Parameter | Mean (S.D.) | |||||
---|---|---|---|---|---|---|
Ibrutinib | PCI-45227 | Total Radioactivity | ||||
Blood | Plasma | Blood | Plasma | Blood | Plasma | |
% | % | % | % | % | % | |
Cmax (ng/ml) | 33.9 (19.1) | 37.1 (22.4) | 49.6 (9.3) | 43.5 (9.01) | 480 (72.5)a | 634 (87.9)a |
tmax (hour)b | 0.52 (0.50–1.50) | 0.52 (0.50–1.50) | 0.78 (0.50–1.50) | 0.78 (0.50–1.50) | 0.78 (0.50–1.50) | 0.77 (0.50–1.50) |
tlast (hour) | 17.34 (3.26) | 17.34 (3.26) | 56.01 (12.39) | 56.01 (12.39) | 11.34 (6.89) | 72.03 (0.03) |
AUC24 (ng⋅h/ml) | NA | NA | 248 (50.3) | 227 (56.0) | NA | 3690 (434)c |
AUClast (ng⋅h/ml) | 52.0 (32.9) | 61.5 (39.2) | 280 (55.0) | 257 (61.5) | 1932 (1054)c | 6821 (908)c |
AUC∞ (ng⋅h/ml) | 59.6 (31.6) | 70.5 (37.8) | 283 (54.7) | 259 (60.7) | —d | —d |
t1/2 (hour) | 3.33 (0.98) | 3.14 (0.81) | 8.45 (0.84) | 8.37 (0.88) | 25.79 (35.93) | 47.25 (11.60) |
Vd/F (liter) | 14,385 (9102) | 11,038 (5485) | 708 (154) | 941 (161) | ||
CL/F (l/h) | 2825 (1258) | 2443 (1188) | 46.3 (38.7) | 14.2 (2.49) | ||
CLR (l/h) | 0.00365 (0.00156) |
AUClast, area under the concentration-time curve from time 0 to time of the last quantifiable concentration; AUC∞, area under the concentration-time curve from time 0 to infinite time; AUC24, area under the concentration-time curve from time 0 to 24 hours; Cmax, maximum concentration; CL/F, total clearance of drug after extravascular administration; CLR, renal clearance of drug; NA, not applicable; tlast, time to last quantifiable concentration; tmax, time to reach the maximum concentration; t1/2, elimination half-life; Vd/F, apparent volume of distribution based on the terminal phase.
↵a ng⋅Eq/ml.
↵b Median (range).
↵c ng⋅Eq⋅h/ml.
↵d not calculated.