Skip to main content

Table 1 Summary of preclinical PK parameters of nilotinib after a single intravenous or oral dose in preclinical species. Data, mean ± SD

From: Preclinical pharmacokinetic evaluation to facilitate repurposing of tyrosine kinase inhibitors nilotinib and imatinib as antiviral agents

PK parameter C57BL/6 mice Prairie dogs Cynomolgus monkeys
IV Dose (mg/kg) 10 10 10
No. of animals 3a 5 3
T1/2 (h) 1.81 6.51 ± 2.97 7.79 ± 0.71
MRT (h) 2.21 6.7 ± 2.9 8.9 ± 1.1
CL (ml/hr./kg) 131.14 190 ± 77 639 ± 141
Vss (ml/kg) 289.77 1157 ± 326 5737 ± 1783
AUC0-inf (ng.hr./ml) 76,252 57,551 ± 15,508 16,135 ± 3296
Oral Dose (mg/kg) 10b 20b 10c 10c
No. of animals 3a 5 6 3
Tmax (h) 0.50 7.2 ± 1.79 5.6 ± 2.19 1.67 ± 0.58
Cmax (ng/ml) 17,979 1673 ± 315 951 ± 255 410 ± 46
Apparent T1/2 (h) 2.94 7.57 ± 2.01 3.5 ± 0.6 5.16 ± 0.52
AUC0-inf (ng.hr./ml) 38,366 27,991 ± 6842 9329 ± 3630 2103 ± 468
Bioavailability (%) 50 24 16 13
  1. aper time point; boral dose prepared in NMP/PEG 300; coral dose prepared in Avicel/HPMC