TABLE 5

Metabolic profiles of garenoxacin in the plasma and excreta of dogs

Metabolic profiles were determined in samples pooled from three animals following intravenous administration of 14C-garenoxacin at 100 mg/kg. Results are expressed as percentage of radioactivity in samples. Amounts excreted into the urine and feces were expressed as percentage of dose (mean ± S.D.).


Sample

Amount (% Dose)

Metabolites (Percentage of Sample Radioactivity)
GRX
M1
M2
M3
M4
M5
M6
UN 2 m
Plasma 5 min N.A. 100 N.D. N.D. N.D. N.D. N.D. N.D. N.D.
Plasma 2 h N.A. 91.8 8.2 N.D. N.D. N.D. N.D. N.D. N.D.
Plasma 6 h N.A. 90.9 9.1 N.D. N.D. N.D. N.D. N.D. N.D.
Plasma 24 h N.A. 100 N.D. N.D. N.D. N.D. N.D. N.D. N.D.
Urine 0-24 h 30.0 ± 2.7 88.3 4.6 0.8 N.D. N.D. N.D. 2.1 4.2
Feces 0-24 h
30.7 ± 8.1
70.4
18.5
1.5
3.1
N.D.
N.D.
1.9
4.5
  • Amount, excretion of radioactivity as percentage of dose; GRX, garenoxacin; M1, T-3811M1; M2, carbamoyl glucuronide; M3, carbamic acid; M4, T-3811M4; M5, T-3811M5; UN 2 m, unknown metabolite at retention time 2 min; N.D., not detected; N.A., not applicable.