TABLE 6

Metabolic profiles of garenoxacin in the plasma and excreta of monkeys

Metabolic profiles were determined in samples pooled from three animals following oral, intraduodenal, and intravenous administration of 14C-garenoxacin at 5 mg/kg (plasma and bile samples were determined from one animal). Results are expressed as percentage of radioactivity in samples. Amounts excreted into the urine, feces, and bile 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
UN 32 m
i.v.
Plasma 5 min a N.A. 98.6 1.4 N.D. N.D. N.D. N.D. N.D. N.D. N.D.
Plasma 4 h a N.A. 92.3 7.7 N.D. N.D. N.D. N.D. N.D. N.D. N.D.
Urine 0-24 h 44.3 ± 9.4 91.0 5.6 0.9 N.D. 0.4 N.D. 1.6 N.D. N.D.
Feces 0-24 h 35.6 ± 3.8 24.1 73.5 N.D. N.D. 0.6 N.D. N.D. 0.2 N.D.
Bile 0-6 h a 20.5 4.5
80.5
2.7
4.0
N.D.
N.D.
0.6
2.3
4.5
p.o.
Urine 0-24 h 35.9 ± 10.7 88.5 8.5 0.9 N.D. 0.4 N.D. 1.6 N.D. N.D.
Feces 0-24 h b 43.3 ± 10.6 25.4
72.4
N.D.
N.D.
0.4
N.D.
N.D.
0.3
N.D.
i.d.
Plasma 1 h a N.A. 75.6 24.4 N.D. N.D. N.D. N.D. N.D. N.D. N.D.
Plasma 4 h a N.A. 74.6 25.4 N.D. N.D. N.D. N.D. N.D. N.D. N.D.
Bile 0-6 h a
12.3
2.9
81.1
2.9
3.7
N.D.
N.D.
0.3
2.7
4.4

  • Amount, excretion of radioactivity as percentage of dose; GRX, garenoxacin; M1, T-3811 M1;M2, carbamoyl glucuronide; M3, carbamic acid; M4, T-3811 M4; M5, T-3811 M5; UN 2 m, unknown metabolite at retention time 2 min; UN 32 m, unknown metabolite at retention time 32 min; N.D., not detected; N.A., not applicable.

  • ↵ a Results obtained are from one animal.

  • ↵ b The feces of one animal was obtained at 24 to 48 h because radioactivity was not recovered from 0- to 24-h feces.