TABLE 1

Mean (S.D.) pharmacokinetic parameters and total radioactivity of ibrutinib and PCI-45227

ParameterMean (S.D.)
IbrutinibPCI-45227Total Radioactivity
BloodPlasmaBloodPlasmaBloodPlasma
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Cmax (ng/ml)33.9 (19.1)37.1 (22.4)49.6 (9.3)43.5 (9.01)480 (72.5)a634 (87.9)a
tmax (hour)b0.52 (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)NANA248 (50.3)227 (56.0)NA3690 (434)c
AUClast (ng⋅h/ml)52.0 (32.9)61.5 (39.2)280 (55.0)257 (61.5)1932 (1054)c6821 (908)c
AUC (ng⋅h/ml)59.6 (31.6)70.5 (37.8)283 (54.7)259 (60.7)dd
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.