TABLE 5

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

MetabolitesPercentage of Administered Dose
MiceRatsMarmosets
MaleFemaleMaleFemaleMaleFemale
0–24 h0–48 h
Ticagrelor32.933.534.547.923.629.5
M1NDNDNDND0.4ND
M4aNDNDNDND0.1ND
M5 (AR-C133913)13.94.025.66.13.12.8
M7a8.4615.10.81.10.80.6
M7bNDND0.60.30.60.3
M7c4.096.850.5NDNQNQ
M7dNDND3.62.42.71.8
M7eNDND2.11.91.40.8
M8 (AR-C124910)27.729.54.96.02.83.8
M9aNDND0.70.2NQ0.1
M10a**1.11.51.10.8
M10b7.255.532.12.10.91.4
M10cNDNDNDND0.2ND
M10dNDND0.7ND0.20.2
M12**0.61.11.01.0
M13NDND6.98.54.84.3
Othersa1.280.409.02.74.83.7
  • ND, not detected; NQ, detected by LC/MS only, not quantifiable by radiodetector.

  • * M12 coeluted with M5; M7a coeluted with M10a in mice samples.

  • a Sum of total uncharacterized radioactivity.