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. 2008 Nov 11;99(10):1579–1585. doi: 10.1038/sj.bjc.6604724

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.

a

Median (range).

b

Sample size reduced by 2.

c

Sample size reduced by 1.