Table 3. Geometric mean (%CV) day 14 telatinib and BAY 60–8246 pharmacokinetic parameters after oral administration of telatinib.
Telatinib | |||||||
Dose | 75 mg BID | 150 mg BID | 300 mg BID | 600 mg BID | 900 mg BID | 1200 mg BID | 1500 mg BID |
n | 4 | 6 | 6 | 11 | 12 | 6 | 12 |
Mesylate tablet | 25 mg | 25 mg | 25 mg | 150 mg | 150 mg | 150 mg | 150 mg |
Cmax (mg l−1) | 0.212 (140%) | 0.219 (80%) | 0.389 (153%) | 0.810 (87%) | 1.275 (57%) | 1.144 (40%) | 0.964 (83%) |
tmax (h)a | 2.1 (2.0–3.1) | 3.0 (0.52–5.5) | 1.5 (0–8.5) | 2.1 (1.0–4.2) | 2.0 (0.5–8.1) | 2.5 (1–4.3) | 2.5 (0.6–6.0) |
AUC0–tn (mg h l−1) | 1.38 (150%) | 1.75 (84%) | 1.92 (142%) | 5.43 (68%) | 7.41 (51%) | 7.10 (31%) | 6.17 (80%) |
AUC0–12 (mg h l−1) | 1.39 (146%) | 1.73 (81%) | 2.86 (176%)b | 5.43 (68%) | 7.30 (52%) | 7.26 (31%) | 6.29 (84%) |
t1/2 (h) | 7.4 (33%) | 10.9 (66%)† | 8.0 (58%)b | 8.7 (46%) | 5.6 (62%)b | 5.6 (100%) | 6.6 (65%) |
BAY 60–8246 | |||||||
Cmax (mg l−1) | 0.02 (202%) | 0.018 (89%) | 0.021 (133%) | 0.084 (140%) | 0.216 (74%) | 0.226 (87%) | 0.102 (147%) |
tmax (h)a | 3.0 (0.5–6.0) | 2.5 (1.0–12.3) | 1.5 (0–8.5) | 2.1 (0.6–10) | 3.7 (1.0–8.6) | 4.0 (2.1–4.3) | 3.5 (0.5–6.1) |
AUC0–tn (mg h l−1) | 0.125 (333%)c | 0.157 (74%) | 0.115 (113%)b | 0.650 (128%) | 1.27 (79%) | 1.66 (81%) | 0.74 (155%) |
AUC0–12 (mg h l−1) | 0.153 (232%) | 0.155 (72%) | 0.219 (58%)b | 0.650 (128%) | 1.25 (80%) | 1.71 (84%) | 0.76 (160%) |
AUC0–12=area under the plasma concentration versus time curve from time 0–12 h; AUC0–tn=area under the plasma concentration versus time curve from time 0 to last data point; BID=two times daily; Cmax=maximum plasma concentration; %CV=percent coefficient of variation; tmax=time to reach maximum plasma concentration; t1/2=terminal half-life.
Median (range).
Sample size reduced by 2.
Sample size reduced by 1.