TABLE 3

Estimated exposures to apixaban and O-demethyl apixaban sulfate (M1) after oral administration of [14C]apixaban (20 mg) in group 1 (n = 6) and group 2 (n = 4, with bile collection) male subjects

Time
Total Radioactivity
[Apixaban]a
[M1]a
AUC(apixaban)T1T2a
AUC(M1)T1T2a
AUC(M1)0-48 h/AUC(apixaban)0-48 h
G1
G2
G1
G2
G1
G2
G1
G2
G1
G2
G1
G2
dpm/ml μM μM · h
1 h 6120 7540 1.084 1.336 0.018 0.021 0.542 0.668 0.009 0.011
6 h 5280 4780 0.791 0.718 0.150 0.128 4.687 5.135 0.421 0.373
12 h 2750 2390 0.354 0.308 0.141 0.118 3.436 3.078 0.872 0.740
24 h 935 885 0.108 0.097 0.061 0.054 2.773 2.429 1.207 1.034
48 h 275 265 0.029 0.025 0.021 0.022 1.640 1.471 0.974 0.916
0-48 h
13.078
12.780
3.483
3.073
0.2663
0.2405

  • G1, group 1; G2, group 2.

  • ↵ a Concentration is estimated from the relative distribution of apixaban or M1 in the plasma, the total concentration of radioactivity, and the specific activity (5.44 μCi/mg) of the administered drug. AUCT1—T2 is estimated from the concentration in plasma at limited time points (1, 6, 12, 24, and 48 h) using the trapezoidal rule.