TABLE 6

Relative distribution of metabolites in feces and bile from mice, rats, dogs, and humans after oral administration of [14C]canagliflozin

Metabolite Identification%Dose
FecesaBileb
Mouse (100 mg/kg)Rat (3 mg/kg)Dog (4 mg/kg)Human (188 mg)Mouse (100 mg/kg)Rat (3 mg/kg)
MaleFemaleMaleFemaleMaleMaleMaleMale
Canagliflozin32.510.13.55.311.138.74.42.17
M1NDND5.518NDNDMSc2.41
M2NDNDNDNDNDNDMSND
M42.79.3NDND11.2NDNDND
M50.82.4NDNDNDNDND4.01
M5BNDNDNDNDNDNDND2.13
M61.83.710.17.9NDNDND5.93
M76.414NDND7.12.336.912.26
M813.617.351.958.841.8ND6.97.12
M927.62917.62.122.57.6NDND
M10NDND2.61.4NDNDNDND
M12NDNDNDNDNDNDND1.52
M13/M14NDNDNDNDNDNDND1.56
M15NDNDNDNDNDNDND2.69
M16NDNDNDNDNDNDND1.27
M17NDNDNDNDNDNDND0.82
M18NDNDNDNDNDNDND1.93
M19NDNDNDNDNDNDND1.55
Total85.485.891.293.593.748.648.247.37

  • MS, mass spectrometry; ND, not detected.

  • ↵a Feces samples pooled over 0 to 48 h for mice, rats, and humans, and 0 to 72 h for dogs

  • ↵b Collection interval of 0–24 h

  • ↵c MS indicates the metabolite was only observed by mass spectrometry