TABLE 6

Relative distribution (percentage of dose) of radioactive metabolites in pooled urine and feces after an oral dose of [14C]muraglitazar to intact rats, dogs, monkeys, and humans

Metabolitea
Muraglitazar Metabolite Distribution in Urine and Fecesb
Rat
Dog
Monkey
Human
Urine
Feces
Urine
Feces
Urine
Feces
Urine
Feces
% of dose
M1 0.22 1.75 0.44 0.89 1.04 2.81 0.06 0.80
M2 0.05 9.65 N.D. N.D. 0.08 1.29 N.D. 0.56
M3 tracec N.D. N.D. N.D. N.D. 2.41 N.D. 1.36
M4 N.D.d N.D. N.D. 0.34 N.D. 0.16 N.D. 2.83
M5 0.01 2.63 N.D. 0.38 0.26 1.61 0.16 11.45
M6 0.01 N.D. N.D. N.D. 0.01 3.22 N.D. 1.48
M7 N.D. 0.43 N.D. 0.18 N.D. 0.32 N.D. 2.21
M8 N.D. N.D. N.D. 0.89 0.13 6.43 N.D. 0.56
M8a trace 4.39 N.D. 0.18 0.12 N.D. 0.03 0.56
M9 N.D. 2.63 N.D. 0.89 N.D. 0.56 N.D. 2.46
M10 0.03 0.88 N.D. 1.10 0.01 7.24 0.03 8.20
M11 trace 0.88 N.D. 1.78 0.59 25.73 0.07 5.92
M12 trace N.D. N.D. 0.10 0.04 1.61 N.D. 0.13
M13 trace 0.88 N.D. N.D. 0.02 0.80 1.00 0.06
M14 trace 0.88 N.D. 0.85 0.03 0.56 N.D. 1.60
M15 0.12 34.20 N.D. 24.92 0.08 7.24 N.D. 3.33
M16 N.D. 0.88 N.D. 0.18 N.D. 0.16 N.D. 3.21
M18 trace N.D. N.D. N.D. trace N.D. 0.20 N.D.
M20 trace N.D. N.D. N.D. trace N.D. N.D. N.D.
M21 0.21 0.88 0.01 N.D. 0.33 0.40 0.04 0.40
Parent 0.02 13.16 0.01 52.51 0.11 7.24 0.29 9.62
Otherse 0.3 13.6 0.02 N.A. 0.79 4.02 0.58 2.40
Total 0.97 74.1 0.48 85.2 3.63 73.49 2.46 59.20
Percentage Excretion
1.0
87.7
0.5
89.0
3.7
80.4
2.56
61.59

  • ↵ a Metabolites are assigned based on retention times of radioactive peaks and LC/MS analysis.

  • ↵ b Radioactive peaks are reported as a percentage of dose (% of the sample multiplied by % excretion).

  • ↵ c trace = <0.01% radioactivity and detected by LC/MS.

  • ↵ d N.D., not detected. Criteria are no discernible radioactive peak, <0.01% radioactivity, and not detected by LC/MS. N.A., not applicable.

  • ↵ e Others = uncharacterized peaks.