Pharmacokinetics
Pharmacokinetic data after single dose palbociclib were collected and
analyzed for a total of 34 patients (7 at 50 mg/m2, 21
at 75 mg/m2, and 6 at 95 mg/m2).
Data after repeated palbociclib doses were available for a total of 27
patients (6 at 50 mg/m2, 18 at 75
mg/m2, and 3 at 95 mg/m2). The
palbociclib plasma concentration-time profiles are depicted for each
dosing group in Supplementary Figure S1 , and the associated
pharmacokinetic parameters are reported in Table 6 .
Palbociclib was absorbed with a mean Tmax between 4.9
and 6.6 h post-dose, and exhibited an elimination with a mean half-life
between 11.3 and 19.5 h and a mean apparent oral clearance ranging from
26.8 and 52.6 L/h/m2. Within 50 and 95
mg/m2, following single and repeated doses, mean
palbociclib Cmax and AUC0-Tlastincreased in proportional manner; however, large inter-individual
variabilities were observed among the pharmacokinetic parameters.