Table 3.

Pharmacokinetic evaluation (mean ± SD) of EKB-569 and the N-desmethyl metabolite on day 15

Cmax, ng/mLAUC, h ng/mLt1/2
25 mg EKB-569 FOLFIRIEKB-56916.6 ± 9.8235.9 ± 138.522.4 ± 9.4
n = 16n = 16n = 11
N-desmethyl2.5 ± 1.627.6 ± 25.212.9 ± 4.8
Metaboliten = 12n = 12n = 7
35 mg EKB-569 FOLFIRIEKB-56926.7 ± 12.1398.0 ± 164.314.4 ± 2.7
n = 7n = 7n = 7
N-desmethyl2.9 ± 1.842.9 ± 26.713.5 ± 3.3
Metaboliten = 7n = 7n = 7
50 mg EKB-569 mod. FOLFIRIEKB-56954.6 ± 26.8774.3 ± 439.115.6 ± 3.0
n = 3n = 3n = 3
N-desmethyl5.5 ± 2.181.8 ± 28.513.8 ± 0.3
Metaboliten = 3n = 3n = 3