Disposition, metabolism and mass balance of delafloxacin in healthy human volunteers following intravenous administration. (2nd December 2015)

• Record Type: Journal Article
• Authors: McEwen, Andrew; Lawrence, Laura; Hoover, Randy; Stevens, Lloyd; Mair, Stuart; Ford, Gill; Williams, Dylan; Wood, Stuart
• Is Part Of: Xenobiotica. Volume 45:Number 12(2015:Dec.)
• Page Start: 1054
• Page End: 1062
• Publication Date: 2015-12-02
• Subjects: Delafloxacin -- human -- metabolism -- quinolone; Metabolism -- Periodicals; Drugs -- Physiological effect -- Periodicals; Food additives -- Periodicals; Chemicals -- Physiological effect -- Periodicals; Biochemistry -- Periodicals; Pharmaceutical Preparations -- metabolism -- Periodicals; Metabolism -- Periodicals; 574.133
• DOI: 10.3109/00498254.2015.1042946
• Languages: English
• ISSNs: 0049-8254

Abstract

Abstract: 1. The pharmacokinetics and disposition of delafloxacin was investigated following a single intravenous (300 mg, 100 µCi) dose to healthy male subjects. 2. Mean C max, AUC0–∞, T max and t 1/2 values for delafloxacin were 8.98 µg/mL, 21.31 µg 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.