TABLE 6

Metabolic pathways observed in excreta of mice, rats, and dogs after single oral administration of [14C]casopitant

Percent dose figures are reported as a range because of metabolite coelutions.

Species (Gender)Piperazine Ring Opening and OxidationMethyl and Piperazine OxidationN-Demethylation and OxidationN-Dealkylation at Carbamate GroupN-Deacetylation and OxidationGlucuronidationGlutathione Conjugation
Mice (male)M141M3, M61, M50, M80M63M16, M20, M21, M28 M138M137
    %Dose0–429–360–83–150–6N.A.
Rat (male)M31, M123, M134, M169M41, M50, M80M1, M33, M63M16, M20, M21, M28 M138M100, M102, M103, M106, M118, M119, M171, M172 M173M81
    %Dose1–251–764–90–125–350–9
Rat (female)M31, M123, M134, M169M3, M13, M41, M50, M61,M80M1, M33, M63M20, M28, M138M76M78, M103, M104 M119
    %Dose9–1710–206–160–10–55
Dog (male)M31, M123, M134, M169M3, M37M1, M33M16, M21 M28,M138M9, M12M103, M104, M119M81, M82
    %Dose8–123–95–82–31–33–70–4
  • N.A., not applicable, because mouse bile was not collected.