TABLE 4

Distribution of radioactive metabolites in urine after oral dosing [14C]ticagrelor in mice, rats, and marmosets

MetabolitesPercentage of Administered Dose
MiceRatsMarmosets
MaleFemaleMaleFemaleMaleFemale
0–48 h0–120 h
TicagrelorNDNDNDNDNQ0.1
M11.380.040.30.60.80.7
M20.950.010.40.30.040.2
M3aNDNDNDND0.10.1
M4aNDNDNDND0.40.5
M5 (AR-C133913)0.480.031.21.63.92.8
M7aNDND0.230.04NQ0.08
M7bNDND0.080.01NQNQ
M7dNDNDNDNDNQ0.02
M10aNDND0.090.08NQNQ
M10bNDND0.250.25NQ0.1
M8 (AR-C124910)NDNDNDNDNQNQ
M110.680.040.40.70.10.2
M120.300.020.40.41.31.1
M13NDNDNDNDNQ0.04
Othersa0.730.071.20.50.50.8
  • ND, not detected; NQ, detected by LC-MS/MS only, not quantifiable by radiodetector.

  • a Sum of total uncharacterized radioactivity.