TABLE 2

Exposure of KAE609 and its metabolites in human plasma after an oral dose of 300 mg [14C] KAE609

Plasma samples were pooled according to the AUC pooling method. The pooled plasma samples were extracted and analyzed by LC-MS/MS for metabolic profiling.

Subject IDExposure of KAE609 and Metabolites in Human Plasma
KAE609M14M16M18M23M23M23.5B
ngEq⋅h/ml
510192,19111,7031646767918,84318,8433018
5102a115,7752454ND14,16254885488ND
510361,9454052415693112,51512,515ND
510472,6203042ND636913,33013,330ND
510540,920NDND401637963796ND
510666,5374162ND751316,17616,176ND
Mean74,9984236344777811,69111,691503
SD25,95139586593397592459241232
Meanb75.83.790.287.8211.911.90.37
SD6.812.960.501.564.954.950.91
  • ND, not detectable (zero was used for calculation of mean values).

  • a Plasma samples were pooled from all subjects (except 1502) from 0 to 120 hours postdose, and plasma samples from subject 1502 were pooled from 0 to 144 hours.

  • b Mean values represented as the percentage of total radioactivity in human plasma.