TABLE 4

Recovery of KAE609 and its metabolites in human excreta (expressed as percentage of dose) after an oral dose of 300 mg [14C] KAE609

The pooled urine and fecal samples were extracted and analyzed by LC-MS/MS for metabolic profiling. The HPLC separation of KAE609 and metabolites was performed using a Zorbax SB-C18 column, as described in the Materials and Methods.

KAE609/MetaboliteFecesUrine
MeanSDAverageb
M140.3850.9431.45
M162.650.6530.45
M180.3920.960ND
M20.8NDND0.15
M21.8NDNDND
M2336.212.51.4
M23.5A/M23.5Ba2.411.19ND
M24NDND0.4
M29.82.291.45ND
M322.530.7800.05
M331.971.26ND
M341.972.17ND
M35.8NDND0.10
M482.390.5460.05
KAE60931.717.1ND
Percentage of dose85.02.474.05

  • ND, not detectable.

  • ↵a M23.5A/M23.5B: two metabolites were coeluted and the recovery represented the mixture of two metabolites.

  • ↵b The pooled urine samples were extracted from only two subjects (numbers 5103 and 5104).