TABLE 1

Pharmacokinetic parameters of the radioactivity in the plasma of rats during and after 21 daily multiple oral administrations of [14C]MLN3126 at a daily dose of 10 mg at 4.71 MBq/kg

Each value represents the mean ± S.D.value for three animals.

DayPharmacokinetic Parameter
TmaxCmaxaCmina,bt1/2AUC0–24 ha
hμg Eq/mlμg Eq/mlhμg Eq⋅h/ml
11.0 ± 0.04.321 ± 1.3510.845 ± 0.28011.5 ± 0.848.587 ± 15.443
41.0 ± 0.05.392 ± 1.0411.214 ± 0.33713.1 ± 0.362.364 ± 16.729
70.7 ± 0.35.717 ± 0.5071.062 ± 0.17112.5 ± 0.457.117 ± 7.340
110.8 ± 0.36.857 ± 1.9631.129 ± 0.29412.5 ± 0.163.574 ± 15.484
140.7 ± 0.37.502 ± 1.1951.349 ± 0.29813.6 ± 0.570.882 ± 13.612
180.7 ± 0.35.331 ± 1.0921.184 ± 0.30214.1 ± 0.658.867 ± 15.921
211.0 ± 0.05.936 ± 1.5271.237 ± 0.44513.9 ± 1.163.425 ± 23.450
  • Cmin, concentration 24 hours after administration; Tmax, time to reach Cmax.

  • a MLN3126 equivalent.

  • b Concentration 24 hours after administration.