cheng, L
    Eller, MG
    Weir, SJ
    DRUG METABOLISM AND DISPOSITION, 1998, 26 (08) : 732 - 738
  • [45] Physiologic effects of intravenous fluid administration in healthy volunteers
    Holte, K
    Jensen, P
    Kehlet, H
    ANESTHESIA AND ANALGESIA, 2003, 96 (05): : 1504 - 1509
  • [46] Absorption, disposition, metabolic fate and elimination of the anti-epileptic drug lacosamide in humans: mass balance following intravenous and oral administration
    Cawello, Willi
    Boekens, Hilmar
    Bonn, Rainer
    EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS, 2012, 37 (04) : 241 - 248
  • [47] Absorption, disposition, metabolic fate and elimination of the anti-epileptic drug lacosamide in humans: mass balance following intravenous and oral administration
    Willi Cawello
    Hilmar Boekens
    Rainer Bonn
    European Journal of Drug Metabolism and Pharmacokinetics, 2012, 37 : 241 - 248
  • [48] MALTOTRIOSE AND MALTOTETRAOSE EXCRETED IN URINE FOLLOWING INTRAVENOUS ADMINISTRATION OF MALTOSE TO HUMAN VOLUNTEERS
    YUGE, O
    MORIO, M
    FUKUI, T
    FUJII, K
    KIKUCHI, H
    TAKAHASHI, S
    JAPANESE JOURNAL OF SURGERY, 1983, 13 (04): : 296 - 303
  • [49] Disposition and metabolism of 2′,2′"-Dithiobisbenzanilide in rodents following intravenous and oral administration and dermal application
    Garner, C. Edwin
    Wegerski, Christopher J.
    Doyle-Eisele, Melanie
    McDonald, Jacob D.
    Sanders, J. Michael
    Moeller, Benjamin C.
    Waidyanatha, Suramya
    TOXICOLOGY REPORTS, 2020, 7 : 883 - 892
  • [50] Metabolism and disposition of [14C]dibromoacetonitrile in rats and mice following oral and intravenous administration
    Mathews, J. M.
    Pulliam, D., Jr.
    Black, S. R.
    Burka, L. T.
    XENOBIOTICA, 2010, 40 (07) : 499 - 509