Clinical Study

Efficacy and Pharmacologic Data of Second-Generation Tyrosine Kinase Inhibitor Nilotinib in BCR-ABL-Positive Leukemia Patients with Central Nervous System Relapse after Allogeneic Stem Cell Transplantation

Table 2

Pharmacokinetic data.

PatientNilotinib csf concentration [ng/mL], (range)Nilotinib plasma concentration [ng/mL], (range)Nilotinib csf/plasma ratio [%], (range)Csf protein concentration [g/L]Plasma protein concentration [g/L]Free nilotinib in plasma concentration [ng/mL]* Nilotinib csf concentration/free nilotinib plasma concentration [%,]*

14 (3.6–15)1640 (1544–1736)0.26 (0.23–0.84)0.49 (0.31–0.75)76 (69–77)32.812
213 (4–18)955 (734–1176)0.83 (0.54–1.52)0.40 (0.34–0.89)65 (56–69)19.168
37 (6–9)1159 (1082–1237)0.63 (0.5–0.79)0.50 (0.28–0.67)59 (56–67)23.230
42.7 (1.5–4.8)682 (430–1034)0.42 (0.26–0.58)0.23 (0.19–0.31)71 (62–78)13.620

All values are given as median.
*Unbound (=free) nilotinib concentration calculated by using published nilotinib protein binding of 98%.