Table 1.
Pharmacokinetic Parameters for Belinostat After 30 Minutes of Intravenous Infusion
Study Time | Parameter* | Dose Level (mg/m2) |
|||
---|---|---|---|---|---|
600 | 900 | 1,200 | 1,400 | ||
Day 1 | No. of patients | 3 | 3 | 6 | 22 |
Cmax, ng/mL | 28,052 ± 2,710 | 31,308 ± 9,443 | 48,800 ± 16,024 | 58,234 ± 17,865 | |
tmax, hours | 0.35 | 0.42 | 0.42 | 0.45 | |
AUC0-5 hours, h · ng/mL | 18,929 ± 136 | 21,796 ± 5,490 | 36,887 ± 10,540 | 45,596 ± 13,910 | |
AUC0-24 hours, h · ng/mL | 19,499 ± 370 | 22,267 ± 5,485 | 38,988 ± 11,781 | 47,503 ± 14,044 | |
t1/2, hours | 3.54 ± 0.34 | 4.07 ± 0.39 | 4.14 ± 0.42 | 3.49 ± 0.73 | |
Cl, L/h | 52.6 ± 3.75 | 70.5 ± 17.9 | 54.6 ± 15.8 | 54.1 ± 18.0 | |
Vz, L | 268 ± 26.6 | 409 ± 76.7 | 305 ± 186 | 283 ± 151 | |
Day 5 | AUC0-5 hours, h · ng/mL | 17,770 ± 1,323 | 20,485 ± 4,965 | 32,530 ± 8,054 | 52,555 ± 16,535 |
Day 5/day 1† | AUC ratio | 0.94 | 0.94 | 0.88 | 1.15 |
Abbreviations: AUC, area under the serum concentration-time curve; AUC0-t, AUC from 0 to t hours; Cmax, maximum serum concentration; Cl, clearance; t1/2, terminal half-life; tmax, time to maximum serum concentration; Vz, volume of distribution.
Mean ± standard deviation except for tmax.
AUC ratio is calculated based on AUC0-5 hours on day 5 divided by AUC0-5 hours on day 1.