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
  • [31] Metabolism and disposition of pyrotinib in healthy male volunteers: covalent binding with human plasma protein
    Jian Meng
    Xiao-yun Liu
    Sheng Ma
    Hua Zhang
    Song-da Yu
    Yi-fan Zhang
    Mei-xia Chen
    Xiao-yu Zhu
    Yi Liu
    Ling Yi
    Xiao-liang Ding
    Xiao-yan Chen
    Li-yan Miao
    Da-fang Zhong
    Acta Pharmacologica Sinica, 2019, 40 : 980 - 988
  • [32] PHARMACOKINETICS OF ISOXICAM FOLLOWING INTRAVENOUS, INTRAMUSCULAR, ORAL AND RECTAL ADMINISTRATION IN HEALTHY-VOLUNTEERS
    KOLLE, EU
    VOLLMER, KO
    BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1986, 22 : S135 - S141
  • [33] Pharmacokinetics of the antiepileptic drug levetiracetam in healthy Japanese and Caucasian volunteers following intravenous administration
    Toublanc, Nathalie
    Okagaki, Takuya
    Boyce, Malcolm
    Chan, Robert
    Mugitani, Ayumi
    Watanabe, Shikiko
    Yamamoto, Katsumi
    Yoshida, Katsumi
    Andreas, Jens-Otto
    EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS, 2015, 40 (04) : 461 - 469
  • [34] Pharmacokinetics of the antiepileptic drug levetiracetam in healthy Japanese and Caucasian volunteers following intravenous administration
    Nathalie Toublanc
    Takuya Okagaki
    Malcolm Boyce
    Robert Chan
    Ayumi Mugitani
    Shikiko Watanabe
    Katsumi Yamamoto
    Katsumi Yoshida
    Jens-Otto Andreas
    European Journal of Drug Metabolism and Pharmacokinetics, 2015, 40 : 461 - 469
  • [35] Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers
    Hoover, Randall
    Hunt, Thomas
    Benedict, Michael
    Paulson, Susan K.
    Lawrence, Laura
    Cammarata, Sue
    Sun, Eugene
    CLINICAL THERAPEUTICS, 2016, 38 (01) : 53 - 65
  • [36] Pharmacokinetics of fosfluconazole and fluconazole following multiple intravenous administration of fosfluconazole in healthy male volunteers
    Sobue, S
    Tan, K
    Layton, G
    Eve, M
    Sanderson, JB
    BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 2004, 58 (01) : 20 - 25
  • [37] Time Course for Measuring Endolymphatic Size in Healthy Volunteers Following Intravenous Administration of Gadoteridol
    Naganawa, Shinji
    Suzuki, Kojiro
    Yamazaki, Masahiro
    Sakurai, Yasuo
    Ikeda, Mitsuru
    MAGNETIC RESONANCE IN MEDICAL SCIENCES, 2014, 13 (02) : 73 - 80
  • [38] BIOAVAILABILITY OF FOLIC-ACID FOLLOWING INTRAMUSCULAR AND INTRAVENOUS ADMINISTRATION TO HEALTHY-VOLUNTEERS
    MENKE, G
    MULLER, J
    WEIMANN, HJ
    SCHUSTER, O
    ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH, 1993, 43-1 (01): : 22 - 27
  • [39] Effects of concurrent administration of nevirapine on the disposition of quinine in healthy volunteers
    Soyinka, Julius O.
    Onyeji, Cyprian O.
    Omoruyi, Sharon I.
    Owolabi, Adegbenga R.
    Sarma, Pullela V.
    Cook, James M.
    JOURNAL OF PHARMACY AND PHARMACOLOGY, 2009, 61 (04) : 439 - 443
  • [40] Effects of prior administration of amodiaquine on the disposition of halofantrine in healthy volunteers
    Omoruyi, Sharon I.
    Onyeji, Cyprian O.
    Daniyan, Michael O.
    THERAPEUTIC DRUG MONITORING, 2007, 29 (02) : 203 - 206